tag:blogger.com,1999:blog-89606966290072912422024-03-18T02:54:44.551-07:00ORGANIC SPECTROSCOPY INTERNATIONALOrganic Chemists from Industry and academics to Interact on Spectroscopy Techniques for Organic Compounds ie NMR, MASS, IR, UV Etc. Starters, Learners, advanced, all alike, contains content which is basic or advanced, by Dr Anthony Melvin Crasto, Worlddrugtracker, email me ........... amcrasto@gmail.com, call +91 9323115463 India skype amcrasto64DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.comBlogger1784125tag:blogger.com,1999:blog-8960696629007291242.post-34011186017891653302023-03-09T18:48:00.002-08:002023-03-09T18:48:34.955-08:00Smartchem by Row2 Technologies<p> </p>
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</div><div><br /></div><div class="separator" style="clear: both; text-align: center;"><iframe allowfullscreen='allowfullscreen' webkitallowfullscreen='webkitallowfullscreen' mozallowfullscreen='mozallowfullscreen' width='563' height='468' src='https://www.blogger.com/video.g?token=AD6v5dwUOFNUq5QnqdAET8tU04lP3DznGJ0YaIsfMLe8fdTMabOTYFr0StebH90EF8wEUyjcNgjl_BddJCUdHXyL9g' class='b-hbp-video b-uploaded' frameborder='0'></iframe></div><br /><div><br /></div>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com2tag:blogger.com,1999:blog-8960696629007291242.post-58516268931198939322023-01-24T18:48:00.005-08:002023-01-24T18:48:38.001-08:00Indira Diversity award 2023 for never give up attitude in life, 21 Jan 2023.<p> </p><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEiLw3y_HhotuC2mEjL8aYDg_IU0xZfcjEUkJMW32jNuI4zEK3YnxEfMV_ETxO_tlaxSWEHxf42k1nL0ud1zNSC55dzthgjmnyyWMTyw1HstilX1q99p_yLNoqlZ-JuoXPeNLbHGYg66G0SLOfw1B3m0TT-SaQQ8n4qG6ckvGCio0Aas6I91E52eLECN_A/s1707/INDIRA%2021%20JAN%202023.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="1707" data-original-width="1280" height="422" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEiLw3y_HhotuC2mEjL8aYDg_IU0xZfcjEUkJMW32jNuI4zEK3YnxEfMV_ETxO_tlaxSWEHxf42k1nL0ud1zNSC55dzthgjmnyyWMTyw1HstilX1q99p_yLNoqlZ-JuoXPeNLbHGYg66G0SLOfw1B3m0TT-SaQQ8n4qG6ckvGCio0Aas6I91E52eLECN_A/w537-h422/INDIRA%2021%20JAN%202023.jpg" width="537" /></a></div><br /><p></p><p><br /></p><h2 aria-label="false" class="element wsite-content-title editable-text cke_editable cke_editable_inline cke_contents_ltr cke_focus cke_show_borders" id="617593517315496600" role="textbox" spellcheck="true" style="background-color: white; color: #333333; cursor: text; font-family: "Open Sans", sans-serif; font-size: 22px; font-weight: 400; line-height: 1.2; margin: 0px; outline: none; overflow-wrap: break-word; padding: 0.5em 0px 0.2em;" tabindex="0"><span color="rgba(0, 0, 0, 0.9)">Proud to recieve Indira Diversity award 2023 for never give up attitude in life, </span><span color="rgba(0, 0, 0, 0.9)">21 Jan 2023. Indira institute Pune India, </span><span color="rgba(0, 0, 0, 0.9)">Indira Diversity Awards-2023", to witness the presence of super achievers who have contributed to our country's glory, along with organizations that have celebrated inclusivity and diversity,</span></h2>
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2.56 (s, 2H), 4.05 (m, 4H), 4.81 (d, J = 25.02 Hz, 2H), 6.76 (s, 1H), 6.93 (s, 1H). </p><p>13C
NMR (125 MHz, CDCl3) δ = 24.7, 27.5, 31.9, 37.9, 42.2, 43.3, 105.2, 117.8, 124.6,
145.4, 147.7, 149.9, 150.8, 154.6, 156.9, 171.3.</p><p><br /></p><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhp4BEF_dlnKE6nzKaJ0VUsntGu-oFZLmJCM6F0FiMZtZ_aZJbG_YeijMwENRFxgg1zaTYw3RYcba8DbgycDgh-ZRCa3L8lKFuvKJkHnGiDihIQxODnL42P-aArLrzaRqXD_hXZdJ2ocNg1PiQal0jCbJhQcg-ZzTQ2ALRpiwgstgbMzF2mi_d5-yQWuw/s716/str1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="452" data-original-width="716" height="368" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhp4BEF_dlnKE6nzKaJ0VUsntGu-oFZLmJCM6F0FiMZtZ_aZJbG_YeijMwENRFxgg1zaTYw3RYcba8DbgycDgh-ZRCa3L8lKFuvKJkHnGiDihIQxODnL42P-aArLrzaRqXD_hXZdJ2ocNg1PiQal0jCbJhQcg-ZzTQ2ALRpiwgstgbMzF2mi_d5-yQWuw/w582-h368/str1.jpg" width="582" /></a></div><div class="separator" style="clear: both; text-align: center;">1HNMR CDCL3</div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEj8OLGSJNtDrJLuxqBt-_yhQ0DsCnHRbOy-UwrFvU3aPArwcG02Gq6K-ZDbqSeKLu5bQF7nUmUeG5kQTgOUJP11ejF0SI482tWVYF1LsqQ6q93i2P_KkdZV7m5UVpKGLq6At9QAwRE9y5kLZXTd9zWlVAC_BDfXpWbOs_Fdc_2HR42R8sbYdJVou5BiWA/s724/str1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="453" data-original-width="724" height="377" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEj8OLGSJNtDrJLuxqBt-_yhQ0DsCnHRbOy-UwrFvU3aPArwcG02Gq6K-ZDbqSeKLu5bQF7nUmUeG5kQTgOUJP11ejF0SI482tWVYF1LsqQ6q93i2P_KkdZV7m5UVpKGLq6At9QAwRE9y5kLZXTd9zWlVAC_BDfXpWbOs_Fdc_2HR42R8sbYdJVou5BiWA/w603-h377/str1.jpg" width="603" /></a></div><div class="separator" style="clear: both; text-align: center;">13C NMR CDCL3</div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgbyr1KM7nW2hxqPQD2ROTq7ogf2B2MnUiqpxTRw7tysn2Qv1IJjMKzWBe7blKA5s1LwI6tlw0kO_lGzU6M8Gx4JL7hgvqKAXqNOxkiXBHlvmfH4SKWGdi6uPhvTwKp-mB7jmP5roqXK4KrcHyyJp9jRxDnllPSGRy9rEe1GSxYCguUxgMOZ24P01CP3Q/s683/str1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="315" data-original-width="683" height="273" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgbyr1KM7nW2hxqPQD2ROTq7ogf2B2MnUiqpxTRw7tysn2Qv1IJjMKzWBe7blKA5s1LwI6tlw0kO_lGzU6M8Gx4JL7hgvqKAXqNOxkiXBHlvmfH4SKWGdi6uPhvTwKp-mB7jmP5roqXK4KrcHyyJp9jRxDnllPSGRy9rEe1GSxYCguUxgMOZ24P01CP3Q/w590-h273/str1.jpg" width="590" /></a></div><div class="separator" style="clear: both; text-align: center;">13C DEPT NMR CDCL3</div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEghdpo3Ot4Y6_6NRVkX_FGsi5qb2FIIgNPhUZBj4f3rs3Ar8LPN2wA5BHkOYRRkEnkOfxg8HUnIz_y2-nXRyy6F1dS3lnabgcONxGPC3em7TGkeWit28nUdFf-aucRgS7lIKATWZtzilJDQrCnFSCbs9JWT0k0pmcly8G60W67zqInyYKZH8KpNXTqeUg/s700/str1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="436" data-original-width="700" height="343" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEghdpo3Ot4Y6_6NRVkX_FGsi5qb2FIIgNPhUZBj4f3rs3Ar8LPN2wA5BHkOYRRkEnkOfxg8HUnIz_y2-nXRyy6F1dS3lnabgcONxGPC3em7TGkeWit28nUdFf-aucRgS7lIKATWZtzilJDQrCnFSCbs9JWT0k0pmcly8G60W67zqInyYKZH8KpNXTqeUg/w551-h343/str1.jpg" width="551" /></a></div><div class="separator" style="clear: both; text-align: center;">H H COSY NMR CDCL3</div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg3xVzEAmFRzcCC-C5Y1SUG7k8Sw6CyDmkhSdS0wgyrM84ZPevr-cR0Dn2UQAajq1TqP29v5OvFxdKJ4PDDB-ujOkj2J9DXk0CCMIUWBaOvuHxIfhtDZv49cFVhTM4eFbcbskmhrcQjhqvdabHezLUhVi_4IVDzHT_UvBOqwu7jY1if_VU_C4d8pUwYxQ/s718/str1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="450" data-original-width="718" height="363" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg3xVzEAmFRzcCC-C5Y1SUG7k8Sw6CyDmkhSdS0wgyrM84ZPevr-cR0Dn2UQAajq1TqP29v5OvFxdKJ4PDDB-ujOkj2J9DXk0CCMIUWBaOvuHxIfhtDZv49cFVhTM4eFbcbskmhrcQjhqvdabHezLUhVi_4IVDzHT_UvBOqwu7jY1if_VU_C4d8pUwYxQ/w577-h363/str1.jpg" width="577" /></a></div><div class="separator" style="clear: both; text-align: center;">HSQC NMR CDCL3</div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEghc6NRWPrpLe8ecLEdFyWZasYrRD5WQzI4Cz29JPDHxiXMx4AxLwaDc1hyWX-S5JQYLRQVtVknYyHC_bn5pCJGC5uZG7aYP2hSawnp6aOdko14RBnrBEpTSNqr35e8ujcbJvOuiL_3GI5cJmS_I6g-k3goHYWE_wB_TSpjOCQS8-GCSOKIU476Qg7WiQ/s551/str1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="457" data-original-width="551" height="467" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEghc6NRWPrpLe8ecLEdFyWZasYrRD5WQzI4Cz29JPDHxiXMx4AxLwaDc1hyWX-S5JQYLRQVtVknYyHC_bn5pCJGC5uZG7aYP2hSawnp6aOdko14RBnrBEpTSNqr35e8ujcbJvOuiL_3GI5cJmS_I6g-k3goHYWE_wB_TSpjOCQS8-GCSOKIU476Qg7WiQ/w564-h467/str1.jpg" width="564" /></a></div><div class="separator" style="clear: both; text-align: center;">HMBC NMR CDCL3</div><br /><div class="separator" style="clear: both; text-align: center;"><br /></div><br /><div class="separator" style="clear: both; text-align: center;"><br /></div><br /><div class="separator" style="clear: both; text-align: center;"><br /></div><br /><div class="separator" style="clear: both; text-align: center;"><br /></div><br /><div class="separator" style="clear: both; text-align: center;"><br /></div><br />DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com6tag:blogger.com,1999:blog-8960696629007291242.post-88478896674622783992022-04-26T22:55:00.002-07:002022-04-26T22:55:31.749-07:001,3-dichloro-2-fluorobenzene<p> </p><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhyvYCcz6QFNMmxb2951vBGd6HRf067R-BgTZW0eXtPMfkNVD6eS2w4z1Y_MBnk2ilzIU5QUMy0p_zP6xhCYyVDy4jbRgfll7soD3AZ9v1DpxhyGf4RIERAr1D6iwEZ4BLSl-4wmBHcbbere9eBcSPmfGq1OqNmUYwHbzyKxDQCTxq1NBxy_qHLxn9yIg/s204/str1.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="200" data-original-width="204" height="264" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhyvYCcz6QFNMmxb2951vBGd6HRf067R-BgTZW0eXtPMfkNVD6eS2w4z1Y_MBnk2ilzIU5QUMy0p_zP6xhCYyVDy4jbRgfll7soD3AZ9v1DpxhyGf4RIERAr1D6iwEZ4BLSl-4wmBHcbbere9eBcSPmfGq1OqNmUYwHbzyKxDQCTxq1NBxy_qHLxn9yIg/w269-h264/str1.JPG" width="269" /></a></div><br /><p><br /></p><p><b style="background-color: white;">Compound Name:</b><br style="background-color: white;" /><span style="background-color: white;">1,3-dichloro-2-fluorobenzene</span><br style="background-color: white;" /><br style="background-color: white;" /><b style="background-color: white;">Molecular Formula: </b><span style="background-color: white;">C</span><sub style="background-color: white;">6</sub><span style="background-color: white;">H</span><sub style="background-color: white;">3</sub><span style="background-color: white;">Cl</span><sub style="background-color: white;">2</sub><span style="background-color: white;">F</span><br style="background-color: white;" /><br style="background-color: white;" /><b style="background-color: white;">Molecular Weight: </b><span style="background-color: white;">165.0</span><br style="background-color: white;" /><br style="background-color: white;" /><b style="background-color: white;">CAS Registry No.:</b><span style="background-color: white;"></span><br style="background-color: white;" /><span style="background-color: white;">2268-05-5</span><br style="background-color: white;" /></p><p><span style="background-color: white;"><br /></span></p><p><span style="background-color: white;">1H NMR CDCL3</span></p><p><span style="background-color: white;"><br /></span></p><p></p><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg1mPQ1JwYo5lLUKizT16yr7H0rKltRd-6O5ORKVm9v5szdjtE8OE7-XJtTK65snwIRzq3HGk8_pyFBfWbM1pAlwa23eBmo9NDUtjA7k2ffVQMTNTLakogQXcYvI15VFRFdpCTaYLnlJ0Y2GDoX7Luyt0rQvm7ivMCP1VvDq3gf2yX7dgVc126TJexMDg/s571/str1.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="395" data-original-width="571" height="389" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg1mPQ1JwYo5lLUKizT16yr7H0rKltRd-6O5ORKVm9v5szdjtE8OE7-XJtTK65snwIRzq3HGk8_pyFBfWbM1pAlwa23eBmo9NDUtjA7k2ffVQMTNTLakogQXcYvI15VFRFdpCTaYLnlJ0Y2GDoX7Luyt0rQvm7ivMCP1VvDq3gf2yX7dgVc126TJexMDg/w563-h389/str1.JPG" width="563" /></a></div><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg1EtL30Tr81GIWnK257pplXiZ2ALGVllhXJ5dBRyECQ10E1RxARj1RbW5SYeWAkDhd4ZYOLvJGUH3L3TyH80XLgb0l_wZ9O4g5RL3CI6QFCx95_fZyDo6esQw2nkYrX8-f74vWt2s8tvN4lUfPbbDpXlhIUe7xDsw0YF1TOcHM0_JnFfvAOInkqfz49g/s233/str2.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="225" data-original-width="233" height="471" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg1EtL30Tr81GIWnK257pplXiZ2ALGVllhXJ5dBRyECQ10E1RxARj1RbW5SYeWAkDhd4ZYOLvJGUH3L3TyH80XLgb0l_wZ9O4g5RL3CI6QFCx95_fZyDo6esQw2nkYrX8-f74vWt2s8tvN4lUfPbbDpXlhIUe7xDsw0YF1TOcHM0_JnFfvAOInkqfz49g/w488-h471/str2.jpg" width="488" /></a></div><br /><span style="background-color: white;"><br /></span><p></p><table border="0" style="color: black; width: 100%px;"><tbody><tr><td></td><td>399.65 MHz</td></tr><tr><td>C<sub>6</sub> H<sub>3</sub> Cl<sub>2</sub> F</td><td>0.040 g : 0.5 ml CDCl<sub>3</sub></td></tr><tr><td colspan="2"><span style="font-size: medium;"><b>1,3-dichloro-2-fluorobenzene</b></span></td></tr></tbody></table><hr /><pre> <b>Hz ppm Int.</b>
</pre><p></p><pre> 2926.51 7.323 808
2919.92 7.307 846
2918.33 7.303 1000
2911.87 7.287 952
2905.15 7.270 25
2817.26 7.050 318
2815.67 7.046 313
2809.45 7.030 388
2808.84 7.029 347
2807.74 7.026 400
2801.03 7.009 244
2799.44 7.005 236</pre><p><span style="background-color: white;"><br /></span></p><p><span style="background-color: white;">13C NMR</span></p><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEggPJqLSgjoP5hy11JwF1JqyDfWPuBlKw06ic4kVXeYCRTKkdnC-AEI7_Ocl8-mFBKNf4HXAwKbyfXiGl11cz01B18HNsUruqBkkEt-1k8pUyx8B_mz_B__Oi-CB-qQ_eSwHfqXhf_IA3i0skLzYzw1tJXNXA8An2bumMlYsznZhFY2uOWwicoH4xjLKg/s329/str2.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="329" data-original-width="237" height="526" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEggPJqLSgjoP5hy11JwF1JqyDfWPuBlKw06ic4kVXeYCRTKkdnC-AEI7_Ocl8-mFBKNf4HXAwKbyfXiGl11cz01B18HNsUruqBkkEt-1k8pUyx8B_mz_B__Oi-CB-qQ_eSwHfqXhf_IA3i0skLzYzw1tJXNXA8An2bumMlYsznZhFY2uOWwicoH4xjLKg/w380-h526/str2.jpg" width="380" /></a></div><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEirhY_Va1-JD5FFgK-sspPbDFbp-54ZYUGxbiG8AvmwCbx-2y8lnEPdBnc5eQDzZFAdG_PZbQDwrPwE4rjfhiBx4LJ4CTtor28SzHBODrk97BZzfGd6Es2z1TfUrlAAsO567qntYhal6WPlHj1ZbUIADttiwWhTHLldm7NEgzMVI6Wn2bGl8FrfmTSffg/s557/str1.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="380" data-original-width="557" height="392" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEirhY_Va1-JD5FFgK-sspPbDFbp-54ZYUGxbiG8AvmwCbx-2y8lnEPdBnc5eQDzZFAdG_PZbQDwrPwE4rjfhiBx4LJ4CTtor28SzHBODrk97BZzfGd6Es2z1TfUrlAAsO567qntYhal6WPlHj1ZbUIADttiwWhTHLldm7NEgzMVI6Wn2bGl8FrfmTSffg/w575-h392/str1.JPG" width="575" /></a></div><br /><table border="0" style="color: black; width: 100%px;"><tbody><tr><td>100.53 MHz</td></tr><tr><td><br /><br /><br /></td><td>0.040 g : 0.5 ml CDCl<sub>3<br /><br /><br /><br /></sub></td></tr></tbody></table><p><span style="background-color: white;">MASS</span></p><p></p><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgqsbe3bTJ6wHCoHHexrQBkRwnsZV31OKPBAOEMDdKXGdhgFAWH5UsHPD36YBZDUfGhQGGevoSaeyy0Uz2U3QNB6rnAqqqY2_P8CAXxMEle3OiE_B8JAeElXgwKj2gJm9Wj-nP-ydnq40s7dVACY9k5DsmjhviWJShvrBdwA1t5Ua5Z2HdXJ5zcES9LmA/s609/str1.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="446" data-original-width="609" height="393" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgqsbe3bTJ6wHCoHHexrQBkRwnsZV31OKPBAOEMDdKXGdhgFAWH5UsHPD36YBZDUfGhQGGevoSaeyy0Uz2U3QNB6rnAqqqY2_P8CAXxMEle3OiE_B8JAeElXgwKj2gJm9Wj-nP-ydnq40s7dVACY9k5DsmjhviWJShvrBdwA1t5Ua5Z2HdXJ5zcES9LmA/w538-h393/str1.JPG" width="538" /></a></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;">IR NUJOL</div><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgMknnaKjgFfkhcKyzVmPBjm0xV49dIFJwlsKaM2HF_HT4eFjvjLXm91dX4n_MhRYWo2T9UYlQdFZNrb2YBiEDSD3Zhpmd7aLOwhE2gPCADcRVORjjvQr7Y19mETbad9bomFK7X6fge2P64kLlcR-EJyNqAPV9jvihtYkiuVh7wubBbDPs_MKzNoG6Axw/s657/str2.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="486" data-original-width="657" height="409" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgMknnaKjgFfkhcKyzVmPBjm0xV49dIFJwlsKaM2HF_HT4eFjvjLXm91dX4n_MhRYWo2T9UYlQdFZNrb2YBiEDSD3Zhpmd7aLOwhE2gPCADcRVORjjvQr7Y19mETbad9bomFK7X6fge2P64kLlcR-EJyNqAPV9jvihtYkiuVh7wubBbDPs_MKzNoG6Axw/w553-h409/str2.jpg" width="553" /></a></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;">IR KBR</div><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjtbjVjpzLF9HGReaN8EnE4s0WrjM71HvvFZYPlK8uOmDthE8M4M3QB72G84r4rfmteu1-1ajHsCQenrwU8MvZFApPW9ikHWteJWh3kada9YwIb5_Gb-0e1YsosMgXvfXxiIJ9ZoR40d6hpA6jsyWLyQPA2ej0XfFhvMhycGKLuO_HkPa737QB2MGCYdA/s652/STR3.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="491" data-original-width="652" height="391" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjtbjVjpzLF9HGReaN8EnE4s0WrjM71HvvFZYPlK8uOmDthE8M4M3QB72G84r4rfmteu1-1ajHsCQenrwU8MvZFApPW9ikHWteJWh3kada9YwIb5_Gb-0e1YsosMgXvfXxiIJ9ZoR40d6hpA6jsyWLyQPA2ej0XfFhvMhycGKLuO_HkPa737QB2MGCYdA/w519-h391/STR3.JPG" width="519" /></a></div><br /><span style="background-color: white;"><br /></span><p></p><p><span style="background-color: white;"><br /></span></p><p><span style="background-color: white;">///////</span></p>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com1tag:blogger.com,1999:blog-8960696629007291242.post-47260025412032220542021-12-17T18:29:00.001-08:002021-12-17T18:29:15.420-08:00ZY 19489, MMV 253<p> <a href="http://drugapprovalsint.com/wp-content/uploads/2021/12/str1-7.jpg" style="border: 0px; color: #993366; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px; vertical-align: baseline;"><img alt="str1" class="alignnone size-medium wp-image-15053" height="195" sizes="(max-width: 300px) 100vw, 300px" src="http://drugapprovalsint.com/wp-content/uploads/2021/12/str1-7-300x195.jpg" srcset="http://drugapprovalsint.com/wp-content/uploads/2021/12/str1-7-300x195.jpg 300w, http://drugapprovalsint.com/wp-content/uploads/2021/12/str1-7.jpg 413w" style="border: 0px; box-sizing: border-box; height: auto; margin: 8px 0px 10px; max-width: 100%; padding: 0px; vertical-align: middle;" width="300" /></a></p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;"><img src="https://www.mmv.org/sites/default/files/styles/formula/public/portfolio-project/formula-images/MMV253_0.jpg?itok=1XxUCChw" style="border: 0px; box-sizing: border-box; height: auto; margin: 8px 0px 10px; max-width: 100%; padding: 0px; vertical-align: middle;" /></p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;"><img alt="2-N-(4-cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-5-[(3R)-3,4-dimethylpiperazin-1-yl]-4-N-(1,5-dimethylpyrazol-3-yl)pyrimidine-2,4-diamine.png" src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?cid=92045019&t=l" style="border: 0px; box-sizing: border-box; height: auto; margin: 8px 0px 10px; max-width: 100%; padding: 0px; vertical-align: middle;" /></p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">ZY 19489, MMV 253</p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">C24 H32 FN9, 465.5</p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">CAS 1821293-40-6</p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">MMV253, GTPL10024, MMV674253</p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">N-(4-cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-5-((3R)-2-((1,5-dimethyl-1H-pyrazol-3-yl)amino)-3,4-dimethylpiperazin-1-yl)pyrimidin-2-amine</p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">2-<i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">N</i>-(4-cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-5-[(3<i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">R</i>)-3,4-dimethylpiperazin-1-yl]-4-<i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">N</i>-(1,5-dimethylpyrazol-3-yl)pyrimidine-2,4-diamine</p><ul style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; list-style: none; margin: 0.5em 0px 1em 30px; padding: 0px; vertical-align: baseline;"><li style="border: 0px; margin: 0px; padding: 5px 0px 0px 20px; position: relative; vertical-align: baseline;">N<span style="border: 0px; bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; vertical-align: baseline;">2</span>-(4-Cyclopropyl-5-fluoro-6-methyl-2-pyridinyl)-5-[(3R)-3,4-dimethyl-1-piperazinyl]-N<span style="border: 0px; bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; vertical-align: baseline;">4</span>-(1,5-dimethyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine</li><li class="alt" style="border: 0px; margin: 0px; padding: 5px 0px 0px 20px; position: relative; vertical-align: baseline;">(R)-N<span style="border: 0px; bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; vertical-align: baseline;">2</span>-(4-Cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-N<span style="border: 0px; bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; vertical-align: baseline;">4</span>-(1,5-dimethyl-1H-pyrazol-3-yl)-5-(3,4-dimethylpiperazin-1-yl)pyrimidine-2,4-diamine</li></ul><p><br /></p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">Nature Communications (2015), 6, 6715.