DR ANTHONY MELVIN CRASTO,WorldDrugTracker, helping millions, A 90 % paralysed man in action for you, I am suffering from transverse mylitis and bound to a wheel chair, With death on the horizon, nothing will not stop me except God................DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 25Yrs Exp. in the feld of Organic Chemistry,Working for GLENMARK GENERICS at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution

Sunday 7 March 2021

Buspirone

 

Buspirone 200.svg

Buspirone


Buspirone

  • Molecular FormulaC21H31N5O2
  • Average mass385.503 Da
  • буспирон
    بوسبيرون
    丁螺酮
251-489-4 [EINECS]
253-072-2 [EINECS]
36505-84-7 [RN]
8-[4-(4-Pyrimidin-2-yl-piperazin-1-yl)-butyl]-8-aza-spiro[4.5]decane-7,9-dione
8-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione
  • 8-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione
  • Buspin
  • Buspirone
  • Spitomin
Buspirone

PAPER

https://pubs.rsc.org/en/content/articlelanding/2019/GC/C8GC03328E#!divAbstract

  1. Green Chemistry, 21(1), 59-63; 2019

Abstract

A continuous flow method for the direct conversion of alcohols to amines via a hydrogen borrowing approach is reported. The method utilises a low loading (0.5%) of a commercial catalyst system ([Ru(p-cymene)Cl2]2 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 (5) and Buspirone (25) were accomplished in good yields employing these new methods.

Graphical abstract: Fast continuous alcohol amination employing a hydrogen borrowing protocol
http://www.rsc.org/suppdata/c8/gc/c8gc03328e/c8gc03328e2.pdf
 
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.
 
 
 
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.


CAS Registry Number: 36505-84-7
CAS Name: 8-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione
Molecular Formula: C21H31N5O2
Molecular Weight: 385.50
Percent Composition: C 65.43%, H 8.11%, N 18.17%, O 8.30%
Literature References: Non-benzodiazepine anxiolytic; 5-hydroxytryptamine (5-HT1) receptor agonist. Prepn: Y. H. Wu et al., J. Med. Chem. 15, 477 (1972); Y. H. Wu, J. W. Rayburn, DE 2057845 (1971 to Bristol-Myers); eidem, US 3717634 (1973 to Mead-Johnson). Pharmacology: L. E. Allen et al., Arzneim.-Forsch. 24, 917 (1974). Comparison with diazepam in treatment of anxiety: H. L. Goldberg, R. J. Finnerty, Am. J. Psychiatry 136, 1184 (1979); A. F. Jacobson et al., Pharmacotherapy 5, 290 (1985). Nonsynergistic effect with alcohol: T. Seppala et al., Clin. Pharmacol. Ther. 32, 201 (1982). Disposition and metabolism: S. Caccia et al., Xenobiotica 13, 147 (1983). Series of articles on chemistry, pharmacology, addictive potential, and clinical trials: J. Clin. Psychiatry 43, pp 1-116 (1982); on pharmacology, safety and clinical comparison with clorazepate: Am. J. Med. 80, Suppl. 3B, 1-51 (1986). Review of pharmacology and therapeutic efficacy: K. L. Goa, A. Ward, Drugs 32, 114-129 (1986). Review: M. W. Jann, Pharmacotherapy 8, 100-116 (1988); D. P. Taylor, FASEB J. 2, 2445-2452 (1988).
 
Derivative Type: Hydrochloride
CAS Registry Number: 33386-08-2
Trademarks: Ansial (Vita); Ansiced (Abello); Axoren (Glaxo Wellcome); Bespar (BMS); Buspar (BMS); Buspimen (Menarini); Buspinol (Zdravlje); Buspisal (Lesvi); Narol (Almirall)
Molecular Formula: C21H31N5O2.HCl
Molecular Weight: 421.96
Percent Composition: C 59.77%, H 7.64%, N 16.60%, O 7.58%, Cl 8.40%
Properties: Crystals from abs ethanol, mp 201.5-202.5°. LD50 i.p. in rats: 136 mg/kg (Allen).
Melting point: mp 201.5-202.5°
Toxicity data: LD50 i.p. in rats: 136 mg/kg (Allen)
 
Therap-Cat: Anxiolytic.
Keywords: Anxiolytic; Arylpiperazines; Serotonin Receptor Agonist.

