N-[(1R,4R)-4-氨基-5-苯基-1-(苄基)戊基]氨基甲酸 5-噻唑基甲基酯置于盐酸,碳酸氢钠,Sodium Carbonate,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺体系中,用 四氢呋喃,1,4-二氧六环,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 29.0H,反应生成可比司他 参考文献: Methods And Intermediates For Preparing Pharmaceutical Agents[fr] Procédés Et Intermédiaires Pour La Préparation D'Agents Pharmaceutiques 标题: Methods And Intermediates For Preparing Pharmaceutical Agents[fr] Procédés Et Intermédiaires Pour La Préparation D'Agents Pharmaceutiques 摘要:用于制备式i化合物及其盐的方法和中间体.
专利信息
专利号:WO-2024028893-A1 优先权日:2022-08-01 标 题:Substituted benzimidazoles for treating viral diseases 发明人:CHAUDHARI VINOD DINKAR; THAKUR KRISHAN GOPAL; RINGE RAJESH PRAKASH; SINGH DESHKANWAR; KAUR SIMRAN; CHAWLA RAVNEET SINGH; JOSHI AKSHAY 权利人:COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF S 摘要:The invention relates to benzimidazole compounds, pharmaceutically acceptable salts thereof and its pharmaceutical compositions for reducing/treating viral infections. The present invention also relates to synthesis of such benzimidazole compounds. The present invention further relates to compositions which comprise such benzimidazole compounds or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination. The compounds of the invention are useful in reducing/treating viral infections particularly coronavirus infections caused by SARS-CoV, MERS-CoV and SARS-CoV-2.
专利号:US-5935946-A 优先权日:1997-07-25 标 题 :Nucleotide analog composition and synthesis method 发明人:MUNGER JR JOHN D; ROHLOFF JOHN C; SCHULTZE LISA M 权利人:GILEAD SCIENCES INC 摘要:The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p-toluenesulfonylmethoxyphosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.
专利号:US-2014051888-A1 优先权日:2012-08-20 标题 :Novel stereoisomeric mixtures, synthesis and uses thereof 发明人:DUBAY WILLIAM; BUTLER JEFFREY D; LIOTTA CHARLES L 权利人:AMPAC FINE CHEMICALS LLC 摘要:A novel stereochemical mixture of 1,6-diaryl-2,5-diaminohexanes, such as a mixture of stereoisomers of 1,6-diphenylhexane-2,5-diamine, is described. Also described are methods of preparing stereochemically pure 1,6-diaryl-2,5-diaminohexanes, and particularly stereochemically pure 1,6-diphenyl-2,5-diaminohexane. Also described is the use of both the mixture of stereoisomers and the individual stereoisomers.
专利号:CN-104193643-B 优先权日:2014-09-12 标 题:For the synthesis of the intermediate of anti-AIDS drug toughener cobicistat
专利号:CN-104193643-A 优先权日:2014-09-12 标 题 :A new intermediate for the synthesis of cobicistat, an anti-AIDS drug enhancer
专利号:CN-109912426-B 优先权日:2017-12-13 标题:Intermediate for the synthesis of anti-AIDS drug enhancer cobicistant
1: Cattaneo D, Cossu MV, Rizzardini G. Pharmacokinetic drug evaluation of ritonavir (versus cobicistat) as adjunctive therapy in the treatment of HIV. Expert Opin Drug Metab Toxicol. 2019 Nov;15(11):927-935. doi: 10.1080/17425255.2019.1685495. Epub 2019 Nov 3. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK540525/ No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK540287/ doi: 10.1080/14656566.2018.1559299. Epub 2018 Dec 26. Review. doi: 10.2147/DDDT.S147493. eCollection 2018. Review. 6: Deeks ED. Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2018 Jul;78(10):1013-1024. doi: 10.1007/s40265-018-0934-2. Review. doi: 10.1097/COH.0000000000000465. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK458451/ Available from http://www.ncbi.nlm.nih.gov/books/NBK458440/ doi: 10.1177/1060028017717018. Epub 2017 Jun 19. Review. 11: Angione SA, Cherian SM, Özdener AE. A Review of the Efficacy and Safety of Genvoya® (Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide) in the Management of HIV-1 Infection. J Pharm Pract. 2018 Apr;31(2):216-221. doi: 10.1177/0897190017710519. Epub 2017 May 30. Review. doi: 10.1080/14787210.2017.1323634. Epub 2017 May 9. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK409851/ doi: 10.1016/S0213-005X(17)30006-X. Review. Spanish. eCollection 2016. Review.
合成参考文献
摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from 参考文献:10.1358/dot.2012.48.12.1895682 摘要:Temesgen Z. Cobicistat-boosted elvitegravir-based fixed-dose combination antiretroviral therapy for HIV infection. Drugs Today (Barc). 2012 Dec;48(12):765–71. doi: 10.1358/dot.2012.48.12.1895682.