</p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;"><a href="https://www.nature.com/articles/ncomms7715" style="border: 0px; color: #222222; margin: 0px; padding: 0px; vertical-align: baseline;">https://www.nature.com/articles/ncomms7715</a></p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">Hameed P., S., Solapure, S., Patil, V. <i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">et al.</i> Triaminopyrimidine is a fast-killing and long-acting antimalarial clinical candidate. <i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">Nat Commun</i> <b style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">6, </b>6715 (2015). https://doi.org/10.1038/ncomms7715</p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;">Synthesis of (R)-N2-(4-cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-N4-(1, 5-dimethyl-1H-pyrazol-3-yl)-5-(3, 4-dimethylpiperazin-1-yl)pyrimidine-2,4-diamine (<b style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">12</b>). (R)-N2-(4-cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-N4-(1,5-dimethyl-1H-pyrazol-3-yl)-5-(3-methylpiperazin-1-yl)pyrimidine-2,4-diamine hydrochloride (compound <b style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">9</b>, 190 mg, 0.42 mmol) was taken in dichloromethane (2 ml) to give a yellow suspension. To this Hunig’s Base (0.184 ml, 1.05 mmol) was added and the suspension turned clear. After 10 min of stirring, reaction mixture turned into a white suspension and then it was concentrated to dryness. Resultant residue was dissolved in ethanol (absolute, 99.5%) (3 ml), and formaldehyde (0.042 ml, 0.63 mmol) was added and stirred for 10 min. To this clear solution, sodium cyanoborohydride (26.4 mg, 0.42 mmol) was added in one portion to get a white suspension. The reaction mixture was concentrated and the crude product was purified through reverse-phase chromatography to get the pure off-white solid of (R)-N2-(4-cyclopropyl-5-fluoro-6-methylpyridin-2-yl)-N4-(1, 5-dimethyl-1H-pyrazol-3-yl)-5-(3,4-dimethylpiperazin-1-yl)pyrimidine-2,4-diamine (80 mg, 40.8%). Yield: 40.8%, purity: >95% by HPLC (ultraviolet at 220 and 254 nm). <span style="border: 0px; bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; vertical-align: baseline;">1</span>H NMR (300 MHz, DMSO-d<span style="border: 0px; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; top: 0.5ex; vertical-align: baseline;">6</span>) <i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">δ</i> 9.26 (s,1H), 8.03 (s, 1H) 8.00 (s, 1H) 7.67 (d, <i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">J</i>=5.1 Hz, 1H) 6.83 (s, 1H) 3.33 (s, 3H) 2.96–2.73 (m, 4H) 2.75–2.50 (m, 1H) 2.38–2.30 (m, 4H) 2.23 (s, 7H) 2.10–1.96 (m, 1H),1.08–1.02 (m, 2H) 1.00 (d, <i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">J</i>=6.2 Hz, 3H) 0.78–0.67 (m, 2H). <span style="border: 0px; bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; vertical-align: baseline;">13</span>C-NMR (126 MHz, DMO-d<span style="border: 0px; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; top: 0.5ex; vertical-align: baseline;">6</span>) <i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">δ</i> 155.30, 154.67, 152.10, 150.93, 148.98, 146.81. 145.29, 141.95, 140.31, 138.81, 124.91, 106.20, 97.07, 58.78, 51.87, 42.16, 35.28, 17.23. 10.99 and 8.77, HRMS (ESI): <i style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">m/z</i> calculated for C<span style="border: 0px; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; top: 0.5ex; vertical-align: baseline;">24</span>H<span style="border: 0px; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; top: 0.5ex; vertical-align: baseline;">32</span>FN<span style="border: 0px; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; top: 0.5ex; vertical-align: baseline;">9</span>+H [M+H]: 466.2765. Found: 466. 2838. Traces of LC-MS, HRMS, <span style="border: 0px; bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; vertical-align: baseline;">1</span>H NMR and <span style="border: 0px; bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; margin: 0px; padding: 0px; position: relative; vertical-align: baseline;">13</span>C-NMR of compound <b style="border: 0px; margin: 0px; padding: 0px; vertical-align: baseline;">12</b> are shown in <a data-track-action="supplementary material anchor" data-track-label="link" data-track="click" href="https://www.nature.com/articles/ncomms7715#MOESM46" style="border: 0px; color: #222222; margin: 0px; padding: 0px; vertical-align: baseline;">Supplementary Figs 1–3</a>.</p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;"> </p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px 0px 1em; vertical-align: baseline;"><img src="http://drugapprovalsint.com/wp-content/uploads/2021/12/str1-5.jpg" style="border: 0px; box-sizing: border-box; height: auto; margin: 8px 0px 10px; max-width: 100%; padding: 0px; vertical-align: middle;" /></p><p style="background-color: white; border: 0px; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0px; padding: 0px; vertical-align: baseline;"><img src="http://drugapprovalsint.com/wp-content/uploads/2021/12/str2-2.jpg" style="border: 0px; box-sizing: border-box; height: auto; margin: 8px 0px 10px; max-width: 100%; padding: 0px; vertical-align: middle;" /></p>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com10tag:blogger.com,1999:blog-8960696629007291242.post-13133484377804817062021-09-03T03:02:00.003-07:002021-09-03T03:07:24.390-07:00THIAMINE, VIT B1<p> </p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img alt="Thiamin.svg" data-mce-src="https://upload.wikimedia.org/wikipedia/commons/thumb/f/f0/Thiamin.svg/220px-Thiamin.svg.png" src="https://upload.wikimedia.org/wikipedia/commons/thumb/f/f0/Thiamin.svg/220px-Thiamin.svg.png" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img alt="Thiamine" data-mce-src="http://www.druglead.com/cds/structure/Thiamine.gif" src="http://www.druglead.com/cds/structure/Thiamine.gif" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">THIAMINE</p><ul class="struct-props" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span class="prop_title">Molecular Formula</span><span id="ctl00_ctl00_ContentSection_ContentPlaceHolder1_RecordViewDetails_rptDetailsView_ctl00_prop_MF">C<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">12</span>H<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">17</span>N<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">4</span>OS</span></li><li style="padding-top: 5px;"><span class="prop_title">Average mass</span>265.354 Da</li></ul><ul style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span title="commonchemistry.cas.org"><a class="external text" data-mce-href="https://commonchemistry.cas.org/detail?cas_rn=" href="https://commonchemistry.cas.org/detail?cas_rn=" rel="nofollow" style="color: #222222;">59-43-8 </a> has cl atom</span></li><li style="padding-top: 5px;"><strong>70-16-6</strong> <a class="synonym_ref" data-mce-href="http://www.ncbi.nlm.nih.gov/sites/entrez?db=pccompound&amp;term=%2270-16-6%22[CompleteSynonym]" href="http://www.ncbi.nlm.nih.gov/sites/entrez?db=pccompound&amp;term=%2270-16-6%22[CompleteSynonym]" style="color: #222222;" target="reference" title="RN">[RN]</a> no cl atom</li></ul><ul class="substanceInfo" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0.5em 0px 1em 30px;"><li class="indexName" style="padding-top: 5px;">Thiazolium, 3-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-5-(2-hydroxyethyl)-4-methyl-, chloride, hydrochloride (1:1:1), Thiamine CL hcl, 67-03-8, (Component: 70-16-6) 1;1;1,</li><li style="padding-top: 5px;">C<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">12</span> H<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">17</span> N<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">4</span> O S . Cl H . Cl</li></ul><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><span class="">3595616</span> <a class="synonym_ref" data-mce-href="http://en.wikipedia.org/wiki/Beilstein_database" href="http://en.wikipedia.org/wiki/Beilstein_database" style="color: #222222;" target="reference" title="Beilstein">[Beilstein]</a></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><strong>3-[(4-Amino-2-methy<wbr></wbr>l-5-pyrimidinyl)met<wbr></wbr>hyl]-5-(2-hydroxyet<wbr></wbr>hyl)-4-methylthiazo<wbr></wbr>lium</strong></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">thiamin hydrochloride<br />Vitamin B1 hydrochloride<br />thiamine hydrochloride<br />aneurin hydrochloride<br />3-(4-amino-2-methyl-5-pyrimidinyl)methyl-5-(2-hydroxyethyl)-4-methylthiazolium chloride hydrochloride</p><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">SPECTROSCOPY</div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str1-4.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str1-4.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><b>Compound Name:</b><br />Thiamin hydrochloride<b>Molecular Formula: </b>C<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">12</span>H<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">17</span>ClN<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">4</span>OS<b>Molecular Weight: </b>300.8<b>CAS Registry No.:</b><br />67-03-8</div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"> MASS</div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str1.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str1.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">13C NMR D2O</div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str1-2.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str1-2.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str2-1.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str2-1.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"> <br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">1</span>H NMR : 400 MHz in DMSO-d<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">6</span></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str2-2.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str2-2.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/09/STR3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/09/STR3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"> <br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"> <br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">IR</div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str1-3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str1-3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str2-3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/09/str2-3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"> <br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">Syn</div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><span style="background-color: white;">HELVETICA CHIMICA ACTA ~ Vol. 73 (1990)</span></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><br /></div><div align="left" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><p style="padding: 0px 0px 1em;">3. 3-1 (4-Amino-2-methylpyrimidin-5-yl)methyl]-5-(2-hydroxyethyl)-4-methylthiazolium Chloride Hydrochlo ride (Thiamine Hydrochloride, la). Compound 4 (7.4 g, 0.05 mol) was dissolved in 100 ml of HCOOH. To this slightly yellow soh, 5a (9.25 g, 0.052 mol) was immediately added at such a rate so that the temp. did not exceed 3540". The mixture was further stirred for 30 min at r.t. and then 25 ml of a freshly prepared sat. soh. of HCI in abs. EtOH was added dropwise. The temp. rose to 35-36O, and the mixture was further stirred for 30 min at r.t.''), The crude mixture was then poured into a 500-ml flask and evaporated at 50" under reduced pressure to give 26.07 g of a green-yellow solid residue, which was taken up in 100 ml of ahs. EtOH. Aq. HCI soh. (25%, 30 ml) was then added and the crude mixture heated on a steam-bath, until a clear soln. was obtained. The soln. was cooled to r.t. and placed overnight in the refrigerator. The resulting white crystals were collected and dried in vucuo to yield 14.56 g (86.3%) of la. M.p. 245-246' (dec.). The mother-liquor was then evaporated at 50O under reduced pressure and the residue taken up in 50 ml of H,O. The aq. phase was then washed twice with 25 ml of CH2C1, and evaporated under reduced pressure to give 3.29 g of a still slightly greenish residue, which was again taken up in 20 ml of abs. EtOH. Aq. HCI soln. (25%, 5 ml) was added and the mixture heated on a steam-bath, until a clear soln. was obtained. It was then cooled to r.t. and kept overnight in the refrigerator. The white crystals were filtered to give 1.42 g (8.4%) of la. M.p. 244-24So(dec.) (combined yieldI2) of la: 94.7% based on 4).</p><p style="padding: 0px 0px 1em;">Recrystallization. The two crops of la were combined and dissolved in 100 ml of warm abs. EtOH. Aq. HCI soh (25 %, 40 ml) was added. The soln. was then allowed to cool slowly to r.t. and kept at Oo overnight. The white crystals were filtered and dried in vucuo at 50" to give 13.6 g (0.04 mol, 80.6 %) of la.</p><p style="padding: 0px 0px 1em;">M.p. 243-244" (dec.). UV: 234 (4.1), 266 (3.9).</p><p style="padding: 0px 0px 1em;">IR (KBr): 3500m, 3430m. 3340m. 3240m. 3065s. 2615m. 1660s, 1607m, 1380m.</p><p style="padding: 0px 0px 1em;">'H-NMR (D,O): 2.54(s,Me);2.62(s,Me);3.19(t,J= 5.8,CH2);3.88(t,J= 5.8,CH20);5.56(s,1H,CH2N);8.02(s,1arom.H); proton of thiazole ring is exchanged with deuterium of D,O.</p><p style="padding: 0px 0px 1em;">FAB-MS: 265 (100, M+), 181 (18), 144 (30), 123 (65), 122 (65), 91 (78).</p><p style="padding: 0px 0px 1em;">Anal. calc. for C,2H18C1,N40S (337.27): C 42.74, H 5.38, N 16.61, S 9.51, CI 21.02; found: C 42.93, H 5.28, N 16.70, S 9.61, C121.17.</p></div>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com5tag:blogger.com,1999:blog-8960696629007291242.post-28480384851629180252021-08-02T02:10:00.001-07:002021-08-02T02:10:09.357-07:00Ezutromid<p> </p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/08/str2.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/08/str2.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/08/STR3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/08/STR3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">Dibenzoate5-(ethylsulfone)-2-(naphthalen-2- yl)benzo[d]oxazole (Ezotrumid) 5a:</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">5- (ethylthio)-2-(naphthalen-2-yl)Benzo[d]oxazole (30.5 mg, 0.1 mmol), UO2(OAc)2 . 2H2O (0.8 mg, 0.002 mol), H2O (10 equiv., 36 μL), o-xylene (8.3 equiv., 0.2 mL), CH3CN (1 mL) were stirred under oxygen atmosphere (1 atm, balloon) at room temperature until the total consumption of sulfide and sulfoxide under the irradiation of three 2 w blue LEDs in a paralleled reactor. 5a (27.3 mg, 81%) was obtained through column chromatography (PE/EA = 20/1-5/1) as a white solid, Rf = 0.6 (PE/EA = 2/1);</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">1H NMR (500 MHz, Chloroform-d) δ 8.82 (s, 1H), 8.37 (s, 1H), 8.32 (d, J = 8.5 Hz, 1H), 8.02 (d, J = 8.0 Hz, 2H), 7.99 – 7.89 (m, 2H), 7.84 – 7.76 (m, 1H), 7.61 (t, J = 7.3 Hz, 2H), 3.28 – 3.08 (m, 2H), 1.32 (dt, J = 7.3, 3.6 Hz, 3H)..</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">13C NMR (126 MHz, Chloroform-d) δ 165.57, 153.87, 142.86, 135.26, 135.14, 132.86, 129.09, 128.97, 128.37, 127.99, 127.19, 125.35, 123.87, 123.34, 121.00, 111.36, 51.04, 7.62.</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">IR (KBr) 2933, 1507, 1498, 1258, 1064, 1046, 756, 474 cm-1 .</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">HRMS (ESI) Calcd for C19H16NO3S 338.0851 (M+H), Found 338.0865.</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><a data-mce-href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201906080" href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201906080" style="background-color: white; color: #993366;">https://onlinelibrary.wiley.com/doi/10.1002/anie.201906080</a></p>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com18tag:blogger.com,1999:blog-8960696629007291242.post-91491772331116156422021-04-12T02:26:00.004-07:002021-04-12T02:26:52.087-07:00DEXMETHYLPHENIDATE<p> </p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img alt="Dexmethylphenidate structure.svg" data-mce-src="https://upload.wikimedia.org/wikipedia/commons/thumb/c/c8/Dexmethylphenidate_structure.svg/200px-Dexmethylphenidate_structure.svg.png" src="https://upload.wikimedia.org/wikipedia/commons/thumb/c/c8/Dexmethylphenidate_structure.svg/200px-Dexmethylphenidate_structure.svg.png" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">DEXMETHYLPHENIDATE</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">Synonyms<span class="separated-list-container">Dexmethylphenidate HCl, </span>UNII<a data-mce-href="https://fdasis.nlm.nih.gov/srs/srsdirect.jsp?regno=1678OK0E08" href="https://fdasis.nlm.nih.gov/srs/srsdirect.jsp?regno=1678OK0E08" rel="noopener" style="color: #222222;" target="_blank">1678OK0E08</a>, CAS Number19262-68-1, WeightAverage: 269.77<br />Chemical FormulaC<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">14</span>H<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">20</span>ClNO<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">methyl (2R)-2-phenyl-2-[(2R)-piperidin-2-yl]acetate hydrochloride</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img alt="Thumb" data-mce-src="https://go.drugbank.com/structures/DBSALT001458/thumb.svg" src="https://go.drugbank.com/structures/DBSALT001458/thumb.svg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><table class="infobox mce-item-table" style="border: 1px dashed rgb(187, 187, 187); color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><tbody><tr><th class="infobox-label" scope="row" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;"><a data-mce-href="https://en.wikipedia.org/wiki/CAS_Registry_Number" href="https://en.wikipedia.org/wiki/CAS_Registry_Number" style="color: #222222;" title="CAS Registry Number">CAS Number</a></th><td class="infobox-data" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div class="plainlist"><ul style="margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span title="www.commonchemistry.cas.org"><a class="external text" data-mce-href="https://commonchemistry.cas.org/detail?cas_rn=40431-64-9" href="https://commonchemistry.cas.org/detail?cas_rn=40431-64-9" rel="nofollow" style="color: #222222;">40431-64-9</a></span><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;"> <img alt="☒" data-file-height="600" data-file-width="525" data-mce-src="https://upload.wikimedia.org/wikipedia/commons/thumb/a/a2/X_mark.svg/7px-X_mark.svg.png" height="8" src="https://upload.wikimedia.org/wikipedia/commons/thumb/a/a2/X_mark.svg/7px-X_mark.svg.png" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/a/a2/X_mark.svg/11px-X_mark.