24 comments:

  1. Kashmir Tour
    Beautiful ponds, stunning views, and a once-in-a-lifetime chance to stay in a boathouse. The Kashmir Trip takes you to Gulmarg, where you can participate in fun winter sports The captivating Kashmir journey takes you through the lovely Aru and Betaab Valleys, as well as the gushing Sindh River, to the Zoji La Pass, the highest pass on the Kashmir-Ladakh Road. The entire state of Kashmir is being explored.

    ReplyDelete
  2. Hi there,

    Thank you so much for the post you do and also I like your post, Are you looking for buy Buspirone online without prescription in UAE? We are buy Buspirone online without prescription, health bio-pharma online pharmacy, online pharmacy In Saudi Arabia, Buy Pills Online, High Rated Pills for Sale, Online Pharmacy Near you, Abortion Pills in Offer, Abortion pills Cytotec available in Dubai, Abortion Pills Cytotec available in Dubai, discount e pharmacy online in Riyadh, online e-pharmacy market In Bahrain, online pharmacy help Saudi Arabia, online pharmacy hub In Saudi Arabia, online pharmacy near me, online pharmacy stock, how to get online doctors prescriptions, anxiety pills prescribed, Is miferpristone and misoprostel available in UAE, Cytotec medicine in UAE,How to get abortion pills in UAE, Where to buy cytotec in Dubai, , Dubai online shopping tablets, Mifegest kit price online order, Vimax pills in Dubai, Cytotec 200 Mcg in Riffa, Cytotec 200 Mcg in , Misoprostol in Dubai pharmacy what are good anxiety pills, anxiety pills buy online in Saudi Arabia, anxiety pills best in Kuwait, for you with the well price and our services are very fast.
    Click here for href="https://onlineplanpharmacist.com/product/buy-buspirone-online-with-prescription/" />title" Buy Buspirone Online without prescription |Buy Pills Online| High rated pills for sale| Online Pharmacy Near You" />MORE DETAILS......

    Contact Us: +1 (443) 718-9645
    Email Us At: support@healthsbiopharma.com

    ReplyDelete
  3. looking to buy 4-emc online from a leading supplier? onlineresearchchemlab.com is the best research chemicals store where you can buy
    more info

    ReplyDelete
  4. looking to Buy Crystal Meth Online from a leading supplier? onlineresearchchemlab.com is the best research chemicals store where you can buy
    For More Info

    Email: info@onlineresearchchemlab.com / onlineresearchchemlab@gmail.com
    Wickr: locallegit
    whatsapp: +1662-403-4557
    Skype: williamjune1

    ReplyDelete
  5. looking to BUY 4-CMC CRYSTAL ONLINE from a leading supplier? onlineresearchchemlab.com is the best research chemicals store where you can buy
    For More Info

    Email: info@onlineresearchchemlab.com / onlineresearchchemlab@gmail.com
    Wickr: locallegit
    whatsapp: +1662-403-4557
    Skype: williamjune1

    ReplyDelete
  6. amazing post. Thank you for sharing this post. Our platform is also used by the Derma Products Pcd Companies & Third Party Derma PCD Manufacturing companies to invites Derma PCD company products supplier to get Derma Pcd Pharma Companies opportunity in pan India level locations.
    Derma company in India

    ReplyDelete
  7. Hi there,
    Thank you so much for the post you do and also I like your post, Ayahuasca, also known as the tea, the vine, and la purga is a brew made from the leaves of the Psychotria Viridis shrub along with the stalks of the Banisteriopsis caapi vine

    Contact Us
    Phone: +1 (571) 310-3529
    Email: info@psychedelicplugonline.com

    Click here for MORE DETAILS....

    ReplyDelete
  8. Hi There,
    Thank you for sharing the knowledgeable blog with us I hope that you will post many more blog with us:-
    N,N-Diethyl-2-[[4-(1-methylethoxy)phenyl]methyl]-5-nitro-1H-benzimidazole-1-ethanamine (isotonitazene) is a synthetic opioid analgesic.
    Email:info@onlineresearchchemlab.com
    Click here for more information:- more info

    ReplyDelete
  9. BUY NOW - Redditpharmacy
    Get Upto 10% Discount on All Medicines Use Coupon Code "SAVE10" at Redditpharmacy

