Benzyl glycidyl ether

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Benzyl glycidyl ether



Chiral HPLC
Column: Chiralcel OD-H (0.46 x 25 cm)
Detection: UV (254 nm) (In a few cases 214 nm was used.)
Benzyl Glycidyl Ether Analysis
Eluent: 10% iPrOH:90% Hexanes
Flow rate: 1.0 mL/min
Retention times of the two enantiomers: 8.2 and 9.0 minutes
Typical percentages of the two enantiomers using catalyst synthesized using L-Tartaric acid: 98.7% (8.2 min RT), 1.3% (9.0 min RT)
Typical percentages of the two enantiomers using catalyst synthesized using D-Tartaric acid: 3.5% (8.2 min RT), 96.5% (9.0 min RT)
3-Benzyloxy-1,2-propanediol Analysis
Eluent: 15% iPrOH:85% Hexanes
Flow rate: 0.9 mL/min
Retention times of the two enantiomers: 11.1 and 13.1 minutes
Typical percentages of the two enantiomers using catalyst synthesized using L-Tartaric acid: 84.0% (11.1 min RT), 16.0% (13.1 min RT)
Typical percentages of the two enantiomers using catalyst synthesized using D-Tartaric acid: 2.7% (11.1 min RT), 97.3% (13.1 min RT)
Optical Rotation
Jacobsen reports that the R enantiomer of benzyl glycidyl ether is the major one remaining using the (R,R) catalyst. (This is the catalyst produced using the L-Tartaric acid.) For a sample with >99% ee he reports: []²⁶_D +10° (c 5.2, MeOH).
Jacobsen reports that the R enantiomer of the diol is the major one produced using the (R,R) catalyst. (This is the catalyst produced using the L-Tartaric acid.) For a sample with 95% ee he reports: []²³_D -1.4° (c 3.31, EtOH).





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II snapped these mini-Viking vessels tied up on the bay across from the Thor Hyerdahl Museum in Oslo, Norway. I loved their vibrant colors on one of the few ...






 


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ANAGLIPTIN

N-[2-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide
CAS No.:	739366-20-2
Synonyms:	Anagliptin;
Formula:	C19H25N7O2
Exact Mass:	383.20700

Anagliptin chemically known as N-[2-[2-[2(S)-cyanopyrrolidin-l-yl]-2-oxoethylamino]- 2-methylpropyl]-2-methylpyrazolo[l,5-a]pyrimidine-6-carboxamide is represented by the structural formula:

Anagliptin is a dipeptidyl peptidase IV- inhibitor. United States Patent No 7345 1 80- (IJS' 180) discloses anagliptin.     Example 5: Synthesis of N-[2-2[2(S)-Cyano pyrrolidin-l-yl]-2-oxoethyIamino]-2- methyIpropyl]-2-methyaIpyrazoIo [1, 5-a] pyrimidine-6-carboxamide (I, anagliptin). 1H NMR (300 MHz, CDC1₃): δ 1.16 (s, 6H), 2.23(m, 4H), 2.54(s, 3H), 3.25-3.51 (m, 6H), 4.78 (m, 1H), 6.53 (s, 1H), 8.05 (s, 1H), 8.93 (s, 1H), 9.22(s, 1H) HPLC Purity: 99.71%, Chiral purity: 100%

.........WO2014147640A2




 Kato, M.; Oka, M.; Murase, T.; Yoshida, M.; Sakairi, M.; Yamashita, S.; Yasuda, Y.; Yoshikawa, A.; Hayashi, Y.; Makino, M.; Takeda, M.; Mirensha, Y.; Kakigami, T. Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]- 2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor. Bioorg. Med. Chem. 2011, 19, 7221–7227. http://www.sciencedirect.com/science/article/pii/S0968089611007784


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Norway: Oslo to Bergen by train










ALESUND




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Norway Bergen Tramway







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Arterolane maleate

Arterolane

cas 664338-39-0, UNII-3N1TN351VB, OZ277, RBX-11160, NCGC00274173-01

Molecular Formula: C₂₂H₃₆N₂O₄

 Molecular Weight: 392.53224

Medicines For Malaria Venture Mmv

Ranbaxy Lab Ltd innovator

 cis-adamantane-2-spiro-3’-8’-[[[(2’-amino-2’ methylpropyl) amino] carbonyl] methyl] 1’,2’,4’-trioxaspiro [4.5] decane

cis-adamantane-2-spiro-3′-8′-[[[(2′- amino-2′-methylpropyl)amino]carbonyl]-methyl]- 1 ‘,2′,4′-trioxaspiro[4.5]decane

Arterolane maleate is a synthetic trioxolane compound. The chemical name of arterolane maleate is cis-adamantane-2-spiro-3’-8’-[[[(2’-amino-2’ methylpropyl) amino] carbonyl] methyl] 1’,2’,4’-trioxaspiro [4.5] decane hydrogen maleate. The molecular formula is C26H40N2O8 and molecular weight is 508.61. The structural formula is as follows:

PATENT

http://www.google.st/patents/WO2007138435A2?cl=en

Example 6: Preparation of c/s-adamantane-2-spiro-3′ -8 ‘-πT(2′-amino-2′ -methyl propyl) amino! carbonyl] methyli-l ‘, 2\ 4′-U-JoXaSpJrQ [4.51 decane maleate To a solution of c/s-adamantane-2-spiro-3′-8′-[[[(2′-amino-2′-methyl propyl) amino] carbonyl] methyl]-! ‘, 2′, 4′-trioxaspiro [4.5] decane (example 5) (60 g, 0.153 moles) in ethanol (150 mL) was added a solution of maleic acid (17.3 g, 0.15 moles, 0.98 equiv. in ethanol 90 mL) and the reaction mixture was stirred for about 1 h. To this clear solution, n- heptane (720 mL) was added at room temperature in 1 h and the reaction mixture was stirred for 3 h. It was then cooled to 0 to 10⁰C and filtered. The cake was washed with n-heptane (60 mL) and dried under vacuum at 40-45⁰C.

Yield: 67 g, 77.4%,

 mp: 149⁰C (decomp), 

(M⁺+l) 393.5,  

¹HNMR (300 MHz, DMSO-^ ): δ 1.05-1.11 (2H,m), 1.18 (6H,s), 1.64-1.89 (21H,m), 2.07(2H,d), 3.21 (2H,d), 6.06 (2H,d), 7.797 (2H, bs), 8.07 (IH, t).

SEE FULL ARTICLE WITH SYNTHESIS AT

 http://newdrugapprovals.org/2014/12/18/ranbaxy-to-introduce-malarial-treatment-synriam-in-african-nations/




NMR PREDICTIONS

H-NMR spectral analysis

CAS NO. 664338-39-0, Arterolane H-NMR spectral analysis

C-NMR spectral analysis

CAS NO. 664338-39-0, Arterolane C-NMR spectral analysis

 
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http://newdrugapprovals.org/

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO

 
 amcrasto@gmail.com

http://newdrugapprovals.org/

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO

NORWAY\

























Norway: Oslo to Bergen by train










ALESUND




Stave church Heddal, Norway






Norway Bergen Tramway







At the top of Preikestolen with view over the Lysefjord, Norway 





Norway - Bergen Cityscape by AgiVega