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/a/a2/X_mark.svg/14px-X_mark.svg.png 2x" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" width="7" /></span></li><li style="padding-top: 5px;">as HCl: <span title="www.commonchemistry.cas.org"><a class="external text" data-mce-href="https://commonchemistry.cas.org/detail?cas_rn=19262-68-1" href="https://commonchemistry.cas.org/detail?cas_rn=19262-68-1" rel="nofollow" style="color: #222222;">19262-68-1</a></span></li></ul></div></td></tr><tr><th class="infobox-label" scope="row" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;"><a data-mce-href="https://en.wikipedia.org/wiki/PubChem#CID" href="https://en.wikipedia.org/wiki/PubChem#CID" style="color: #222222;" title="PubChem">PubChem</a> <abbr title="Compound ID">CID</abbr></th><td class="infobox-data" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div class="plainlist"><ul style="margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span title="pubchem.ncbi.nlm.nih.gov"><a class="external text" data-mce-href="https://pubchem.ncbi.nlm.nih.gov/compound/154101" href="https://pubchem.ncbi.nlm.nih.gov/compound/154101" rel="nofollow" style="color: #222222;">154101</a></span></li><li style="padding-top: 5px;">as HCl: <span title="pubchem.ncbi.nlm.nih.gov"><a class="external text" data-mce-href="https://pubchem.ncbi.nlm.nih.gov/compound/154100" href="https://pubchem.ncbi.nlm.nih.gov/compound/154100" rel="nofollow" style="color: #222222;">154100</a></span></li></ul></div></td></tr><tr><th class="infobox-label" scope="row" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;"><a data-mce-href="https://en.wikipedia.org/wiki/Guide_to_Pharmacology" href="https://en.wikipedia.org/wiki/Guide_to_Pharmacology" style="color: #222222;" title="Guide to Pharmacology">IUPHAR/BPS</a></th><td class="infobox-data" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div class="plainlist"><ul style="margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span title="www.guidetopharmacology.org"><a class="external text" data-mce-href="http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7554" href="http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7554" rel="nofollow" style="color: #222222;">7554</a></span></li></ul></div></td></tr><tr><th class="infobox-label" scope="row" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;"><a data-mce-href="https://en.wikipedia.org/wiki/DrugBank" href="https://en.wikipedia.org/wiki/DrugBank" style="color: #222222;" title="DrugBank">DrugBank</a></th><td class="infobox-data" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div class="plainlist"><ul style="margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span title="www.drugbank.ca"><a class="external text" data-mce-href="https://www.drugbank.ca/drugs/DB06701" href="https://www.drugbank.ca/drugs/DB06701" rel="nofollow" style="color: #222222;">DB06701</a></span><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;"> <img alt="check" data-file-height="600" data-file-width="600" data-mce-src="https://upload.wikimedia.org/wikipedia/en/thumb/f/fb/Yes_check.svg/7px-Yes_check.svg.png" height="7" src="https://upload.wikimedia.org/wikipedia/en/thumb/f/fb/Yes_check.svg/7px-Yes_check.svg.png" srcset="//upload.wikimedia.org/wikipedia/en/thumb/f/fb/Yes_check.svg/11px-Yes_check.svg.png 1.5x, //upload.wikimedia.org/wikipedia/en/thumb/f/fb/Yes_check.svg/14px-Yes_check.svg.png 2x" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" width="7" /></span></li><li style="padding-top: 5px;">as HCl: <span title="www.drugbank.ca"><a class="external text" data-mce-href="https://www.drugbank.ca/drugs/DBSALT001458" href="https://www.drugbank.ca/drugs/DBSALT001458" rel="nofollow" style="color: #222222;">DBSALT001458</a></span></li></ul></div></td></tr><tr><th class="infobox-label" scope="row" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;"><a data-mce-href="https://en.wikipedia.org/wiki/ChemSpider" href="https://en.wikipedia.org/wiki/ChemSpider" style="color: #222222;" title="ChemSpider">ChemSpider</a></th><td class="infobox-data" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div class="plainlist"><ul style="margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span title="www.chemspider.com"><a class="external text" data-mce-href="http://www.chemspider.com/Chemical-Structure.135807.html" href="http://www.chemspider.com/Chemical-Structure.135807.html" rel="nofollow" style="color: #222222;">135807</a></span><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;"> <img alt="check" data-file-height="600" data-file-width="600" data-mce-src="https://upload.wikimedia.org/wikipedia/en/thumb/f/fb/Yes_check.svg/7px-Yes_check.svg.png" height="7" src="https://upload.wikimedia.org/wikipedia/en/thumb/f/fb/Yes_check.svg/7px-Yes_check.svg.png" srcset="//upload.wikimedia.org/wikipedia/en/thumb/f/fb/Yes_check.svg/11px-Yes_check.svg.png 1.5x, //upload.wikimedia.org/wikipedia/en/thumb/f/fb/Yes_check.svg/14px-Yes_check.svg.png 2x" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" width="7" /></span></li><li style="padding-top: 5px;">as HCl: <span title="www.chemspider.com"><a class="external text" data-mce-href="http://www.chemspider.com/Chemical-Structure.135806.html" href="http://www.chemspider.com/Chemical-Structure.135806.html" rel="nofollow" style="color: #222222;">135806</a></span></li></ul></div></td></tr><tr><th class="infobox-label" scope="row" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;"><a data-mce-href="https://en.wikipedia.org/wiki/Unique_Ingredient_Identifier" href="https://en.wikipedia.org/wiki/Unique_Ingredient_Identifier" style="color: #222222;" title="Unique Ingredient Identifier">UNII</a></th><td class="infobox-data" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div class="plainlist"><ul style="margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span title="fdasis.nlm.nih.gov"><a class="external text" data-mce-href="https://fdasis.nlm.nih.gov/srs/unii/M32RH9MFGP" href="https://fdasis.nlm.nih.gov/srs/unii/M32RH9MFGP" rel="nofollow" style="color: #222222;">M32RH9MFGP</a></span></li><li style="padding-top: 5px;">as HCl: <span title="fdasis.nlm.nih.gov"><a class="external text" data-mce-href="https://fdasis.nlm.nih.gov/srs/unii/1678OK0E08" href="https://fdasis.nlm.nih.gov/srs/unii/1678OK0E08" rel="nofollow" style="color: #222222;">1678OK0E08</a></span></li><li></li></ul></div></td></tr></tbody></table><p><br /></p><div class="box-hclx" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><p style="padding: 0px 0px 1em;">CLIP</p><p style="padding: 0px 0px 1em;"><strong>An Improved and Efficient Process for the Production of Highly Pure Dexmethylphenidate Hydrochloride</strong><strong> </strong></p><p style="padding: 0px 0px 1em;">Long-Xuan Xing, Cheng-Wu Shen, Yuan-Yuan Sun, Lei Huang, Yong-Yong Zheng,<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">*</span> Jian-Qi Li<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">*</span></p><p style="padding: 0px 0px 1em;"><a data-mce-href="https://onlinelibrary.wiley.com/doi/abs/10.1002/jhet.2705" href="https://onlinelibrary.wiley.com/doi/abs/10.1002/jhet.2705" style="color: #222222;">https://onlinelibrary.wiley.com/doi/abs/10.1002/jhet.2705</a></p><p style="padding: 0px 0px 1em;">The present work describes an efficient and commercially viable process for the synthesis of dexmethylphenidate hydrochloride (1), a mild nervous system stimulant. The overall yield is 23% with ~99.9% purity (including seven chemical steps). Formation and control of possible impurities are also described in this report.</p><p style="padding: 0px 0px 1em;"><img alt="An Improved and Efficient Process for the Production of Highly Pure Dexmethylphenidate Hydrochloride - Xing - 2017 - Journal of Heterocyclic Chemistry - Wiley Online Library" data-mce-src="https://onlinelibrary.wiley.com/cms/asset/c94113da-3bd3-4b82-a88c-42bf56cc550f/jhet2705-toc-0001-m.jpg" src="https://onlinelibrary.wiley.com/cms/asset/c94113da-3bd3-4b82-a88c-42bf56cc550f/jhet2705-toc-0001-m.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="padding: 0px 0px 1em;">(R)-methyl 2-phenyl-2-((R)-piperidin-2-yl)acetate hydrochloride (1). ............ afford 1 as a white solid (107.6 g, 87.3% yield) with 99.50% purity and 99.70% ee. The crude product (107.6 g, 0.4 mol) was further purified by recrystallization from pure water (100 mL) to obtain the qualified product 1 (98.3 g, 91.4% yield) with 99.92 purity and 99.98% ee.</p><p style="padding: 0px 0px 1em;">[α] 25 D +85.6 (MeOH, c 1) (lit [4b]. [α] 25 D +84 (MeOH, c 1));</p><p style="padding: 0px 0px 1em;">Mp 222-223 C (lit [4b]. Mp 222– 224°C); MS m/z 234 [M + H]+ .</p><p style="padding: 0px 0px 1em;">1 H NMR (400Hz, DMSO-d6) δ 1 H NMR (400 MHz, DMSO-d6) δ 9.64 (br, 1H), 8.97 (br, 1H), 7.41-7.26 (m, 5H), 4.18-4.16 (d, J = 9.2Hz, 1H), 3.77-3.75 (m, 1H), 3.66 (s, 3H), 3.25 (m, 1H), 2.94 (m, 1H), 1.67-1.64 (m, 3H), 1.41-1.25 (m, 3H).</p><p style="padding: 0px 0px 1em;">13C NMR (100.6 MHz, DMSO-d6) δ 171.3, 134.2, 129.1, 128.6, 128.2, 56.8, 53.3, 52.6, 44.5, 25.7, 21.5, 21.4.</p><p style="padding: 0px 0px 1em;"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">1</span>H-NMR, and <span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">13</span>C-NMR of compound <strong>1</strong>......................................... 10-11</p><p style="padding: 0px 0px 1em;"><br /></p><p style="padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str1-11.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str1-11.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str2-3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str2-3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="padding: 0px 0px 1em;">DEPT,</p><p style="padding: 0px 0px 1em;"><br /></p><p style="padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str3-1.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str3-1.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="padding: 0px 0px 1em;">COSY, NOESY, GHMBC, and HMQC of compound <strong>1</strong>.................. 12-14</p><p style="padding: 0px 0px 1em;"><br /></p><p style="padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str1-10.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str1-10.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="padding: 0px 0px 1em;">COSY</p><p style="padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str2-2.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str2-2.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="padding: 0px 0px 1em;">NOESY</p><p style="padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="padding: 0px 0px 1em;">GHMBC</p><p style="padding: 0px;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str4.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/04/str4.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p></div><h2 style="color: #222222; font-family: "PT Serif", TimesNewRoman, "Times New Roman", Times, Baskerville, Georgia, serif; font-size: 30px; line-height: 33px; margin: 0px; padding: 30px 0px 10px;">HMQC</h2><h2 style="color: #222222; font-family: "PT Serif", TimesNewRoman, "Times New Roman", Times, Baskerville, Georgia, serif; font-size: 30px; line-height: 33px; margin: 0px; padding: 30px 0px 10px;"><span class="mw-headline" id="Medical_uses">Medical uses</span></h2>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com25tag:blogger.com,1999:blog-8960696629007291242.post-76915755082745816152021-03-07T03:28:00.002-08:002021-03-07T03:28:58.237-08:00Buspirone<p> </p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img alt="Buspirone 200.svg" data-mce-src="https://upload.wikimedia.org/wikipedia/commons/thumb/0/03/Buspirone_200.svg/250px-Buspirone_200.svg.png" src="https://upload.wikimedia.org/wikipedia/commons/thumb/0/03/Buspirone_200.svg/250px-Buspirone_200.svg.png" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img alt="Buspirone" data-mce-src="https://www.drugfuture.com/chemdata/structure/Buspirone.gif" src="https://www.drugfuture.com/chemdata/structure/Buspirone.gif" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><br /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">Buspirone</p><ul class="struct-props" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;"><span class="prop_title">Molecular Formula</span><span id="ctl00_ctl00_ContentSection_ContentPlaceHolder1_RecordViewDetails_rptDetailsView_ctl00_prop_MF">C<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">21</span>H<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">31</span>N<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">5</span>O<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span></span></li><li style="padding-top: 5px;"><span class="prop_title">Average mass</span>385.503 Da</li><li style="padding-top: 5px;"><div class="syn"><span class="">буспирон</span></div><div class="syn"><span class="">بوسبيرون</span></div><div class="syn"><span class="">丁螺酮</span></div></li></ul><div class="syn" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><strong>251-489-4</strong> <a class="synonym_ref" data-mce-href="http://echa.europa.eu/web/guest/information-on-chemicals/ec-inventory" href="http://echa.europa.eu/web/guest/information-on-chemicals/ec-inventory" style="color: #222222;" target="reference" title="EINECS">[EINECS]</a></div><div class="syn" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><strong>253-072-2</strong> <a class="synonym_ref" data-mce-href="http://echa.europa.eu/web/guest/information-on-chemicals/ec-inventory" href="http://echa.europa.eu/web/guest/information-on-chemicals/ec-inventory" style="color: #222222;" target="reference" title="EINECS">[EINECS]</a></div><div class="syn" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><strong>36505-84-7</strong> <a class="synonym_ref" data-mce-href="http://www.ncbi.nlm.nih.gov/sites/entrez?db=pccompound&amp;term=%2236505-84-7%22[CompleteSynonym]" href="http://www.ncbi.nlm.nih.gov/sites/entrez?db=pccompound&amp;term=%2236505-84-7%22[CompleteSynonym]" style="color: #222222;" target="reference" title="RN">[RN]</a></div><div class="syn" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><strong>8-[4-(4-Pyrimidin-2<wbr></wbr>-yl-piperazin-1-yl)<wbr></wbr>-butyl]-8-aza-spiro<wbr></wbr>[4.5]decane-7,9-dio<wbr></wbr>ne</strong></div><div class="syn" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><strong>8-[4-[4-(2-Pyrimidi<wbr></wbr>nyl)-1-piperazinyl]<wbr></wbr>butyl]-8-azaspiro[4<wbr></wbr>.5]decane-7,9-dione</strong></div><div class="syn" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><ul style="margin: 0.5em 0px 1em 30px;"><li style="padding-top: 5px;">8-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione</li><li class="alt" style="padding-top: 5px;">Buspin</li><li style="padding-top: 5px;">Buspirone</li><li class="alt" style="padding-top: 5px;">Spitomin</li></ul></div><div class="syn" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><div align="left">Buspirone</div><div align="left"><br /></div><div align="left"><p style="padding: 0px 0px 1em;">PAPER</p><p style="padding: 0px 0px 1em;"><a data-mce-href="https://pubs.rsc.org/en/content/articlelanding/2019/GC/C8GC03328E#!divAbstract" href="https://pubs.rsc.org/en/content/articlelanding/2019/GC/C8GC03328E#!divAbstract" style="color: #222222;">https://pubs.rsc.org/en/content/articlelanding/2019/GC/C8GC03328E#!divAbstract</a></p><ol style="list-style-image: initial; list-style-position: initial; margin: 0.5em 0px 1em 50px;"><li style="padding-top: 5px;">Green Chemistry, 21(1), 59-63; 2019</li></ol><h3 class="h--heading3 article-abstract__heading" style="font-family: "PT Serif", TimesNewRoman, "Times New Roman", Times, Baskerville, Georgia, serif; font-size: 24px; line-height: 26.4px; margin: 0px; padding: 30px 0px 10px;">Abstract</h3><div class="capsule__column-wrapper"><div class="capsule__text"><p style="padding: 0px;">A continuous flow method for the direct conversion of alcohols to amines <em>via</em> a hydrogen borrowing approach is reported. The method utilises a low loading (0.5%) of a commercial catalyst system ([Ru(<em>p</em>-cymene)Cl<small style="font-size: 12px;"><span style="font-size: 9px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span></small>]<small style="font-size: 12px;"><span style="font-size: 9px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span></small> and DPEPhos), reagent grade solvent and is selective for primary alcohols. Successful methylation of amines using methanol and the direct dimethylamination of alcohols using commercial dimethylamine solution are reported. The synthesis of two pharmaceutical agents Piribedil (<strong>5</strong>) and Buspirone (<strong>25</strong>) were accomplished in good yields employing these new methods.</p></div><div class="capsule__article-image fixpadv--s"><img alt="Graphical abstract: Fast continuous alcohol amination employing a hydrogen borrowing protocol" data-mce-src="https://pubs.rsc.org/en/Image/Get?imageInfo.ImageType=GA&imageInfo.ImageIdentifier.ManuscriptID=C8GC03328E&imageInfo.ImageIdentifier.Year=2019" src="https://pubs.rsc.org/en/Image/Get?imageInfo.ImageType=GA&imageInfo.ImageIdentifier.ManuscriptID=C8GC03328E&imageInfo.ImageIdentifier.Year=2019" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" title="Graphical abstract" /></div></div><div class="capsule__article-image fixpadv--s"><a data-mce-href="http://www.rsc.org/suppdata/c8/gc/c8gc03328e/c8gc03328e2.pdf" href="http://www.rsc.org/suppdata/c8/gc/c8gc03328e/c8gc03328e2.pdf" style="color: #222222;">http://www.rsc.org/suppdata/c8/gc/c8gc03328e/c8gc03328e2.pdf</a></div><div class="capsule__article-image fixpadv--s"> <br /></div><div class="capsule__article-image fixpadv--s">8-(4-hydroxybutyl)-8-azaspiro[4.5]decane-7,9-dione (23): A solution of 3,3-tetramethyleneglutaric anhydride (0.25 mol/L in THF) was combined in a tee piece with a solution of 4-amino-1-butanol (0.25 mol/L in THF) and reacted in a 20 mL reactor coil (stainless steel, 20 min residence time) heated at 250 °C. The output was concentrated in vacuo and the residue purified by column chromatography on silica gel to afford the product in 84% yield (Rf = 0.31, 63% DCM/AcOEt). 1H NMR (400 MHz, CDCl3) δ = 3.78 (t, J = 7.2 Hz, 2H), 3.65 (t, J = 6.0 Hz, 2H), 2.58 (s, 4H), 1.77 – 1.64 (m, 4H), 1.64 – 1.53 (m, 4H), 1.53 – 1.43 (m, 4H). 13C NMR (100 MHz, CDCl3) δ = 172.33, 62.28, 44.87, 39.47, 39.14, 37.54, 29.81, 24.35, 24.17. HRMS for [C13H22NO3] + calculated 240.1594 found 240.1605.</div><div class="capsule__article-image fixpadv--s"> <br /></div><div class="capsule__article-image fixpadv--s"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/03/STR3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/03/STR3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div><div class="capsule__article-image fixpadv--s"> <br /></div><div class="capsule__article-image fixpadv--s"> <br /></div><div class="capsule__column-wrapper"><div class="capsule__article-image fixpadv--s">8-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)-8-azaspiro[4.5]decane-7,9-dione (Buspirone, 25): The flow system was flushed with THF, the back-pressure regulator was set to 50 bar, and the coil reactor heated to 250 °C. Then a solution (10 mL overall volume) containing 1-(2-pyrimidyl)piperazine (2 mmol), 8-(4-hydroxybutyl)- 8-azaspiro[4.5]decane-7,9-dione (23) (2 mmol), dichloro(p-cymene)ruthenium(II) dimer (0.08 mmol) and bis[(2- diphenylphosphino)phenyl] ether (DPEPhos, 0.17 mmol) was pumped at 0.8 ml/min through a heated coil (8 mL, Phoenix reactor). The output solution obtained in steady state (monitored using the FlowUV) was concentrated in vacuo and purified by column chromatography on silica gel to afford the desired product in 76% yield (Rf = 0.29, 5% MeOH/DCM). 1H NMR (400 MHz, CDCl3) δ = 8.31 (d, J = 4.7 Hz, 2H), 6.48 (t, J = 4.7 Hz, 1H), 3.84 (t, J = 5.1 Hz, 4H), 3.79 (t, J = 6.8 Hz, 2H), 2.60 (s, 4H), 2.50 (t, J = 5.1 Hz, 4H), 2.40 (t, J = 6.8 Hz, 2H), 1.79 – 1.65 (m, 4H), 1.65 – 1.42 (m, 8H). 13C NMR (100 MHz, CDCl3) δ = 172.19, 161.63, 157.68, 109.77, 58.31, 53.06, 44.92, 43.60, 39.48, 39.35, 37.56, 26.04, 24.19, 24.19. HRMS for [C21H32N5O2] + calculated 386.2551 found 386.2570.</div></div><p style="padding: 0px 0px 1em;"><br /></p><p style="padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/03/str1-4.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/03/str1-4.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p><p style="padding: 0px 0px 1em;"><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2021/03/STR2.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2021/03/STR2.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></p></div><div align="left"><b>CAS Registry Number:</b> 36505-84-7</div><div align="left"><b>CAS Name:</b> 8-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione</div><div align="left"><b>Molecular Formula:</b> C21H31N5O2</div><div align="left"><b>Molecular Weight:</b> 385.50</div><div align="left"><b>Percent Composition:</b> C 65.43%, H 8.11%, N 18.17%, O 8.30%</div><div align="left"><b>Literature References:</b> Non-benzodiazepine anxiolytic; 5-hydroxytryptamine (5-HT1) receptor agonist. Prepn: Y. H. Wu <i>et al.,</i> <i>J. Med. Chem.</i> <b>15,</b> 477 (1972); Y. H. Wu, J. W. Rayburn, <b>DE</b> <b>2057845</b> (1971 to Bristol-Myers); <i>eidem,</i> <b>US</b> <b>3717634</b> (1973 to Mead-Johnson). Pharmacology: L. E. Allen <i>et al.,</i> <i>Arzneim.