    ReplyDelete
  10. Text/Call: +966572737505

    Cytotec in Jeddah, Cytotec in Riyadh, Cytotec in Dammam Abortion pills in Riyadh, Abortion pills in Jeddah, Abortion pills in Riyadh, Abortion pills in Dammam, Where to buy cytotec in Jeddah, Where to buy cytotec in Riyadh,
    Where to buy cytotec in Dammam
    , Where to buy cytotec in Saudi Arabia, How to buy abortion pills in Saudi Arabia. Good Stuff Available I’m allowed over 50 pounds in my possession. I am looking to supply a min of 1 oz of the following abortion pills to anyone who wants grade. We do discreet ######## and no signatures during delivery. The parcel has no label indicating it is carrying the what. We do give high discounts for orders above 2 to 3 pound.


    For all interested, do email us back with your order. Below is some of our available strains Good for Pain, cancer, insomnia..

    #Abortion pills in Riyadh::::::::::::: Grade: AA

    #Abortion pills in Dammam:::::::::::::::Grade: AA+

    #Where to buy cytotec in Saudi Arabia::::Grade: A

    #
    Where to buy cytotec in Dammam :::::::Grade: AA


    And many more..


    Deliveries 24/7 everywhere!!!! very clean smelling, awesome taste and VERY potent hash oil. purged for hours so no impurities left. used stainless steel tubes.


    Phone: +966572737505

    Website: https://abortionpillshomeuae.com/

    ReplyDelete
  11. onlinepharmas.com is an online pharmacy that sells generic medications in the United States at reasonable pricing. You can purchase generic prescription medications from an internet pharmacy.


    Click Here For Order: Buy Alko 1 MG Tablet Online USA

    Click Here For Order: Buy Tapentadol 100 MG Tablet Online USA

    Click Here For Order: Buy Lypin 10 Mg Tablet Online USA

    Click Here For Order: Buy Cialis 20 MG online USA

    Click Here For Order: Buy Citra Tablets online USA

    ReplyDelete
  12. Awesome write up, thank you for your share.

    https://genuinevenompharmacy.com/product/bufo-alvarius-toad-venom-for-sale/

    BUFO ALVARIUS TOAD VENOM FOR SALE| BUY SCORPION VENOM ONLINE| BUY SNAKE VENOM ONLINE

    Toad venom, snake venom, scorpion venom,

    BUY BUFO BUFO TOAD VENOM ONLINE. Toad venom smokers ‘milk’ live Bufo Alvarius toads of their venom by stroking the areas around their paratoid glands which causes the toad to excrete its venom. This venom is caught on a piece of glass or mirror and left to dry into a crystal-type form which can be smoked.
    Whatsapp: +1 626 598 8048
    Wickr Me: jeomallory

    ReplyDelete
  13. Xanax is a brand name drug that contains Alprazolam 1 MG as an active salt. Xanax 1 MG is used to treat anxiety disorders, insomnia, Nervousness and to relieve anxiety that's associated with depression. Xanax 1 MG is a member of drugs group commonly known as benzodiazepines (ben-zoe-dye-AZE-eh-peens). Xanax 1 MG impacts chemicals in the brain that may become unbalanced or disturbed and cause anxiety.

    ReplyDelete
  14. Hi there,

    Thank you so much for the post you do and also I like your post, Are you looking for a High-Quality SSD Chemical Solution online in the whole USA? We are providing High-Quality Gamma butyrolactone online, Buy Ketamine Online, Buy SSD chemical solution Online, Buy iboga Online, Buy FUB-AMB Online, 5-mapb crystals for sale, Buy good Crystal Meth Online, BUY 2C-D Online, BUY 5-METHYL-MDA online,Buy Actavis Promethazine Online with the good price and our services are very fast.

    Click here for Contact +1 (626) 598-8048, Email: sales@legitchemsales.com

    ReplyDelete
  15. Hi there,

    Thank you so much for the post you do and also I like your post, are you looking for a High-Quality Buy Ketamine online in the whole USA? We are providing High-Quality Buy Ketamine, Gamma butyrolactone online, Buy Ketamine Online, Buy SSD chemical solution Online, Buy iboga Online, Buy FUB-AMB Online, 5-mapb crystals for sale, Buy good Crystal Meth Online, BUY 2C-D Online, BUY 5-METHYL-MDA online,Buy Actavis Promethazine Online with the good price and our services are very fast.