-Forsch.</i> <b>24,</b> 917 (1974). Comparison with diazepam in treatment of anxiety: H. L. Goldberg, R. J. Finnerty, <i>Am. J. Psychiatry</i> <b>136,</b> 1184 (1979); A. F. Jacobson <i>et al.,</i> <i>Pharmacotherapy</i> <b>5,</b> 290 (1985). Nonsynergistic effect with alcohol: T. Seppala <i>et al.,</i> <i>Clin. Pharmacol. Ther.</i> <b>32,</b> 201 (1982). Disposition and metabolism: S. Caccia <i>et al.,</i> <i>Xenobiotica</i> <b>13,</b> 147 (1983). Series of articles on chemistry, pharmacology, addictive potential, and clinical trials: <i>J. Clin. Psychiatry</i> <b>43,</b> pp 1-116 (1982); on pharmacology, safety and clinical comparison with clorazepate: <i>Am. J. Med.</i> <b>80,</b> Suppl. 3B, 1-51 (1986). Review of pharmacology and therapeutic efficacy: K. L. Goa, A. Ward, <i>Drugs</i> <b>32,</b> 114-129 (1986). <i>Review:</i> M. W. Jann, <i>Pharmacotherapy</i> <b>8,</b> 100-116 (1988); D. P. Taylor, <i>FASEB J.</i> <b>2,</b> 2445-2452 (1988).</div><div align="left"> <br /></div><div align="left"><b>Derivative Type:</b> Hydrochloride</div><div align="left"><b>CAS Registry Number:</b> 33386-08-2</div><div align="left"><b>Trademarks:</b> Ansial (Vita); Ansiced (Abello); Axoren (Glaxo Wellcome); Bespar (BMS); Buspar (BMS); Buspimen (Menarini); Buspinol (Zdravlje); Buspisal (Lesvi); Narol (Almirall)</div><div align="left"><b>Molecular Formula:</b> C21H31N5O2.HCl</div><div align="left"><b>Molecular Weight:</b> 421.96</div><div align="left"><b>Percent Composition:</b> C 59.77%, H 7.64%, N 16.60%, O 7.58%, Cl 8.40%</div><div align="left"><b>Properties:</b> Crystals from abs ethanol, mp 201.5-202.5°. LD50 i.p. in rats: 136 mg/kg (Allen).</div><div align="left"><b>Melting point:</b> mp 201.5-202.5°</div><div align="left"><b>Toxicity data:</b> LD50 i.p. in rats: 136 mg/kg (Allen)</div><div align="left"> <br /></div><div align="left"><b>Therap-Cat:</b> Anxiolytic.</div><div align="left"><b>Keywords:</b> Anxiolytic; Arylpiperazines; Serotonin Receptor Agonist.</div></div>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com21tag:blogger.com,1999:blog-8960696629007291242.post-85971370979696562192021-02-27T19:01:00.010-08:002021-02-27T19:29:01.107-08:00AMIODARONE<div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><img alt="Amiodarone structure.svg" data-mce-selected="1" data-mce-src="http://upload.wikimedia.org/wikipedia/commons/thumb/d/d2/Amiodarone_structure.svg/220px-Amiodarone_structure.svg.png" src="http://upload.wikimedia.org/wikipedia/commons/thumb/d/d2/Amiodarone_structure.svg/220px-Amiodarone_structure.svg.png" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%; outline: rgb(114, 119, 124) solid 1px; resize: none; text-align: start;" /></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;"><br /></div><div class="separator" style="clear: both; text-align: center;">AMIODARONE</div><div class="separator" style="clear: both; text-align: center;"><a href="https://lh3.googleusercontent.com/-QV1268WCtCQ/YDsHL9JZqcI/AAAAAAAA59c/ENWO79Z-Rd8sXsXy_kh3oalrcxfdVRMmACNcBGAsYHQ/image.png" style="margin-left: 1em; margin-right: 1em;"><img alt="" data-original-height="534" data-original-width="700" height="334" src="https://lh3.googleusercontent.com/-QV1268WCtCQ/YDsHL9JZqcI/AAAAAAAA59c/ENWO79Z-Rd8sXsXy_kh3oalrcxfdVRMmACNcBGAsYHQ/w439-h334/image.png" width="439" /></a></div><br /><p> </p><p><br /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">PATENT</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">CN109053652-PREPARATION METHOD OF AMIODARONE HYDROCHLORIDE INTERMITTENT</p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><a data-mce-href="https://patentscope.wipo.int/search/en/detail.jsf?docId=CN235615504&_cid=P11-KL0AU0-06410-1" href="https://patentscope.wipo.int/search/en/detail.jsf?docId=CN235615504&_cid=P11-KL0AU0-06410-1" style="color: #222222;">https://patentscope.wipo.int/search/en/detail.jsf?docId=CN235615504&_cid=P11-KL0AU0-06410-1</a></p><table border="0" class="mce-item-table" style="border: 1px dashed rgb(187, 187, 187); color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; width: 800px;"><tbody><tr><td style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><span data-mce-style="font-family: 仿宋; font-size: large;" face="仿宋" style="font-size: large;">Description of the drawings</span></td></tr></tbody></table><table border="0" class="mce-item-table" style="border: 1px dashed rgb(187, 187, 187); color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; width: 800px;"><tbody><tr><td style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><span data-mce-style="font-family: 仿宋; font-size: large;" face="仿宋" style="font-size: large;"> </span></td></tr></tbody></table><table border="0" class="mce-item-table" style="border: 1px dashed rgb(187, 187, 187); color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; width: 800px;"><tbody><tr><td style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><span data-mce-style="font-family: 仿宋; font-size: large;" face="仿宋" style="font-size: large;"> Figure 3 shows the proton nuclear magnetic resonance spectrum of compound 9;</span></td></tr></tbody></table><table border="0" class="mce-item-table" style="border: 1px dashed rgb(187, 187, 187); color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; width: 800px;"><tbody><tr><td style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><span data-mce-style="font-family: 仿宋; font-size: large;" face="仿宋" style="font-size: large;"> Figure 4 shows the carbon nuclear magnetic resonance spectrum of compound 9.</span></td></tr></tbody></table><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img data-mce-src="https://patentscope.wipo.int/search/docs2/nat/CN235615504/pic/4Wi5JBsoV2vBmWQaECbmFp1slu3jCM8SBvYfIQhKePeYyRuMWyj4N26osplabJBbf8tydhv5yCxJIgmFWo6rD5tZl_Ml7b27D4pdOrtGJTIFilbMiD5Zbi9hxkCBTOmKni-wU_2ROVL5R4olgmtuwxLxefOA0yW70LT1Pg0fr-6iuFRlRqI8fS3UyN59mdq7?docId=id00000088188431" height="400" src="https://patentscope.wipo.int/search/docs2/nat/CN235615504/pic/4Wi5JBsoV2vBmWQaECbmFp1slu3jCM8SBvYfIQhKePeYyRuMWyj4N26osplabJBbf8tydhv5yCxJIgmFWo6rD5tZl_Ml7b27D4pdOrtGJTIFilbMiD5Zbi9hxkCBTOmKni-wU_2ROVL5R4olgmtuwxLxefOA0yW70LT1Pg0fr-6iuFRlRqI8fS3UyN59mdq7?docId=id00000088188431" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" width="596" /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><img data-mce-src="https://patentscope.wipo.int/search/docs2/nat/CN235615504/pic/WKvNK3OWd0VzMJ2E_SCZKlbXFtQPzHMdy6P7cxOYwfLTK5eYEEYscELEFAdrsz7L_7B31ha1ZN_qcauyTeaEmjTWndo5Lqjdw1lgJDVwOIsF2VkC8ET8hdN4B6xHjDP4eO8XtL6DUkYzWQ0gJq8_9Tmn6BO0SjfwOR28lNaydQDExmthJxx1Ny7WFVglYw7J?docId=id00000088188431" height="404" src="https://patentscope.wipo.int/search/docs2/nat/CN235615504/pic/WKvNK3OWd0VzMJ2E_SCZKlbXFtQPzHMdy6P7cxOYwfLTK5eYEEYscELEFAdrsz7L_7B31ha1ZN_qcauyTeaEmjTWndo5Lqjdw1lgJDVwOIsF2VkC8ET8hdN4B6xHjDP4eO8XtL6DUkYzWQ0gJq8_9Tmn6BO0SjfwOR28lNaydQDExmthJxx1Ny7WFVglYw7J?docId=id00000088188431" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" width="607" /></p><table border="0" style="background-color: white; border-collapse: collapse; border-spacing: 0px; box-sizing: inherit; color: #1a1a1a; font-family: simplon, arial, meiryo, sans-serif; font-size: 14px; width: 800px;"><tbody style="box-sizing: inherit;"><tr style="box-sizing: inherit;"><td style="box-sizing: inherit; padding: 0px;"><span face="仿宋" style="box-sizing: inherit; font-size: medium;"> compound 9 as an off-white crystalline powder with a yield of about 86.9%.</span></td></tr></tbody></table><table border="0" style="background-color: white; border-collapse: collapse; border-spacing: 0px; box-sizing: inherit; color: #1a1a1a; font-family: simplon, arial, meiryo, sans-serif; font-size: 14px; width: 800px;"><tbody style="box-sizing: inherit;"><tr style="box-sizing: inherit;"><td style="box-sizing: inherit; padding: 0px;"><span face="仿宋" style="box-sizing: inherit; font-size: medium;"> <span style="box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; top: -0.5em; vertical-align: baseline;"><span face="宋体" style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">1</span></span></span></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"> HNMR(400MHz,d</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">DMSO </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">)δ: 0.81~0.85(t,3H,-CH</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">3 </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">),<br />1.24~1.29(m,2H,-CH</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">2 </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">CH</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">3 </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">),1.68~1.70(m,2H,-CH</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">2 </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">CH</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">2 </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">CH</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">3 </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">),<br />2.82~2.85(t,2H,Ar-CH</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">2 </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">-CH</span></span><span style="bottom: -0.25em; box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; vertical-align: baseline;"> <copy style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">2 </span></span></copy></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;">), 6.91~7.72(m,8H,ArH), <br />10.46(m,1H,-OH). <br /></span></span><span style="box-sizing: inherit; font-size: 13.5px; line-height: 0; position: relative; top: -0.5em; vertical-align: baseline;"><span face="宋体" style="box-sizing: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"><br /><br /><br />13</span></span></span></span><span style="box-sizing: inherit; vertical-align: inherit;"><span style="box-sizing: inherit; vertical-align: inherit;"> CNMR(400 Hz,DMSO)δ:189.72,163.49,162.69,153.48,132.08,<br />130.16,127.28,124.87,123.98 ,121.16,116.90,11 5.78,<br />111.51,29.94,27.51,22.09,13.84. </span><span style="box-sizing: inherit; vertical-align: inherit;">See attached drawings 3~4.</span></span></span></td></tr></tbody></table><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><br /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><br /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"></p><div class="separator" style="clear: both; text-align: center;"><a href="https://lh3.googleusercontent.com/-meDcKLLyvq8/YDsITav_27I/AAAAAAAA59k/sdx5IijXv-0YwM8LeVmWtzi3dBsJL_1dQCNcBGAsYHQ/image.png" style="margin-left: 1em; margin-right: 1em;"><img alt="" data-original-height="488" data-original-width="850" height="256" src="https://lh3.googleusercontent.com/-meDcKLLyvq8/YDsITav_27I/AAAAAAAA59k/sdx5IijXv-0YwM8LeVmWtzi3dBsJL_1dQCNcBGAsYHQ/w518-h256/image.png" width="518" /></a></div><p></p><h1 class="nova-e-text nova-e-text--size-m nova-e-text--family-sans-serif nova-e-text--spacing-none nova-e-text--color-inherit" itemprop="caption" style="background-color: white; color: #111111; font-family: Roboto, Arial, sans-serif; font-size: 0.875rem; font-weight: 400; line-height: 1.3; margin-bottom: 0px; margin-top: 0px;">FTIR spectra of Amiodarone, Pluronic F68 and their solid dispersion formulations. ...<a href="https://www.japsonline.com/admin/php/uploads/2119_pdf.pdf">https://www.japsonline.com/admin/php/uploads/2119_pdf.pdf</a></h1><div class="separator" style="clear: both; text-align: center;"></div><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><br /></p><div class="separator" style="clear: both; text-align: center;"><a href="https://lh3.googleusercontent.com/-BDPT81eikrY/YDsK4cVNQNI/AAAAAAAA59s/oZW8AJhn7J8_iqQchpn3Cb5fJNX0cJNcwCNcBGAsYHQ/image.png" style="margin-left: 1em; margin-right: 1em;"><img alt="" data-original-height="350" data-original-width="811" height="244" src="https://lh3.googleusercontent.com/-BDPT81eikrY/YDsK4cVNQNI/AAAAAAAA59s/oZW8AJhn7J8_iqQchpn3Cb5fJNX0cJNcwCNcBGAsYHQ/w567-h244/image.png" width="567" /></a></div><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><br /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><br /></p>CLIP<p></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">MAGNETIC RESONANCE IN CHEMISTRY, VOL. 29, 482493 (1991)
'H and 13C NMR Analyses of Amiodarone,
Desethylamiodarone and Desoxoamiodarone </p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">Amiodarone (AMIO) is an antianginal and antiarrhythmic drug used clinically to treat a wide range of
cardiac arrhythmias.',' Desethylamiodarone (DEA) is
the major metabolite of amiodarone,' and desoxoamiodarone (DOA) is reported to be a less toxic form of
ami~daro<br /><br /></p><div class="separator" style="clear: both; text-align: center;"><a href="https://1.bp.blogspot.com/-bxUsq-waVEg/YDsMVUVsvmI/AAAAAAAA5-A/RoIk8IOm0jAvC5GS8BV7jgvkK6Gek2wcQCNcBGAsYHQ/s376/str1.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="237" data-original-width="376" height="288" src="https://1.bp.blogspot.com/-bxUsq-waVEg/YDsMVUVsvmI/AAAAAAAA5-A/RoIk8IOm0jAvC5GS8BV7jgvkK6Gek2wcQCNcBGAsYHQ/w456-h288/str1.JPG" width="456" /></a></div><br /><div class="separator" style="clear: both; text-align: center;"><br /></div><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://1.bp.blogspot.com/-ZakiMNEUe-U/YDsMJ8sNBTI/AAAAAAAA598/JbiqzQ9gj_su3bUr5l05edmMtDNRqiS1gCNcBGAsYHQ/s520/str1.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="520" data-original-width="364" height="591" src="https://1.bp.blogspot.com/-ZakiMNEUe-U/YDsMJ8sNBTI/AAAAAAAA598/JbiqzQ9gj_su3bUr5l05edmMtDNRqiS1gCNcBGAsYHQ/w414-h591/str1.JPG" width="414" /></a></div><br /><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><br /></p><div class="separator" style="clear: both; text-align: center;"><a href="https://1.bp.blogspot.com/-bDFhCTVkVvg/YDsM_TFKqJI/AAAAAAAA5-Q/S-27CZh9cVUGMYHN7XZgXXJUwKpyHd-aACNcBGAsYHQ/s649/str1.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="228" data-original-width="649" height="210" src="https://1.bp.blogspot.com/-bDFhCTVkVvg/YDsM_TFKqJI/AAAAAAAA5-Q/S-27CZh9cVUGMYHN7XZgXXJUwKpyHd-aACNcBGAsYHQ/w600-h210/str1.JPG" width="600" /></a></div><div class="separator" style="clear: both; text-align: center;">Figure 1. !%O-MHz 'H NMR spectra of (top) AMIO, (middle) DEA and (bottom) DOA in their HCI forms in CDCI, at 27°C. Note the
presence of the 3-CH2 resonance and the upfield shift of the aromatic singlet of DOA and the upfield shift of the HCI signal and the
half-intensity of the ethyl resonances of DEA. See text for details. </div><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://1.bp.blogspot.com/-HerpScs-kB0/YDsM_qrsAmI/AAAAAAAA5-U/-wmyW4SPmqIAk4nsvJ64MuK__Yzf91PAQCNcBGAsYHQ/s367/str2.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="367" data-original-width="318" height="503" src="https://1.bp.blogspot.com/-HerpScs-kB0/YDsM_qrsAmI/AAAAAAAA5-U/-wmyW4SPmqIAk4nsvJ64MuK__Yzf91PAQCNcBGAsYHQ/w436-h503/str2.JPG" width="436" /></a></div><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://1.bp.blogspot.com/-dGQQ_Au5BPE/YDsM_dAjudI/AAAAAAAA5-M/coXEdkAmgRMdb2ZLKip3Kr1NNqKkXabTgCNcBGAsYHQ/s362/STR3.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="362" data-original-width="317" height="464" src="https://1.bp.blogspot.com/-dGQQ_Au5BPE/YDsM_dAjudI/AAAAAAAA5-M/coXEdkAmgRMdb2ZLKip3Kr1NNqKkXabTgCNcBGAsYHQ/w406-h464/STR3.JPG" width="406" /></a></div><br /><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">Figure 2. 500-MHz ‘H 2D COSY NMR spectra showing the spin connectivities in (A) the aliphatic region of AMIO, (B) the aliphatic
region of DEA, (C) the aliphatic region of DOA and (D) the aromatic region of AMIO. Note the similarity of the COSY patterns of AMIO,
DEA and DOA.</p><div class="separator" style="clear: both; text-align: center;"><a href="https://1.bp.blogspot.com/-tWrH4exQWZo/YDsNwlWq45I/AAAAAAAA5-g/qCvK5GG_NX4O2IjWgewFB6awSuXDbZ20wCNcBGAsYHQ/s533/str1.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="396" data-original-width="533" height="433" src="https://1.bp.blogspot.com/-tWrH4exQWZo/YDsNwlWq45I/AAAAAAAA5-g/qCvK5GG_NX4O2IjWgewFB6awSuXDbZ20wCNcBGAsYHQ/w583-h433/str1.JPG" width="583" /></a></div><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://1.bp.blogspot.com/-yzd3YJbdazI/YDsNwwJV4kI/AAAAAAAA5-k/31AYOhRbEvQb0sGySvXtUTPFiIUkIr-SgCNcBGAsYHQ/s479/str2.JPG" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="373" data-original-width="479" height="437" src="https://1.bp.blogspot.com/-yzd3YJbdazI/YDsNwwJV4kI/AAAAAAAA5-k/31AYOhRbEvQb0sGySvXtUTPFiIUkIr-SgCNcBGAsYHQ/w562-h437/str2.JPG" width="562" /></a></div><div class="separator" style="clear: both; text-align: center;">Figure 6. 75-MHz 1D 13C NMR spectrum of AM10 in CDCI, at 27°C (bottom) and selective INEPT spectra transferring from proton
multiplet positions indicated. </div><br /><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;"><br /></p><p style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">///////////</p>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com23tag:blogger.com,1999:blog-8960696629007291242.post-67861153277126621472020-07-29T20:31:00.003-07:002020-07-29T20:31:46.923-07:00Diquafosol<div dir="ltr" style="text-align: left;" trbidi="on">
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READ<br />
<a href="https://newdrugapprovals.org/2020/07/30/diquafosol/">https://newdrugapprovals.org/2020/07/30/diquafosol/</a></div>
DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com116tag:blogger.com,1999:blog-8960696629007291242.post-49434438221780504352020-03-20T02:11:00.003-07:002020-12-17T17:56:26.592-08:00Favipiravir<div dir="ltr" style="text-align: left;" trbidi="on">
<div style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; padding: 0px 0px 1em;">
<img alt="ChemSpider 2D Image | favipiravir | C5H4FN3O2" data-mce-src="http://www.chemspider.com/ImagesHandler.ashx?id=431002&w=250&h=250" src="http://www.chemspider.com/ImagesHandler.ashx?id=431002&w=250&h=250" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div>
<ul class="struct-props" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; margin: 0.5em 0px 1em 30px;">
<li style="padding-top: 5px;"><span class="prop_title">Molecular Formula</span><span id="ctl00_ctl00_ContentSection_ContentPlaceHolder1_RecordViewDetails_rptDetailsView_ctl00_prop_MF">C<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">5</span>H<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">4</span>FN<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">3</span>O<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span></span></li>
<li style="padding-top: 5px;"><span class="prop_title">Average mass</span>157.103 Da</li>
</ul><div><span style="color: #222222; font-family: Open Sans, Tahoma, Verdana, Segoe, sans-serif;"><br /></span></div><div><span style="color: #222222; font-family: Open Sans, Tahoma, Verdana, Segoe, sans-serif;">SYNTHESIS AT <a href="https://newdrugapprovals.org/2015/08/18/filgotinib/">https://newdrugapprovals.org/2015/08/18/filgotinib/</a></span></div><div><span style="color: #222222; font-family: Open Sans, Tahoma, Verdana, Segoe, sans-serif;"><br /></span></div>
<div class="syn" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
<strong>259793-96-9</strong> <a class="synonym_ref" data-mce-href="http://www.ncbi.nlm.nih.gov/sites/entrez?db=pccompound&amp;term=%22259793-96-9%22[CompleteSynonym]" href="http://www.ncbi.nlm.nih.gov/sites/entrez?db=pccompound&amp;term=%22259793-96-9%22[CompleteSynonym]" style="color: #222222;" target="reference" title="RN">[RN]</a></div>
<div class="syn" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
<strong>2-Pyrazinecarboxamide, 6-fluoro-3,4-dihydro-3-oxo-</strong></div>
<div class="syn" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
</div>
<div class="syn" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
<strong>6-Fluoro-3-hydroxypyrazine-2-carboxamide</strong></div>
<div class="syn" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
<strong>6-Fluoro-3-oxo-3,4-dihydro-2-pyrazinecarboxamide</strong></div>
<div class="syn" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
</div>
<div class="syn" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
<strong>8916</strong></div>
<div class="syn" style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
<strong>Avigan</strong></div>
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ファビピラビル<br />Favipiravir</div>
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SYN</div>
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<a data-mce-href="https://link.springer.com/article/10.1007/s11696-018-0654-9" href="https://link.springer.com/article/10.1007/s11696-018-0654-9" style="color: #222222;">https://link.springer.com/article/10.1007/s11696-018-0654-9</a></div>
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Electronic supplementary material</h2>
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Below is the link to the electronic supplementary material.</div>
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Ref</h2>
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<a data-mce-href="https://pdfs.semanticscholar.org/be8e/cb882b99204983d2f60077c7ab8b53f4d62c.pdf" href="https://pdfs.semanticscholar.org/be8e/cb882b99204983d2f60077c7ab8b53f4d62c.pdf" style="color: #222222;">https://pdfs.semanticscholar.org/be8e/cb882b99204983d2f60077c7ab8b53f4d62c.pdf</a></div>
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Drug Discoveries & Therapeutics. 2014; 8(3):117-120.</div>
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mp = 178-180°C. 1 H-NMR (600 MHz, DMSO): δ 12.34 (brs, 1H, OH), 8.31 (d, 1H, pyrazine H, J = 8.0 Hz), 7.44 (s, 1H, CONH2), 5.92 (s, 1H, CONH2). 13C-NMR (75 MHz, DMSO): δ 168.66, 159.69, 153.98, 150.76, 135.68. HRMS (ESI): m/z [M + H]+ calcd for C5H5FN3O2 + : 158.0366; found: 158.0360.</div>
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PAPER</div>
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Chemical Papers (2017), 71(11), 2153-2158.</div>
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<a data-mce-href="https://link.springer.com/article/10.1007%2Fs11696-017-0208-6" href="https://link.springer.com/article/10.1007%2Fs11696-017-0208-6" style="color: #222222;">https://link.springer.com/article/10.1007%2Fs11696-017-0208-6</a></div>
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Below is the link to the electronic supplementary material.</div>
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<a class="print-link" data-mce-href="https://static-content.springer.com/esm/art%3A10.1007%2Fs11696-017-0208-6/MediaObjects/11696_2017_208_MOESM1_ESM.docx" href="https://static-content.springer.com/esm/art%3A10.1007%2Fs11696-017-0208-6/MediaObjects/11696_2017_208_MOESM1_ESM.docx" style="color: #222222; text-decoration-line: none;">Supplementary material 1 (DOCX 514 kb)</a></h3>
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<div style="padding: 0px;"><br /></div><div style="padding: 0px;">Take a tour</div><div style="padding: 0px;"><table class="infobox vcard" style="background-color: #f8f9fa; border-spacing: 3px; border: 1px solid rgb(162, 169, 177); clear: right; color: black; font-family: sans-serif; font-size: 12.32px; line-height: 1.5em; margin: 0.5em 0px 0.5em 1em; padding: 0.2em; width: 22em;"><caption class="fn org" style="font-size: 15.4px; font-weight: bold; padding: 0.2em;">Kerkennah Islands</caption><tbody><tr><td colspan="2" style="text-align: center; vertical-align: top;"><a class="image" href="https://en.wikipedia.org/wiki/File:Kerkennah_Islands_NASA.jpg" style="background: none; color: #0b0080; text-decoration-line: none;"><img alt="Kerkennah Islands NASA.jpg" data-file-height="702" data-file-width="1024" decoding="async" height="165" src="https://upload.wikimedia.org/wikipedia/commons/thumb/4/4e/Kerkennah_Islands_NASA.jpg/240px-Kerkennah_Islands_NASA.jpg" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/4/4e/Kerkennah_Islands_NASA.jpg/360px-Kerkennah_Islands_NASA.jpg 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/4/4e/Kerkennah_Islands_NASA.jpg/480px-Kerkennah_Islands_NASA.jpg 2x" style="border: 0px; vertical-align: middle;" width="240" /></a><div>Kerkennah Islands seen from space</div></td></tr><tr><td colspan="2" style="text-align: center; vertical-align: top;"><div class="center" style="width: 257px;"><div class="locmap" style="clear: both; float: none; margin-left: auto; margin-right: auto; width: 250px;"><div style="margin-left: auto; margin-right: auto; padding: 0px; width: 250px;"><div style="margin-left: auto; margin-right: auto; position: relative; width: 250px;"><a class="image" href="https://en.wikipedia.org/wiki/File:Tunisia_adm_location_map.svg" style="background: none; color: #0b0080; margin-left: auto; margin-right: auto; text-decoration-line: none;" title="Kerkennah Islands is located in Tunisia"><img alt="Kerkennah Islands is located in Tunisia" data-file-height="713" data-file-width="378" decoding="async" height="472" src="https://upload.wikimedia.org/wikipedia/commons/thumb/1/12/Tunisia_adm_location_map.svg/250px-Tunisia_adm_location_map.svg.png" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/1/12/Tunisia_adm_location_map.svg/375px-Tunisia_adm_location_map.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/1/12/Tunisia_adm_location_map.svg/500px-Tunisia_adm_location_map.svg.png 2x" style="border: 0px; margin-left: auto; margin-right: auto; vertical-align: middle;" width="250" /></a><div class="od" style="left: 211.859px; margin-left: auto; margin-right: auto; position: absolute; top: 183.891px;"><div class="id" style="left: -4px; line-height: 0; margin-left: auto; margin-right: auto; position: absolute; top: -4px;"><img alt="Kerkennah Islands" data-file-height="64" data-file-width="64" decoding="async" height="8" src="https://upload.wikimedia.org/wikipedia/commons/thumb/0/0c/Red_pog.svg/8px-Red_pog.svg.png" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/0/0c/Red_pog.svg/12px-Red_pog.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/0/0c/Red_pog.svg/16px-Red_pog.svg.png 2x" style="border: 0px; margin-left: auto; margin-right: auto; vertical-align: middle;" title="Kerkennah Islands" width="8" /></div><div class="pl" style="font-size: 11.2112px; line-height: 12.3323px; margin-left: auto; margin-right: auto; position: absolute; right: 5px; text-align: right; top: -0.75em; width: 6em;"><div style="display: inline; float: right; margin-left: auto; margin-right: auto; padding: 1px;">Kerkennah Islands</div></div></div></div><div style="margin-left: auto; margin-right: auto; padding-top: 0.2em;"></div></div></div></div></td></tr><tr><th colspan="2" style="background-color: #efefef; text-align: center; vertical-align: top;">Geography</th></tr><tr><th scope="row" style="text-align: left; vertical-align: top;">Coordinates</th><td style="vertical-align: top;"><span class="plainlinks nourlexpansion"><span style="white-space: nowrap;"><img alt="" class="wmamapbutton noprint" src="https://upload.wikimedia.org/wikipedia/commons/thumb/5/55/WMA_button2b.png/17px-WMA_button2b.png" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/5/55/WMA_button2b.png/17px-WMA_button2b.png 1x, //upload.wikimedia.org/wikipedia/commons/thumb/5/55/WMA_button2b.png/34px-WMA_button2b.png 2x" style="border: 0px; cursor: pointer; padding: 0px 3px 0px 0px; vertical-align: middle;" title="Show location on an interactive map" /><a class="external text" href="https://geohack.toolforge.org/geohack.php?pagename=Kerkennah_Islands&params=34_42_N_11_11_E_type:isle" rel="nofollow" style="background: none; color: #663366; padding: 0px; text-decoration-line: none; white-space: normal;"><span class="geo-default" style="display: inline;"><span class="geo-dms" style="display: inline;" title="Maps, aerial photos, and other data for this location"><span class="latitude" style="white-space: nowrap;">34°42′N</span> <span class="longitude" style="white-space: nowrap;">11°11′E</span></span></span></a></span></span><span style="font-size: small;"><span id="coordinates" style="float: right; font-size: 11.05px; line-height: 1.5em; margin: 0px; padding: 0px; position: absolute; right: 0px; text-align: right; top: 0px; white-space: nowrap;"><a href="https://en.wikipedia.org/wiki/Geographic_coordinate_system" style="background: none; color: #0b0080; text-decoration-line: none;" title="Geographic coordinate system">Coordinates</a>: <span class="plainlinks nourlexpansion"><img alt="" class="wmamapbutton noprint" src="https://upload.wikimedia.org/wikipedia/commons/thumb/5/55/WMA_button2b.png/17px-WMA_button2b.png" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/5/55/WMA_button2b.png/17px-WMA_button2b.png 1x, //upload.wikimedia.org/wikipedia/commons/thumb/5/55/WMA_button2b.png/34px-WMA_button2b.png 2x" style="border: 0px; cursor: pointer; padding: 0px 3px 0px 0px; vertical-align: middle;" title="Show location on an interactive map" /><a class="external text" href="https://geohack.toolforge.org/geohack.php?pagename=Kerkennah_Islands&params=34_42_N_11_11_E_type:isle" rel="nofollow" style="background: none; color: #663366; padding: 0px; text-decoration-line: none;"><span class="geo-default" style="display: inline;"><span class="geo-dms" style="display: inline;" title="Maps, aerial photos, and other data for this location"><span class="latitude">34°42′N</span> <span class="longitude">11°11′E</span></span></span></a></span></span></span></td></tr><tr><th scope="row" style="text-align: left; vertical-align: top;">Area</th><td style="vertical-align: top;">160 km<sup style="font-size: 9.856px; line-height: 1;">2</sup> (62 sq mi)</td></tr><tr><th colspan="2" style="background-color: #efefef; text-align: center; vertical-align: top;">Administration</th></tr><tr><td colspan="2" style="text-align: center; vertical-align: top;"><b><a href="https://en.wikipedia.org/wiki/Tunisia" style="background: none; color: #0b0080; text-decoration-line: none;" title="Tunisia">Tunisia</a></b></td></tr></tbody></table><p style="color: #202122; font-family: sans-serif; font-size: 14px; margin: 0.5em 0px;"><b>Kerkennah Islands</b> (<a class="mw-redirect" href="https://en.wikipedia.org/wiki/Tunisian_Arabic_language" style="background: none; color: #0b0080; text-decoration-line: none;" title="Tunisian Arabic language">Tunisian Arabic</a>: <span dir="rtl" lang="aeb">قرقنة</span> <i><span class="unicode haudio"><span class="fn"><span style="margin-right: 0.25em; white-space: nowrap;"><a href="https://en.wikipedia.org/wiki/File:9ar9na.wav" style="background: none; color: #0b0080; text-decoration-line: none;" title="About this sound"><img alt="About this sound" data-file-height="20" data-file-width="20" decoding="async" height="11" src="https://upload.wikimedia.org/wikipedia/commons/thumb/8/8a/Loudspeaker.svg/11px-Loudspeaker.svg.png" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/8/8a/Loudspeaker.svg/17px-Loudspeaker.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/8/8a/Loudspeaker.svg/22px-Loudspeaker.svg.png 2x" style="border: 0px; margin: 0px; vertical-align: middle;" width="11" /></a></span><a class="internal" href="https://upload.wikimedia.org/wikipedia/commons/b/b3/9ar9na.wav" style="background: none; color: #0b0080; text-decoration-line: none;" title="9ar9na.wav">qarqna</a></span></span></i>) are a group of islands lying off the east coast of <a href="https://en.wikipedia.org/wiki/Tunisia" style="background: none; color: #0b0080; text-decoration-line: none;" title="Tunisia">Tunisia</a> in the <a href="https://en.wikipedia.org/wiki/Gulf_of_Gab%C3%A8s" style="background: none; color: #0b0080; text-decoration-line: none;" title="Gulf of Gabès">Gulf of Gabès</a>, at <span class="plainlinks nourlexpansion"><span style="position: relative; white-space: nowrap;"><a class="external text" href="https://geohack.toolforge.org/geohack.php?pagename=Kerkennah_Islands&params=34_42_N_11_11_E_" rel="nofollow" style="background: none; color: #663366; padding: 0px; text-decoration-line: none;"><span class="geo-default" style="display: inline;"><span class="geo-dms" style="display: inline;" title="Maps, aerial photos, and other data for this location"><span class="latitude">34°42′N</span> <span class="longitude">11°11′E</span></span></span></a></span></span>. The Islands are low-lying, being no more than 13 metres (43 feet) <a class="mw-redirect" href="https://en.wikipedia.org/wiki/Above_mean_sea_level" style="background: none; color: #0b0080; outline-color: rgb(51, 102, 204);" title="">above sea level</a>. The main islands are <a href="https://en.wikipedia.org/wiki/Chergui" style="background: none; color: #0b0080; text-decoration-line: none;" title="Chergui">Chergui</a> and <a href="https://en.wikipedia.org/wiki/Gharbi,_Tunisia" style="background: none; color: #0b0080; text-decoration-line: none;" title="Gharbi, Tunisia">Gharbi</a>. The archipelago has an area of 160 square kilometres (62 sq mi) and a population of 15,501 (2014).<sup class="reference" id="cite_ref-2" style="font-size: 11.2px; line-height: 1; unicode-bidi: isolate; white-space: nowrap;"><a href="https://en.wikipedia.org/wiki/Kerkennah_Islands#cite_note-2" style="background: none; color: #0b0080; text-decoration-line: none;">[2]</a></sup></p><p style="color: #202122; font-family: sans-serif; font-size: 14px; margin: 0.5em 0px;">Kerkennah's main town, <a href="https://en.wikipedia.org/wiki/Remla" style="background: none; color: #0b0080; text-decoration-line: none;" title="Remla">Remla</a> (on <a href="https://en.wikipedia.org/wiki/Chergui" style="background: none; color: #0b0080; text-decoration-line: none;" title="Chergui">Chergui</a>), has a population of 2,000. The population of the islands significantly decreased during the 1980s due to <a href="https://en.wikipedia.org/wiki/Drought" style="background: none; color: #0b0080; text-decoration-line: none;" title="Drought">drought</a>. The islands were unable to provide suitable <a href="https://en.wikipedia.org/wiki/Irrigation" style="background: none; color: #0b0080; text-decoration-line: none;" title="Irrigation">irrigation</a> systems and, with clean water rapidly running out, many islanders were forced to leave for mainland Tunisia, the nearest town being <a href="https://en.wikipedia.org/wiki/Sfax" style="background: none; color: #0b0080; text-decoration-line: none;" title="Sfax">Sfax</a>.</p><p style="color: #202122; font-family: sans-serif; font-size: 14px; margin: 0.5em 0px;"><a class="image" href="https://en.wikipedia.org/wiki/File:Kerkennah_015.jpg" style="background: none; color: #faa700; font-size: 13.16px; outline-color: rgb(51, 102, 204); text-align: center;"><img alt="" class="thumbimage" data-file-height="2448" data-file-width="3264" decoding="async" height="357" src="https://upload.wikimedia.org/wikipedia/commons/thumb/c/c7/Kerkennah_015.jpg/250px-Kerkennah_015.jpg" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/c/c7/Kerkennah_015.jpg/375px-Kerkennah_015.jpg 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/c/c7/Kerkennah_015.jpg/500px-Kerkennah_015.jpg 2x" style="border: 1px solid rgb(200, 204, 209); vertical-align: middle;" width="473" /></a><span style="background-color: #f8f9fa; font-size: 13.16px; text-align: center;"></span></p><p style="color: #202122; font-family: sans-serif; font-size: 14px; margin: 0.5em 0px;"></p><div class="separator" style="clear: both; text-align: center;"><a href="https://lh3.googleusercontent.com/-dXv-_Qq4Nfc/X9rZyGVDc6I/AAAAAAAA3Wc/qM2MLmT8d_EuEKgr_xEuHXAtHapputT-wCNcBGAsYHQ/image.png" style="margin-left: 1em; margin-right: 1em;"><img alt="" data-original-height="512" data-original-width="386" height="352" src="https://lh3.googleusercontent.com/-dXv-_Qq4Nfc/X9rZyGVDc6I/AAAAAAAA3Wc/qM2MLmT8d_EuEKgr_xEuHXAtHapputT-wCNcBGAsYHQ/w266-h352/image.png" width="266" /></a></div><div class="separator" style="clear: both; text-align: center;"><div class="separator" style="clear: both; text-align: center;"><a href="https://lh3.googleusercontent.com/-BdpMtO_vDaA/X9rZ6LVvuvI/AAAAAAAA3Wg/2hN9mOLDKnMyCO4Cxms_FKaBoRxrQFWyQCNcBGAsYHQ/image.png" style="margin-left: 1em; 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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com49tag:blogger.com,1999:blog-8960696629007291242.post-16724437655581399902020-03-11T04:27:00.001-07:002020-03-11T04:27:47.492-07:00NIDUFEXOR<div dir="ltr" style="text-align: left;" trbidi="on">
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<img alt="Nidufexor Chemical Structure" data-mce-src="https://file.medchemexpress.com/product_pic/hy-109096.gif" src="https://file.medchemexpress.com/product_pic/hy-109096.gif" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div>
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<img alt="Nidufexor.png" data-mce-src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?cid=118063735&t=l" src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?cid=118063735&t=l" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div>
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NIDUFEXOR</div>
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LMB763</div>
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4-[[benzyl-(8-chloro-1-methyl-4<i>H</i>-chromeno[4,3-c]pyrazole-3-carbonyl)amino]methyl]benzoic acid</div>
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Nidufexor is a <b>farnesoid X receptor (FXR)</b> agonist.</div>
<table class="details_info_tbl mce-item-table" style="border: 1px dashed rgb(187, 187, 187); color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;"><tbody>
<tr><th class="details_info_th" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;">Molecular Weight</th><td class="details_info_td" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div id="molecularWeight" style="padding: 0px;">
487.93</div>
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<tr><th class="details_info_th" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;">Formula</th><td class="details_info_td" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div style="padding: 0px;">
C₂₇H₂₂ClN₃O₄</div>
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<tr><th class="details_info_th" style="background: rgb(221, 221, 221); border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 10px 20px;">CAS No.</th><td class="details_info_td" style="border: 1px dashed rgb(187, 187, 187); font-family: inherit; font-size: inherit; padding: 5px 20px;"><div style="padding: 0px;">
1773489-72-7</div>
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PHASE 2 Treatment of Liver and Biliary Tract Disorders,<br />
Agents for Diabetic Nephropathy, NOVARTIS</div>
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<a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22Nidufexor%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22Nidufexor%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">Nidufexor</a></div>
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<a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%221773489-72-7%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%221773489-72-7%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">1773489-72-7</a>, <a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22LMB-763%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22LMB-763%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">LMB-763</a>, <a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22UNII-CJ1PL0TE6J%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22UNII-CJ1PL0TE6J%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">UNII-CJ1PL0TE6J</a>, <a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22CJ1PL0TE6J%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22CJ1PL0TE6J%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">CJ1PL0TE6J</a>, <a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22BCP28929%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22BCP28929%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">BCP28929</a>, <a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22EX-A1854%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22EX-A1854%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">EX-A1854</a></div>