    Click here for Contact +1 (626) 598-8048, Email: sales@legitchemsales.com

    ReplyDelete
  16. Cari yang gacor beneran setiap bermain menang terus ?
    Disini tempatnya juragan kalo mau main mah winbook88 dijamin setiap main win terus dah kalo gak percaya mah gapapa gak bakal maksa aku mah da aslina.

    ReplyDelete
  17. This helped clear up a lot of confusion for me. Thank for sharing!

    Zopiclone Tablets Blue

    ReplyDelete
  18. "I appreciate you taking the time to put this together. Very informative!"
    Buy lorazepam 3mg tablets UK

    ReplyDelete
  19. Thanks for sharing this valuable information. This helped me a lot.

    Actavis Zopiclone 7.5mg

    ReplyDelete
  20. Buy 30 grams Peaceful Nembutal Pentobarbital Sodium Powder Online
    WhatsApp# +1707-851-0613

    Signal / WhatsApp# +44 7931 491607

    Cyber Dust: medsfan

    Wire App: @medsfan

    Email ID (oxydrhere@gmail.com)

    Dosage Form:POWDER

    Dosage Strength: 50 MG/G

    Regulatory Information: Schedule G (CDSA IV)

    Packaging Presentation:50g

    Nembutal Pentobarbital Sodium Powder and Nembutal sodium pentobarbital

    powder is a proven, reliable powder product that brings about a peaceful death.

    Almost no failures are known, despite large statistics (for example, the Toronto

    euthanasia organisation Dignitas reported 920 exits with no single

    failure).Administration is a matter of dissolving up to 15~100 grams of the

    Nembutal Pentobarbital Sodium Powder in 5~50 ml of water and drinking… . .

    Quality 50 grams Pentobarbital sodium (Nembutal) Powder For Sale, If the

    powder is analyzed to be pure, and if ingested in the recommended amounts, so it

    is always better to take dosage than the one required for lethal dose. If the

    substance is pure, a purchase of 95% of pure sodium pentobarbital is enough for

    one adult or animal to Dilute drink and have a Peaceful Exit Nowadays.
    WhatsApp# +1707-851-0613

    Signal / WhatsApp# +44 7931 491607

    Cyber Dust: medsfan

    Wire App: @medsfan

    Email ID (oxydrhere@gmail.com)
    Where & How To Buy Nembutal Pentobarbital Sodium Safely Nowadays

    Nembutal Pentobarbital Sodium is supposedly very difficult to obtain Nowadays,

    as its remaining human use in most of the world is in Powder, liquid and Pills form

    for use as a sedative and anesthetic in hospitals, Veterinary Clinics and Homes. In

    Germany, Belgium, France, Poland, Denmark, Spain, it is even more scarce in the

    USA, UK and CANADA. Because of this, no pharmacy sells Nembutal

    Pentobarbital except of BUY NEMBUTAL PENTOBARBITAL SODIUM

    SAFELY ONLINE AT; any such site that claims to do so Apart from is likely fake

    Nowadays.

    There are very limited ways Nowadays to get Nembutal Pentobarbital Sodium.

    Some people, who have the option, can simply walk into their local Hospitals or

    veterinarian’s Clinics and ask to buy some. (Note: Doing this in the USA, UK &

    CANADA will most likely get you arrested Nowadays. For those who want to

    Buy 30 grams Peaceful Nembutal Pentobarbital Sodium Powder Online, you’ll see

    many places advertising to sell it. If this is the route you choose to take, you must

    be very cautious by Ordering and Buying your Nembutal Pentobarbital Sodium

    Powder, Oral Liquid and Pills by Ordering from POWERALL PHARMACY. The

    overwhelming majority of other Pharmacies are scammers. For an accurate way to

    source a legitimate supplier, you’ll need the Peaceful Pill Handbook (PPH). Inside

    the PPH they have listed the one and only single Pharmacy Supplier of Nembutal

    Pentobarbital Sodium. Yes, that’s right. There’s literally only one person in the

    world who sells legitimate Nembutal Pentobarbital Sodium online and that’s
    WhatsApp# +1707-851-0613

    Signal / WhatsApp# +44 7931 491607

    Cyber Dust: medsfan

    Wire App: @medsfan

    Email ID (oxydrhere@gmail.com)

    Buy Genuine Ambien 12.5mg Online

    ReplyDelete