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<a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22Nidufexor%20pound%20LMB-763%20pound(c)%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22Nidufexor%20pound%20LMB-763%20pound(c)%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">Nidufexor pound LMB-763 pound(c)</a></div>
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<a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22ZINC584641402%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22ZINC584641402%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">ZINC584641402</a></div>
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<a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%224-((N-benzyl-8-chloro-1-methyl-1%2C4-dihydrochromeno%5B4%2C3-c%5Dpyrazole-3-carboxamido)methyl)benzoic%20acid%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%224-((N-benzyl-8-chloro-1-methyl-1%2C4-dihydrochromeno%5B4%2C3-c%5Dpyrazole-3-carboxamido)methyl)benzoic%20acid%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoic acid</a></div>
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<a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22HY-109096%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22HY-109096%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">HY-109096</a></div>
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<a data-action="content-link" data-label="Content Link: Depositor-Supplied-Synonyms" data-mce-href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22CS-0039398%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" href="https://www.ncbi.nlm.nih.gov/pcsubstance/?term=%22CS-0039398%22[CompleteSynonym]%20AND%20118063735[StandardizedCID]" rel="nofollow" style="color: #222222;">CS-0039398</a></div>
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<br /></div>
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<img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR1-3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR1-3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div>
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<a data-mce-href="https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.9b01621" href="https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.9b01621" style="color: #222222;">https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.9b01621</a></div>
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1 (7.6 g, 89% yield) as a white solid. Melting point: 232.6 °C.</div>
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1 H NMR (400 MHz, DMSO): δ 12.93 (s, 1H), 7.96−7.85 (m, 2H), 7.71 (dd, J = 7.1, 2.5 Hz, 1H), 7.42−7.20 (m, 8H), 7.06 (dd, J = 8.7, 1.9 Hz, 1H), 5.45 (d, J = 3.9 Hz, 2H), 5.25 (d, J = 9.2 Hz, 2H), 4.58 (d, J = 12.1 Hz, 2H), 4.12 (d, J = 16.6 Hz, 3H).</div>
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13C NMR (101 MHz, DMSO-d6): δ 167.07, 162.21, 151.98, 142.65, 139.18, 132.20, 132.67, 129.70, 129.50, 129.50, 128.53, 128.53, 127.43, 127.43, 127.43, 127.43, 127.43, 125.53, 122.24, 119.0, 117.09, 116.64, 64.51, 50.68, 48.24. LC-MS m/z: 488.2/490.2 (M +H)+ ; chlorine pattern; method 3; RT = 1.41 min.</div>
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Elemental Analysis calcd for C27H22ClN3O4: C 66.46, H 4.54, N 8.61; found: C 66.43, H 4.56, N 8.62.</div>
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TRIS Salt Formation. Methanol (400 mL) was added to a mixture of 1 (4.0 g, 8.2 mmol) and 2-amino-2-hydroxymethylpropane-1,3-diol (TRIS, 1.0 g, 8.2 mmol). The mixture was heated to 70 °C for 0.5 h. After cooling to room temperature, the solvent was removed in vacuum. The residue was sonicated in dichloromethane (10 mL) and concentrated again. The resulting white solid was dried under vacuum overnight. The crude material was crystallized by slurring the solid residue in a 4:1 mixture of acetonitrile and methanol (5 mL). The mixture was stirred at room temperature for 24 h to give 4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno- [4,3-c]pyrazole-3-carboxamido)methyl)benzoic acid TRIS salt as a white salt (3.7 g, 73% yield). Melting point: 195.6 °C. 1 H NMR (400 MHz, DMSO): δ 7.92−7.80 (m, 2H), 7.78−7.64 (m, 1H), 7.41− 7.19 (m, 8H), 7.13−7.00 (m, 1H), 5.44 (s, 2H), 5.25−5.14 (m, 2H), 4.61−4.48 (m, 2H), 4.18−4.03 (m, 3H), 3.39 (s, 7H). TRIS OH masked by water peak. LC-MS m/z: 488.0/490.0 (M+H)+ ; chlorine pattern, method 3. RT = 1.58 min. Elemental Analysis calc for C31H33ClN4O7: C 61.00, H 5.36, N 9.15; found: C 60.84, H 5.34, N 9.13.</div>
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<img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR1-4.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR1-4.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR2.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR2.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR3.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR3.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2020/03/str4.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2020/03/str4.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2020/03/str5.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2020/03/str5.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /><img data-mce-src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR1-5.jpg" src="http://drugapprovalsint.com/wp-content/uploads/2020/03/STR1-5.jpg" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div>
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Patent</div>
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WO 2015069666</div>
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///////NIDUFEXOR, LMB 763, Phase II, PHASE 2, Liver and Biliary Tract Disorders, Diabetic Nephropathy, NOVARTIS</div>
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CN1C(C2=CC(Cl)=CC=C2OC3)=C3C(C(N(CC4=CC=CC=C4)CC5=CC=C(C(O)=O)C=C5)=O)=N1</div>
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com3tag:blogger.com,1999:blog-8960696629007291242.post-38945730519602556862019-10-15T02:56:00.001-07:002019-10-15T02:56:40.271-07:00Catalyst- and additive-free Baeyer–Villiger-type oxidation of α-iodocyclopentenones to α-pyrones: using air as the oxidant<div dir="ltr" style="text-align: left;" trbidi="on">
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<img alt="Graphical abstract: Catalyst- and additive-free Baeyer–Villiger-type oxidation of α-iodocyclopentenones to α-pyrones: using air as the oxidant" data-mce-src="https://pubs.rsc.org/en/Image/Get?imageInfo.ImageType=GA&imageInfo.ImageIdentifier.ManuscriptID=C9GC02725D&imageInfo.ImageIdentifier.Year=2019" src="https://pubs.rsc.org/en/Image/Get?imageInfo.ImageType=GA&imageInfo.ImageIdentifier.ManuscriptID=C9GC02725D&imageInfo.ImageIdentifier.Year=2019" style="height: auto; max-width: 100%;" title="Graphical abstract" /></div>
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An efficient synthetic approach for the synthesis of α-pyrones <em>via</em> Baeyer–Villiger-type oxidation of α-iodocyclopentenones through a catalyst- and additive-free system using air as an environmentally benign oxidant is described. The reaction exhibits excellent functional group compatibility and provides a simple and efficient protocol for the construction of highly functionalized α-pyrones under mild reaction conditions.</div>
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<h2 class="capsule__title fixpadv--m">
Catalyst- and additive-free Baeyer–Villiger-type oxidation of α-iodocyclopentenones to α-pyrones: using air as the oxidant<a data-mce-href="https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC02725D?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#fn1" href="https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC02725D?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#fn1" title="Electronic supplementary information (ESI) available: Experimental procedures, spectral data, and crystallographic data (CIF). CCDC: 1937263. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c9gc02725d">†</a></h2>
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<span class="article__author-link"><a data-mce-href="https://pubs.rsc.org/en/results?searchtext=Author%3AYuanyuan%20Zhou" href="https://pubs.rsc.org/en/results?searchtext=Author%3AYuanyuan%20Zhou">Yuanyuan Zhou</a>,<sup><i>a</i></sup> </span><span class="article__author-link"><a data-mce-href="https://pubs.rsc.org/en/results?searchtext=Author%3AXianxiao%20Chen" href="https://pubs.rsc.org/en/results?searchtext=Author%3AXianxiao%20Chen">Xianxiao Chen</a>,<sup><i>a</i></sup> </span><span class="article__author-link"><a data-mce-href="https://pubs.rsc.org/en/results?searchtext=Author%3AXiangxiang%20Ling" href="https://pubs.rsc.org/en/results?searchtext=Author%3AXiangxiang%20Ling">Xiangxiang Ling</a><sup><i>a</i></sup> and </span><span class="article__author-link"><a data-mce-href="https://pubs.rsc.org/en/results?searchtext=Author%3AWeidong%20Rao" href="https://pubs.rsc.org/en/results?searchtext=Author%3AWeidong%20Rao">Weidong Rao</a> <span class="orcid ver-b"><a data-mce-href="https://orcid.org/0000-0002-6088-7278" href="https://orcid.org/0000-0002-6088-7278" target="_blank" title="Select to open ORCID record (orcid.org/0000-0002-6088-7278) in a new window"><img alt="ORCID logo" data-mce-src="https://www.rsc-cdn.org/pubs-core/2019.0.1202/content/NewImages/orcid_16x16.png" src="https://www.rsc-cdn.org/pubs-core/2019.0.1202/content/NewImages/orcid_16x16.png" style="height: auto; max-width: 100%;" /></a></span> *<sup><i>a</i></sup> </span></div>
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<a class="drawer__handle" data-mce-href="https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC02725D?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#" href="https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC02725D?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#"> Author affiliations</a><br />
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*Corresponding authors</div>
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<sup>a</sup>Jiangsu Key Laboratory of Biomass-based Green Fuels and Chemicals, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China<br /><b>E-mail:</b><a data-mce-href="mailto:weidong@njfu.edu.cn" href="mailto:weidong@njfu.edu.cn" title="weidong@njfu.edu.cn">weidong@njfu.edu.cn</a></div>
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6-Cyclohexyl-4-phenyl-2H-pyran-2-one (2e)[S3]</div>
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Product 2e was obtained as a pale-yellow solid in 68% yield (52 mg) following the general procedure, mp 96-97 °C;</div>
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1H NMR (600 MHz, CDCl3) δ 7.58-7.56 (m, 2H), 7.48-7.46 (m, 3H), 6.34 (d, J = 1.3 Hz, 1H), 6.26 (d, J = 0.8 Hz, 1H), 2.48 (tt, J = 11.8, 3.3 Hz, 1H), 2.04-2.01 (m, 2H), 1.87-1.84 (m, 2H), 1.47 (qd, J = 12.5, 3.0 Hz, 2H), 1.39-1.32 (m, 2H), 1.28-1.23 (m, 2H);</div>
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13C NMR (150 MHz, CDCl3) δ 169.8, 163.6, 155.6, 136.2, 130.5, 129.1, 126.7, 108.4, 100.9, 42.5, 30.6, 25.9, 25.8</div>
<a data-mce-href="http://www.rsc.org/suppdata/c9/gc/c9gc02725d/c9gc02725d1.pdf" href="http://www.rsc.org/suppdata/c9/gc/c9gc02725d/c9gc02725d1.pdf">http://www.rsc.org/suppdata/c9/gc/c9gc02725d/c9gc02725d1.pdf</a><br />
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/////////<a data-mce-href="https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC02725D?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract" href="https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC02725D?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract">https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C9GC02725D?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract</a></div>
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com136tag:blogger.com,1999:blog-8960696629007291242.post-76231731038616995712019-09-10T20:43:00.001-07:002019-09-10T20:43:05.836-07:00Ethyl 4-(4-cyclopropyl-2-oxo-2H-pyran-6-yl)butanoate<div dir="ltr" style="text-align: left;" trbidi="on">
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Catalyst- and Additive-Free Baeyer−Villiger-type Oxidation of α-Iodocyclopentenones to α-Pyrones: Using Air as the Oxidant</h2>
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<span class="article__author-link"><a data-mce-href="https://pubs.rsc.org/en/results?searchtext=Author%3AYuanyuan%20Zhou" href="https://pubs.rsc.org/en/results?searchtext=Author%3AYuanyuan%20Zhou">Yuanyuan Zhou</a>, </span><span class="article__author-link"><a data-mce-href="https://pubs.rsc.org/en/results?searchtext=Author%3AXianxiao%20Chen" href="https://pubs.rsc.org/en/results?searchtext=Author%3AXianxiao%20Chen">Xianxiao Chen</a>, </span><span class="article__author-link"><a data-mce-href="https://pubs.rsc.org/en/results?searchtext=Author%3AXiangxiang%20Ling" href="https://pubs.rsc.org/en/results?searchtext=Author%3AXiangxiang%20Ling">Xiangxiang Ling</a> and </span><span class="article__author-link"><a data-mce-href="https://pubs.rsc.org/en/results?searchtext=Author%3AWeidong%20Rao" href="https://pubs.rsc.org/en/results?searchtext=Author%3AWeidong%20Rao">Weidong Rao</a> </span></div>
<h3 class="h--heading3" style="color: #333333; font-family: Georgia, "Times New Roman", "Bitstream Charter", Times, serif;">
Abstract</h3>
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An efficient synthetic approach for the synthesis of α-pyrones via Baeyer−Villiger-type oxidation of α-iodocyclopentenones through a catalyst- and additive-free system using air as an environmentally benign oxidant is described. The reaction exhibits excellent functional group compatibility and provides a simple and efficient protocol for the construction of highly functionalized α-pyrones under mild reaction conditions.</div>
Ethyl 4-(4-cyclopropyl-2-oxo-2H-pyran-6-yl)butanoate (2aa) Product 2aa was obtained as yellow oil in 50% yield (38 mg) following the general procedure; 1H NMR (600 MHz, CDCl3) δ 5.84 (s, 1H), 5.61 (s, 1H), 4.13-4.09 (m, 2H), 2.48 (t, J = 7.3 Hz, 2H), 2.33 (td, J = 7.3, 2.3 Hz, 2H), 1.97-1.94 (m, 2H), 1.66-1.63 (m, 1H), 1.26-1.22 (m, 3H), 1.07-1.05 (m, 2H), 0.80-0.79 (m, 2H); 13C NMR (150 MHz, CDCl3) δ 172.8, 163.9, 163.0, 162.8, 106.7, 102.1, 60.5, 33.2, 33.0, 22.1, 15.4, 14.2, 10.0; HRMS (ESI) calcd. for C14H18O4Na [M+Na]+ : 273.1097, found: 273.1101<br />
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com71tag:blogger.com,1999:blog-8960696629007291242.post-81533814026397508242019-09-05T03:22:00.003-07:002019-09-05T03:22:42.562-07:004-(trifluoromethoxy)benzyl trichloroacetimidate: <div dir="ltr" style="text-align: left;" trbidi="on">
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4-(Trifluoromethoxy)benzyl Trichloroacetimidate</h3>
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<span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">To a stirred suspension of NaH (60%, 127 mg, 3.45 mmol) in </span><i style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">t</i><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">-BuOMe (100 mL) was added 4-(trifluoromethoxy)benzyl alcohol </span><b style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">11</b><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> (5 mL, 34.5 mmol) dropwise by syringe at room temperature. After H</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">2</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> evolution had ceased (about 5 min), the clear mixture was cooled to 0 °C. Cl</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">3</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">CCN (3.46 mL, 34.5 mmol) was added dropwise by syringe, and the resulting solution was stirred for 1 h. After warming to room temperature, the solution was concentrated in vacuo, and the residue was resuspended in heptane (100 mL) containing MeOH (0.14 mL, 3.45 mmol). After 10 min of stirring, the suspension was filtered through a thin bed of silica and washed with heptane. Concentration in vacuo affords the title compound as a yellow-orange liquid (11.4 g, 98%) that was used directly without further purification. </span><i style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">R</i><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;"><i>f</i></span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> 0.3 (5% EtOAc/hexanes);</span></div>
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<span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> </span><span style="background-color: white; bottom: 1ex; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; vertical-align: baseline;">1</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">H NMR (501 MHz, CDCl</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">3</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">) δ 8.43 (s, 1H), 7.48 (d, </span><i style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">J</i><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> = 8.2 Hz, 2H), 7.24 (d, </span><i style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">J</i><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> = 8.2 Hz, 2H), 5.35 (s, 2H); </span></div>
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<span style="background-color: white; bottom: 1ex; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; vertical-align: baseline;">13</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">C NMR (126 MHz, CDCl</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">3</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">) δ 162.6, 149.3, 134.3, 129.4, 121.6, 121.3, 119.6, 69.9; </span></div>
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<span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">IR [CH</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">2</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">Cl</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">2</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> solution] ν</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">max</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> (cm</span><span style="background-color: white; bottom: 1ex; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; vertical-align: baseline;">−1</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">) 3345, 2954, 1667, 1511, 1261, 1221, 1166, 1077, 998, 828, 797, 649; </span></div>
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<span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">HRMS (ESI-TOF) calcd for C</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">10</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">H</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">7</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">Cl</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">3</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">F</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">3</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">NO</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">2</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;"> 334.95, found C</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">8</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">H</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">6</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">F</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 12px; height: 0px; line-height: 0; position: relative; text-align: start; top: 0.5ex; vertical-align: baseline;">3</span><span style="background-color: white; color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px; text-align: start;">O 174.03.</span></div>
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com1tag:blogger.com,1999:blog-8960696629007291242.post-49154784330478414852019-09-05T03:19:00.002-07:002019-09-05T03:19:26.542-07:00(R)-3-Chloro-2-hydroxypropyl-4-methoxybenzoate <div dir="ltr" style="text-align: left;" trbidi="on">
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<h3 class="article-section__title" id="_i7" style="background-color: white; color: #222222; font-family: "PT Serif", TimesNewRoman, "Times New Roman", Times, Baskerville, Georgia, serif; font-size: 24px; line-height: 26.4px; margin: 0px; padding: 30px 0px 10px;">
(<i>R</i>)-3-Chloro-2-hydroxypropyl-4-methoxybenzoate <b>10</b></h3>
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To a stirred solution of (<i>R</i>)-3-chloro-1,2-propanediol (6.61 g, 59.8 mmol) in CH<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span>Cl<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span> (120 mL) was added imidazole (4.07 g, 59.8 mmol). After the reaction mixture had cooled to 0 °C, <i>p</i>-methoxybenzoyl chloride (10.2 g, 59.8 mmol) in CH<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span>Cl<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span> (10 mL) was added dropwise via addition funnel. The resulting solution was allowed to warm to room temperature and stirred until complete consumption of starting material by thin layer chromatography (TLC). The mixture was poured into saturated aq NH<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">4</span>Cl (150 mL), and the aqueous layer was extracted with CH<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span>Cl<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span> (3 × 100 mL). The combined organic extracts were dried (MgSO<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">4</span>), filtered, and concentrated in vacuo to provide chlorohydrin <b>10</b>as a clear, viscous oil (11.43 g, 78%) that was used without further purification. <i>R</i><span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;"><i>f</i></span> 0.3 (20% EtOAc/hexanes); ee >99% as determined by chiral SFC (see the <a class="ref internalNav" data-mce-href="https://pubs.acs.org/doi/full/10.1021/jo1015807#si1" href="https://pubs.acs.org/doi/full/10.1021/jo1015807#si1" style="color: #222222;">Supporting Information</a>); </div>
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<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">1</span>H NMR (500 MHz, CDCl<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">3</span>) δ 8.07−7.94 (m, 2H), 7.00−6.88 (m, 2H), 4.46 (d, <i>J</i> = 5.1 Hz, 2H), 4.22 (dd, <i>J</i> = 10.6, 5.3 Hz, 1H), 3.88 (s, 3H), 3.78−3.64 (m, 2H), 2.73 (d, <i>J</i> = 5.6 Hz, 1H); </div>
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<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">13</span>C NMR (126 MHz, CDCl<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">3</span>) δ 166.7, 163.9, 132.1, 121.9, 114.0, 70.1, 65.7, 55.7, 46.3; </div>
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IR [CH<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span>Cl<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span> solution] ν<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">max</span> (cm<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">−1</span>) 3454, 2959, 2889, 1713, 1606, 1512, 1259, 1170, 1104, 1028, 848, 770, 697, 614; </div>
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HRMS (ESI-TOF) calcd for C<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">11</span>H<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">13</span>ClO<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">4</span> (M)<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">+</span>244.0573, found 244.0501.</div>
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<a href="https://pubs.acs.org/doi/full/10.1021/jo1015807" style="background-color: white; color: #0c5390; font-family: Helvetica, Arial, Tahoma, sans-serif; font-size: 14px; text-decoration-line: none;">https://pubs.acs.org/doi/full/10.1021/jo1015807</a><br />
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<a href="https://pubs.acs.org/doi/suppl/10.1021/jo1015807/suppl_file/jo1015807_si_001.pdf">https://pubs.acs.org/doi/suppl/10.1021/jo1015807/suppl_file/jo1015807_si_001.pdf</a></div>
DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com2tag:blogger.com,1999:blog-8960696629007291242.post-64058421558330195902019-09-04T03:56:00.000-07:002019-09-04T03:56:02.576-07:00Pretomanid<div dir="ltr" style="text-align: left;" trbidi="on">
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Pretomanid</div>
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read syn <a href="https://newdrugapprovals.org/2019/09/04/pretomanid-%e3%83%97%e3%83%ac%e3%83%88%e3%83%9e%e3%83%8b%e3%83%89/">https://newdrugapprovals.org/2019/09/04/pretomanid-%e3%83%97%e3%83%ac%e3%83%88%e3%83%9e%e3%83%8b%e3%83%89/</a><br />
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The combined organic extracts were washed with brine, dried (Na<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">2</span>SO<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">4</span>), filtered, and concentrated. Chromatography (75% EtOAc/hexanes) followed by recrystallization (<i>i</i>-PrOH/hexanes) affords PA-824 (<span style="font-weight: 700;">1</span>) (2.41 g, 62%) as a crystalline solid. Mp 150−151 °C (lit.<a class="ref cit11a" href="https://www.blogger.com/null" style="color: #0c5390;">(11a)</a> mp 149−150); <i>R</i><span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;"><i>f</i></span> 0.2 (75% EtOAc/hexanes); ee >99.9% as determined by chiral SFC (see the <a class="ref internalNav" href="https://pubs.acs.org/doi/full/10.1021/jo1015807#si1" style="color: #0c5390; text-decoration-line: none;">Supporting Information</a>);</div>
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<span style="font-size: 9px; line-height: 0; position: relative; top: -0.5em; vertical-align: baseline;">1</span>H NMR (500 MHz, <i>d</i><span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">6</span>-DMSO) δ 8.09 (s, 1H), 7.48 (d, <i>J</i> = 8.6 Hz, 2H), 7.39 (d, <i>J</i> = 8.2 Hz, 2H), 4.81−4.62 (m, 3H), 4.51 (d, <i>J</i> = 11.9 Hz, 1H), 4.39−4.19 (m, 3H);</div>
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<span style="font-size: 9px; line-height: 0; position: relative; top: -0.5em; vertical-align: baseline;">13</span>C NMR (126 MHz, <i>d</i><span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">6</span>-DMSO) δ 148.7, 148.1, 143.0, 138.3, 130.4, 122.0, 120.0, 119.8, 69.7, 68.8, 67.51, 47.73;</div>
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IR [CH<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">2</span>Cl<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">2</span> solution] ν<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">max</span> (cm<span style="font-size: 9px; line-height: 0; position: relative; top: -0.5em; vertical-align: baseline;">−1</span>) 2877, 1580, 1543, 1509, 1475, 1404, 1380, 1342, 1281, 1221, 1162, 1116, 1053, 991, 904, 831, 740;</div>
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HRMS (ESI-TOF) calcd for C<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">14</span>H<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">12</span>F<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">3</span>N<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">3</span>O<span style="bottom: -0.25em; font-size: 9px; line-height: 0; position: relative; vertical-align: baseline;">5</span> 359.0729, found 359.0728.</div>
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<a href="https://pubs.acs.org/doi/full/10.1021/jo1015807" style="color: #0c5390; text-decoration-line: none;">https://pubs.acs.org/doi/full/10.1021/jo1015807</a></div>
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com4tag:blogger.com,1999:blog-8960696629007291242.post-63474166490509444412019-08-06T04:03:00.001-07:002019-08-06T04:03:14.784-07:00Verubecestat Impurity 10<div dir="ltr" style="text-align: left;" trbidi="on">
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Verubecestat</h1>
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Verubecestat Impurity 10</div>
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1H NMR (600 MHz, Acetonitrile-d3) δ 9.86 (s, 1H), 8.21 (d, J = 3.0 Hz, 1H), 8.02 (dd, J = 7.5, 2.8 Hz, 1H), 7.96 (d, J = 8.9 Hz, 1H), 7.81 (ddd, J = 8.7, 4.2, 2.7 Hz, 1H), 7.24 (dd, J = 8.9, 3.0 Hz, 1H), 7.19 (d, J = 8.7 Hz, 2H), 7.07 (dd, J = 12.0, 8.7 Hz, 1H), 6.88 (d, J = 8.7 Hz, 2H), 4.06 (d, J = 14.6 Hz, 1H), 3.92 (d, J = 14.6 Hz, 1H), 3.81 (d, J = 14.2 Hz, 1H), 3.75 (s, 3H), 3.65 (ddd, J = 11.7, 9.8, 3.9 Hz, 1H), 3.39 (d, J = 14.3 Hz, 1H), 2.86 (s, 3H), 2.59 (td, J = 10.3, 4.0 Hz, 1H), 2.55 (s, 3H), 2.28 (s, 3H), 2.22 – 2.09 (m, 1H), 1.78 – 1.71 (m, 2H), 1.69 – 1.64 (m, 1H), 1.61 – 1.54 (m, 4H), 1.41 (qt, J = 13.7, 3.9 Hz, 1H), 1.28 (qt, J = 13.3, 3.8 Hz, 1H), 1.17 – 1.07 (m, 1H).</div>
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13C NMR (151 MHz, Acetonitrile-d3) δ 163.79, 160.26, 156.68, 149.74, 137.95, 136.00 (d, J = 2.3Hz), 134.69 (d, J = 13.7 Hz), 134.15, 130.58, 129.35, 123.67, 120.82 (d, J = 8.7 Hz), 120.51 (d, J = 4.3 Hz), 119.60, 116.85, 114.82, 63.09, 60.77, 60.31 (d, J = 5.5 Hz), 55.84, 54.27 (d, J = 3.4 Hz), 53.30, 34.11, 33.75, 31.85, 30.96, 30.23 (d, J = 3.3 Hz), 28.91, 26.13, 25.25.</div>
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19F NMR (564 MHz, Acetonitrile-d3) δ -119.08. HRMS [M+H] (C32H43FN6O4S) calc. 627.3123, obs. 627.3151.</div>
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<span class=" hlFld-Tiltle ">Improved Process for a Copper-Catalyzed C–N Coupling in the Synthesis of Verubecestat</span></div>
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<span class="hlFld-ContribAuthor">Eric M. Phillips<strong>*</strong></span></div>
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<a data-mce-href="https://pubs.acs.org/action/showCitFormats?doi=10.1021/acs.oprd.9b00192&href=/doi/10.1021/acs.oprd.9b00192" href="https://pubs.acs.org/action/showCitFormats?doi=10.1021/acs.oprd.9b00192&href=/doi/10.1021/acs.oprd.9b00192" style="color: #222222;" title="Cite This"><i class="icon-check-circle"></i><strong>Cite This:</strong></a><i>Org. Process Res. Dev.</i>2019XXXXXXXXXX-XXX</div>
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<span class="pub-date epub-date">Publication Date</span><span class="date-separator">:</span><span class="pub-date-value">July 23, 2019</span></div>
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<a data-mce-href="https://doi.org/10.1021/acs.oprd.9b00192" href="https://doi.org/10.1021/acs.oprd.9b00192" style="color: #222222;" title="DOI URL">https://doi.org/10.1021/acs.oprd.9b00192</a></div>
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Verubecestat is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor which was previously evaluated for the treatment of Alzheimer’s disease. The synthesis of verubecestat relies on a Cu-catalyzed carbon–nitrogen coupling. During process development, observations of impurity formation led to a more robust understanding of the catalyst. The transformation was discovered to be highly dependent on the ratio of ligand to substrate concentration during the course of the reaction. In-depth studies aimed at attaining mechanistic understanding provided an explanation of experimental findings and ultimately led to the identification of conditions that resulted in a more robust process.</div>
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<img data-mce-src="https://pubs.acs.org/na101/home/literatum/publisher/achs/journals/content/oprdfk/0/oprdfk.ahead-of-print/acs.oprd.9b00192/20190723/images/medium/op-2019-001927_0008.gif" src="https://pubs.acs.org/na101/home/literatum/publisher/achs/journals/content/oprdfk/0/oprdfk.ahead-of-print/acs.oprd.9b00192/20190723/images/medium/op-2019-001927_0008.gif" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></div>
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//////////////<a data-mce-href="https://pubs.acs.org/doi/suppl/10.1021/acs.oprd.9b00192/suppl_file/op9b00192_si_001.pdf" href="https://pubs.acs.org/doi/suppl/10.1021/acs.oprd.9b00192/suppl_file/op9b00192_si_001.pdf" style="color: #222222;">https://pubs.acs.org/doi/suppl/10.1021/acs.oprd.9b00192/suppl_file/op9b00192_si_001.pdf</a></div>
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<a data-mce-href="https://pubs.acs.org/doi/10.1021/acs.oprd.9b00192" href="https://pubs.acs.org/doi/10.1021/acs.oprd.9b00192" style="color: #222222;">https://pubs.acs.org/doi/10.1021/acs.oprd.9b00192</a></div>
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///////////Verubecestat, Impurity 10</div>
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com0tag:blogger.com,1999:blog-8960696629007291242.post-11853443327331056352019-04-08T05:58:00.001-07:002019-04-08T05:58:38.994-07:00AB 680 « New Drug Approvals<a href="https://newdrugapprovals.org/2019/04/08/ab-680/">AB 680 « New Drug Approvals</a>: AB 680 C20H24ClFN4O9P2, 580.827 g/mol Cas 2105904-82-1 1H-Pyrazolo[3,4-b]pyridin-4-amine, 6-chloro-N-[(1S)-1-(2-fluorophenyl)ethyl]-1-[5-O-[hydroxy(phosphonomethyl)phosphinyl]-β-D-ribofuranosyl]- […DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com14tag:blogger.com,1999:blog-8960696629007291242.post-59725511288872961742019-04-02T06:46:00.001-07:002019-04-02T06:46:48.725-07:00RISDIPLAM , リスジプラム « New Drug Approvals<a href="https://newdrugapprovals.org/2019/04/02/risdiplam-%e3%83%aa%e3%82%b9%e3%82%b8%e3%83%97%e3%83%a9%e3%83%a0/">RISDIPLAM , リスジプラム « New Drug Approvals</a>DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com1tag:blogger.com,1999:blog-8960696629007291242.post-2152938939762122862019-03-27T01:59:00.000-07:002019-03-27T02:02:42.434-07:00Taselisib<div dir="ltr" style="text-align: left;" trbidi="on">
<img alt="Taselisib skeletal.svg" src="https://upload.wikimedia.org/wikipedia/commons/thumb/4/44/Taselisib_skeletal.svg/220px-Taselisib_skeletal.svg.png" /><br />
TASELISIB<br />
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SYNTHESIS........<a href="https://newdrugapprovals.org/2018/06/15/rg-7604taselisib/">https://newdrugapprovals.org/2018/06/15/rg-7604taselisib/</a><br />
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CLIP</div>
<h1 class="articleTitle" style="color: #222222; font-family: "PT Serif", TimesNewRoman, "Times New Roman", Times, Baskerville, Georgia, serif; font-size: 36px; line-height: 39.6px; margin: 0px; padding: 30px 0px 10px;">
<span class="hlFld-Title">Manufacture of the PI3K β-Sparing Inhibitor Taselisib. Part 2: Development of a Highly Efficient and Regioselective Late-Stage Process</span></h1>
<div id="articleMeta" style="color: #222222; font-family: "Open Sans", Tahoma, Verdana, Segoe, sans-serif; font-size: 16px;">
<div id="authors">
<span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/St-Jean%2C+Fr%C3%A9d%C3%A9ric" href="https://pubs.acs.org/author/St-Jean%2C+Fr%C3%A9d%C3%A9ric" id="authors" style="color: #222222;">Frédéric St-Jean</a><a class="ref" data-mce-href="https://pubs.acs.org/doi/10.1021/acs.oprd.9b00050#cor1" href="https://pubs.acs.org/doi/10.1021/acs.oprd.9b00050#cor1" style="color: #222222;">*</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span><span class="orcid-link-icon"> <a data-mce-href="http://orcid.org/0000-0001-8818-0218" href="http://orcid.org/0000-0001-8818-0218" style="color: #222222;" target="_blank"><img data-mce-src="https://pubs.acs.org/templates/jsp/images/orcid.png" src="https://pubs.acs.org/templates/jsp/images/orcid.png" style="height: auto; margin-bottom: 10px; margin-top: 8px; max-width: 100%;" /></a></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Remarchuk%2C+Travis" href="https://pubs.acs.org/author/Remarchuk%2C+Travis" id="authors" style="color: #222222;">Travis Remarchuk</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Angelaud%2C+R%C3%A9my" href="https://pubs.acs.org/author/Angelaud%2C+R%C3%A9my" id="authors" style="color: #222222;">Rémy Angelaud</a><a class="ref" data-mce-href="https://pubs.acs.org/doi/10.1021/acs.oprd.9b00050#cor2" href="https://pubs.acs.org/doi/10.1021/acs.oprd.9b00050#cor2" style="color: #222222;">*</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Carrera%2C+Diane+E" href="https://pubs.acs.org/author/Carrera%2C+Diane+E" id="authors" style="color: #222222;">Diane E. Carrera</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Beaudry%2C+Danial" href="https://pubs.acs.org/author/Beaudry%2C+Danial" id="authors" style="color: #222222;">Danial Beaudry</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Malhotra%2C+Sushant" href="https://pubs.acs.org/author/Malhotra%2C+Sushant" id="authors" style="color: #222222;">Sushant Malhotra</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/McClory%2C+Andrew" href="https://pubs.acs.org/author/McClory%2C+Andrew" id="authors" style="color: #222222;">Andrew McClory</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Kumar%2C+Archana" href="https://pubs.acs.org/author/Kumar%2C+Archana" id="authors" style="color: #222222;">Archana Kumar</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Ohlenbusch%2C+Gerd" href="https://pubs.acs.org/author/Ohlenbusch%2C+Gerd" id="authors" style="color: #222222;">Gerd Ohlenbusch</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">‡</span></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Schuster%2C+Andreas+M" href="https://pubs.acs.org/author/Schuster%2C+Andreas+M" id="authors" style="color: #222222;">Andreas M. Schuster</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">‡</span></span></span><span class="NLM_x">, and </span><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Gosselin%2C+Francis" href="https://pubs.acs.org/author/Gosselin%2C+Francis" id="authors" style="color: #222222;">Francis Gosselin</a><span class="NLM_xref-aff"><span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span></span></span></div>
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<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">†</span> <span class="institution">Department of Small Molecule Process Chemistry</span>, <span class="institution">Genentech Inc.</span>, <span class="addr-line">1 DNA Way</span>, South San Francisco, California 94080, <span class="country">United States</span></div>
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<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">‡</span> <span class="institution">Small Molecules Technical Development PTDC-C</span>, <span class="institution">F. Hoffmann-La Roche Ltd.</span>, <span class="addr-line">Grenzacherstrasse 124</span>, 4070 Basel, <span class="country">Switzerland</span></div>
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<cite>Org. Process Res. Dev.</cite>, Article ASAP</div>
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<strong>DOI: </strong>10.1021/acs.oprd.9b00050</div>
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*E-mail: <a data-mce-href="mailto:stjean.frederic@gene.com" href="mailto:stjean.frederic@gene.com" style="color: #222222;">stjean.frederic@gene.com</a>. (F.St.-J.), *E-mail: <a data-mce-href="mailto:angelaud.remy@gene.com" href="mailto:angelaud.remy@gene.com" style="color: #222222;">angelaud.remy@gene.com</a>. (R.A.)</div>
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A highly efficient and regioselective manufacturing route for the phosphoinositide 3-kinase β-sparing inhibitor taselisib was developed. Highlights of the synthesis include: (1) magnesium-mediated formation of a challenging cyclic amidine; (2) regioselective imidazole construction via alkylation/condensation with bromopyruvic acid; and (3) triazole formation with 2-isopropyl acetamidrazone to generate the key bromobenzoxazepine core intermediate. Subsequent highly efficient one-pot palladium-catalyzed Miyaura borylation/Suzuki cross-coupling/saponification, followed by a 1,1′-carbonyldiimidazole-mediated coupling with ammonia, led to the pentacyclic taselisib. This new synthetic approach provides a more efficient route to taselisib with a significant decrease in process mass intensity compared to the previous early development routes to the bromobenzoxazepine core. Finally, implementation of a controlled crystallization provided the active pharmaceutical ingredient with the desired polymorphic form.</div>
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Taselisib was obtained in 90% yield (16.2 kg) as a white to off-white solid (>99.9 wt %; >99.9 A%) as Form B crystal.</div>
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mp (DSC): 257–258 °C.</div>
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HRMS (ESI-CID) <i>m</i>/<i>z</i> Calcd for [M + H]<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">+</span> C<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">24</span>H<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">29</span>N<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">8</span>O<span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">2</span>: 461.2408; found: 461.2409.</div>
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<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">1</span>H NMR (600 MHz, DMSO-<i>d</i><span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">6</span>) δ ppm 8.41 (s, 1H), 8.37 (d, <i>J</i> = 8.4, 1H), 8.02 (s, 1H), 7.88 (m, 1H), 7.45 (dd, <i>J</i> = 8.4, 1.7 Hz, 1H), 7.36 (d, <i>J</i> = 1.7 Hz, 1H), 7.20 (br s, 1H), 6.84 (br s, 1 H), 5.83 (sept, <i>J</i> = 6.6 Hz, 1H), 4.53–4.51 (m, 2H), 4.52 (m, 2H), 2.26 (s, 3H), 1.75 (s, 6H), 1.47 (d, <i>J</i> = 6.7 Hz, 6H).</div>
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<span style="bottom: 1ex; font-size: 12px; height: 0px; line-height: 0; position: relative; vertical-align: baseline;">13</span>C NMR (DMSO-<i>d</i><span style="font-size: 12px; height: 0px; line-height: 0; position: relative; top: 0.5ex; vertical-align: baseline;">6</span>, 151 MHz) δ = 173.8, 158.3, 155.9, 147.3, 144.0, 136.6, 134.6, 130.3, 129.9, 126.4, 123.6, 120.4, 119.3, 116.2, 115.3, 68.3, 64.5, 49.9, 49.7, 25.5, 25.5, 22.3, 22.3, 13.8.</div>
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<a data-mce-href="https://pubs.acs.org/doi/10.1021/acs.oprd.9b00050" href="https://pubs.acs.org/doi/10.1021/acs.oprd.9b00050" style="color: #222222;">https://pubs.acs.org/doi/10.1021/acs.oprd.9b00050</a></div>
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<a data-mce-href="https://pubs.acs.org/doi/suppl/10.1021/acs.oprd.9b00050/suppl_file/op9b00050_si_001.pdf" href="https://pubs.acs.org/doi/suppl/10.1021/acs.oprd.9b00050/suppl_file/op9b00050_si_001.pdf" style="color: #222222;">https://pubs.acs.org/doi/suppl/10.1021/acs.oprd.9b00050/suppl_file/op9b00050_si_001.pdf</a></div>
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Ultraviolet/Visible Spectroscopy</div>
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Apparatus: Perkin Elmer, UV-6190, Lambda 25</div>
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Solvent: Acetonitrile/Water 1:1 (v/v)</div>
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<em>“ALL FOR DRUGS” CATERS TO EDUCATION GLOBALLY, No commercial exploits are done or advertisements added by me. This is a compilation for educational purposes only. P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent</em></h3>
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com3tag:blogger.com,1999:blog-8960696629007291242.post-4970494751923771722019-03-27T01:50:00.000-07:002019-03-27T01:50:11.054-07:001-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxylic pivalic anhydride<div dir="ltr" style="text-align: left;" trbidi="on">
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1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxylic pivalic anhydride (10): tan solid,</div>
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mp (DSC): onset = 172.4 °C, peak temperature = 173.0 °C;</div>
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1H NMR (400 MHz, CD3CN) δ 8.23 (d, J = 7.6 Hz, 1 H), 7.35–7.25 (m, 4 H), 6.36 (d, J = 8.0 Hz, 1 H), 2.02 (s, 3 H), 1.25 (s, 9 H);</div>
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13C NMR (100 MHz, CD3CN) 175.9 (1 C), 163.6 (d, 1 C, JCF = 245.4 Hz), 162.9 (1 C ), 161.1 (1 C), 158.2 (1 C), 148.6 (1 C), 135.7 (1 C), 131.0 (d, JCF = 8.7 Hz, 2 C), 117.7 (d, JCF = 23.2 Hz, 2 C), 116.0 (1 C), 107.1 (1 C), 40.4 (1 C), 27.0 (3 C), 22.8 (1 C);</div>
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19F NMR (376 MHz, CD3CN) δ -114.2 (m, 1 F);</div>
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IR (ATR, cm-1 ) 2966 (w), 2939 (w), 2876 (w), 1789 (vs), 1697 (s), 1682 (vs), 1554 (s), 1509 (vs);</div>
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HRMS calcd for C18H18O4NFNa (M+Na+ ) = 354.1112; found 354.1113, δ = 0.3 ppm.</div>
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com1tag:blogger.com,1999:blog-8960696629007291242.post-12904703085403135292019-01-31T01:38:00.002-08:002019-01-31T01:38:44.617-08:00Telescoped Sequence of Exothermic and Endothermic Reactions in Multistep Flow Synthesis<div dir="ltr" style="text-align: left;" trbidi="on">
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<a class="showFiguresEvent" data-mce-href="https://pubs.acs.org/doi/10.1021/acs.oprd.8b00008#" href="https://pubs.acs.org/doi/10.1021/acs.oprd.8b00008#" id="absImg" title="Open Figure Viewer"><img alt="Abstract Image" data-mce-src="https://pubs.acs.org/appl/literatum/publisher/achs/journals/content/oprdfk/0/oprdfk.ahead-of-print/acs.oprd.8b00008/20190122/images/medium/op-2018-00008g_0008.gif" src="https://pubs.acs.org/appl/literatum/publisher/achs/journals/content/oprdfk/0/oprdfk.ahead-of-print/acs.oprd.8b00008/20190122/images/medium/op-2018-00008g_0008.gif" style="height: auto; max-width: 100%;" /></a></div>
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A multistep sequential flow synthesis of isopropyl phenol is demonstrated, involving 4-step exothermic, endothermic, and temperature sensitive reactions such as nitration, reduction, diazotization, and high temperature hydrolysis. Nitration of cumene with fuming nitric acid produces 2- and 4-nitrocumene which are converted into respective cumidines by the hydrogenation using Pd/Ni catalyst in H-cube with gravity separation. Hydrolysis of in situ generated diazonium salts in the boiling acidic conditions is carried out using integration of flow and microwave-assisted synthesis. 58% of 4-isopropyl phenol was obtained. The sequential flow synthesis can be applied to synthesize other organic compounds involving this specific sequence of reactions.</div>
<h1 class="articleTitle" style="color: #333333; font-family: Georgia, "Times New Roman", "Bitstream Charter", Times, serif;">
<span class="hlFld-Title">Telescoped Sequence of Exothermic and Endothermic Reactions in Multistep Flow Synthesis</span></h1>
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<span class="hlFld-ContribAuthor"><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Sharma%2C+Yachita" href="https://pubs.acs.org/author/Sharma%2C+Yachita" id="authors">Yachita Sharma</a></span></span><span class="NLM_x">, </span><span class="hlFld-ContribAuthor"><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Nikam%2C+Arun+V" href="https://pubs.acs.org/author/Nikam%2C+Arun+V" id="authors">Arun V. Nikam</a></span></span><span class="NLM_x">, and </span><span class="hlFld-ContribAuthor"><span class="hlFld-ContribAuthor"><a data-mce-href="https://pubs.acs.org/author/Kulkarni%2C+Amol+A" href="https://pubs.acs.org/author/Kulkarni%2C+Amol+A" id="authors">Amol A. Kulkarni</a></span><a class="ref" data-mce-href="https://pubs.acs.org/doi/10.1021/acs.oprd.8b00008#cor1" href="https://pubs.acs.org/doi/10.1021/acs.oprd.8b00008#cor1">*</a><span class="orcid-link-icon"> <a data-mce-href="http://orcid.org/0000-0001-6146-1255" href="http://orcid.org/0000-0001-6146-1255" target="_blank"><img alt="" data-mce-src="https://pubs.acs.org/templates/jsp/images/orcid.png" src="https://pubs.acs.org/templates/jsp/images/orcid.png" style="height: auto; max-width: 100%;" /></a></span></span></div>
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<span class="institution">Chemical Engineering & Process Development Division</span>, <span class="institution">CSIR-National Chemical Laboratory</span>, <span class="addr-line">Dr. Homi Bhabha Road</span>, Pune 411008, <span class="country">India</span></div>
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<cite>Org. Process Res. Dev.</cite>, Article ASAP</div>
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<strong>DOI: </strong>10.1021/acs.oprd.8b00008</div>
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<a data-mce-href="https://pubs.acs.org/author/Sharma%2C+Yachita" href="https://pubs.acs.org/author/Sharma%2C+Yachita" id="authors">Yachita Sharma</a></div>
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*Phone: <span class="phone">+91-20-25902153</span>, E-mail: <a data-mce-href="mailto:aa.kulkarni@ncl.res.in" href="mailto:aa.kulkarni@ncl.res.in">aa.kulkarni@ncl.res.in</a>.</div>
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<a data-mce-href="https://pubs.acs.org/author/Kulkarni%2C+Amol+A" href="https://pubs.acs.org/author/Kulkarni%2C+Amol+A" id="authors">Amol A. Kulkarni</a></div>
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<span class="proffName">Dr.Amol A. Kulkarni</span><br />Chemical Engineering & Process Development<br />CSIR-National Chemical Laboratory</div>
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Dr. Amol A. Kulkarni is a Scientist in the Chemical Engineering Division at the National Chemical Laboratory. He did his B. Chem. Eng. (1998), M. Chem. Eng (2000) and Ph.D. in chemical engineering (2003) all from the University Dept. of Chem. Technology (UDCT, Mumbai). In 2004 he worked at the Max Planck Institute-Magdeburg (Germany) as a Alexander von Humboldt Research Fellow. At NCL he is driving a research program on the design of microreactors and exploring their applications for continuous syntheses including of nanoparticles. He has been awarded with the Max-Planck-Visiting Fellowship from the Max-Planck-Society, Munich for 2008-2011. His research areas include: (i) design and applications of microreactors, (ii) design of multiphase reactors, (iii) experimental and computational fluid dynamics, and (iv) nonlinear dynamics of coupled systems. He is an active member of Initiative for Research and Innovation in Science (IRIS) supported by Intel’s Education Initiative to organize National Science Fair and popularize science in India.</div>
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Yachita Sharma</div>
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Yachita Sharma is a PhD student at CSIR-National Chemical Laboratory, Pune (India). She received her MSc in Applied Organic Chemistry in 2010. Her work focuses on exploring the continuous flow synthesis involving exothermic reactions and their integration.</div>
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Email: <strong><a data-mce-href="mailto:arun11nikam@gmail.com" href="mailto:arun11nikam@gmail.com">arun11nikam@gmail.com</a></strong><br />
Arun was born and raised in Koregaon, Maharashtra, India. He completed his bachelors and masters in chemical sciences from Shivaji Unversity, Kolhapur, India. Currently, He is pursuing his Ph. D. under the supervision of Dr. Amol A. Kulkarni and Dr. B. L. V. Prasad. His work mainly focuses on flow synthesis of nanoparticles, drug formulation, and polymers. He develops new synthesis procedures and translates into flow chemistry to increase productivity with excellent control over the quality of the product. He is also exploring the application of nanoparticles in catalysis, electronics and pharmaceutical fields. He specializes in microwave-assisted continuous flow synthesis of nanomaterial and organic intermediate. Apart from his research, he actively pursues Yoga and spirituality. He also likes to play volleyball and has competed in inter CSIR tournaments.</div>
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DRUG PATENTS INTERNATIONALhttp://www.blogger.com/profile/12652768774396889936noreply@blogger.com0tag:blogger.com,1999:blog-8960696629007291242.post-41434184261600968462019-01-30T07:02:00.001-08:002019-01-30T07:02:07.212-08:00Nickel-catalyzed regioselective C–H oxygenation: new routes for versatile C–O bond formation<div dir="ltr" style="text-align: left;" trbidi="on">
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<a href="http://pubs.rsc.org/en/Content/ArticleLanding/2019/QO/C8QO01274A" style="border: 0px; color: #227ad1; font-size: 20.88px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;">Nickel-catalyzed regioselective C–H oxygenation: new routes for versatile C–O bond formation</a></h4>
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<i style="border: 0px; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px;"><b style="border: 0px; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px;">Org. Chem. Front.</b></i>, 2019, Advance Article<br /><b style="border: 0px; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px;">DOI</b>: 10.1039/C8QO01274A, Research Article</div>
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Ze-lin Li, Kang-kang Sun, Chun Cai<br />Nickel-catalyzed regioselective C–H oxygenation reactions of chelating arenes using iodobenzene diacetate, alcohols, and benzoic acids respectively as attacking reagents have been developed for the first time.<br />To cite this article before page numbers are assigned, use the DOI form of citation above.</div>
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Nickel-catalyzed regioselective C–H oxygenation reactions of chelating arenes using iodobenzene diacetate, alcohols, and benzoic acids respectively as attacking reagents have been developed for the first time. Simplicity of operation, broad range of functional group tolerance, use of cheap transition metal nickel, and avoiding extraneous directing groups are the key features, thus providing an important complement to C–H oxygenation reactions and expanding the field of nickel-catalyzed C–H functionalizations. Explorations of mechanistic details are also described.</div>
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Nickel-catalyzed regioselective C–H oxygenation: new routes for versatile C–O bond formation</h2>
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<span class="article__author-link" style="border: 0px; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px;"><a href="https://pubs.rsc.org/en/results?searchtext=Author%3AZe-lin%20Li" style="border: 0px; color: #227ad1; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;">Ze-lin Li</a>,<span style="border: 0px; bottom: 1ex; font-size: 0.7em; height: 0px; line-height: 1; margin: 0px; outline: 0px; padding: 0px; position: relative; vertical-align: baseline;">a</span> </span><span class="article__author-link" style="border: 0px; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px;"><a href="https://pubs.rsc.org/en/results?searchtext=Author%3AKang-kang%20Sun" style="border: 0px; color: #227ad1; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;">Kang-kang Sun</a><span style="border: 0px; bottom: 1ex; font-size: 0.7em; height: 0px; line-height: 1; margin: 0px; outline: 0px; padding: 0px; position: relative; vertical-align: baseline;">a</span> and </span><span class="article__author-link" style="border: 0px; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px;"><a href="https://pubs.rsc.org/en/results?searchtext=Author%3AChun%20Cai" style="border: 0px; color: #227ad1; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;">Chun Cai</a>*<span style="border: 0px; bottom: 1ex; font-size: 0.7em; height: 0px; line-height: 1; margin: 0px; outline: 0px; padding: 0px; position: relative; vertical-align: baseline;">a</span> </span></div>
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*Corresponding authors</div>
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<span style="border: 0px; bottom: 1ex; font-size: 0.7em; height: 0px; line-height: 1; margin: 0px; outline: 0px; padding: 0px; position: relative; vertical-align: baseline;">a</span>College of Chemical Engineering, Nanjing University of Science & Technology, 200 Xiaolingwei, Nanjing, China<br /><b style="border: 0px; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px;">E-mail:</b><a href="mailto:c.cai@njust.edu.cn" style="border: 0px; color: #227ad1; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;" title="c.cai@njust.edu.cn">c.cai@njust.edu.cn</a></div>
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<a href="https://pubs.rsc.org/en/Content/ArticleLanding/2019/QO/C8QO01274A#!divAbstract" style="border: 0px; color: #227ad1; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;">https://pubs.rsc.org/en/Content/ArticleLanding/2019/QO/C8QO01274A#!divAbstract</a></div>
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2-(pyridin-2-yl)phenyl acetate (2a)</div>
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<a href="http://www.allfordrugs.com/wp-content/uploads/2019/01/str1-1.jpg" rel="attachment wp-att-11010" style="border: 0px; color: #227ad1; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;"><img alt="str1" class="alignnone size-full wp-image-11010" src="http://www.allfordrugs.com/wp-content/uploads/2019/01/str1-1.jpg" style="border: none; font-size: 13.92px; margin: 0px; max-width: 100%; outline: 0px; padding: 0px;" width="97" /></a></div>
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Formula: C13H11NO2 Mass: 213</div>
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To a mixture of 2-phenylpyridine (77.5 mg, 0.5 mmol) 1a, Ni(acac)2 (25.7 mg, 0.1 mmol, 20 mol %), ligand MePh2P (20.0 mg, 0.1 mmol, 20 mol %), and PhI(OAc)2 (483.2 mg, 0.75 mmol, 1.5 equiv) in a reaction tube was added solvent (CH3CN=2.0 mL). The reaction mixture was stirred at 115 °C for 24 h in air. Following the general procedure, 2a was purified by column chromatography on silica gel (petroleum ether: ethyl acetate = 5:1) as a white solid (80.9 mg, 76%).</div>
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1H NMR (500 MHz, Chloroform-d) δ 8.8 – 8.7 (m, 1H), 7.8 – 7.7 (m, 2H), 7.6 (dd, J = 7.9, 1.1 Hz, 1H), 7.5 (td, J = 7.7, 1.7 Hz, 1H), 7.4 (td, J = 7.5, 1.2 Hz, 1H), 7.3 – 7.3 (m, 1H), 7.2 (dd, J = 8.0, 1.2 Hz, 1H), 2.2 (s, 3H).</div>
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13C NMR (126 MHz, Chloroform-d) δ 168.4, 154.9, 148.6, 147.1, 135.3, 132.2, 129.8, 128.7, 125.4, 122.6, 122.3, 121.2, 20.0. GC-MS (EI) m/z: 213</div>
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<a href="http://www.allfordrugs.com/wp-content/uploads/2019/01/str2-1.jpg" rel="attachment wp-att-11011" style="border: 0px; color: #227ad1; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;"><img alt="str2" class="alignnone size-full wp-image-11011" sizes="(max-width: 756px) 100vw, 756px" src="http://www.allfordrugs.com/wp-content/uploads/2019/01/str2-1.jpg" srcset="http://www.allfordrugs.com/wp-content/uploads/2019/01/str2-1-300x138.jpg 300w, http://www.allfordrugs.com/wp-content/uploads/2019/01/str2-1.jpg 756w" style="border: none; font-size: 13.92px; margin: 0px; max-width: 100%; outline: 0px; padding: 0px;" width="756" /></a> <a href="http://www.allfordrugs.com/wp-content/uploads/2019/01/str3-2.jpg" rel="attachment wp-att-11012" style="border: 0px; color: #227ad1; font-size: 13.92px; margin: 0px; outline: 0px; padding: 0px; text-decoration-line: none;"><img alt="str3" class="alignnone size-full wp-image-11012" sizes="(max-width: 799px) 100vw, 799px" src="http://www.allfordrugs.com/wp-content/uploads/2019/01/str3-2.jpg" srcset="http://www.allfordrugs.com/wp-content/uploads/2019/01/str3-2-300x195.jpg 300w, http://www.allfordrugs.com/wp-content/uploads/2019/01/str3-2-768x500.jpg 768w, http://www.allfordrugs.com/wp-content/uploads/2019/01/str3-2.jpg 799w" style="border: none; font-size: 13.92px; margin: 0px; max-width: 100%; outline: 0px; padding: 0px;" width="799" /></a></div>
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