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CRYSTALLINE (S)-ISOPROPYL 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-DIOXO-3,4-DIHYDROPYRIMIDIN-1-(2H)-YL)-4-FLUORO-3-HYDROXY-4-METHYLTETRAHYDROFURAN-2-YL)METHOXY)(PHENOXY)PHOSPHORYL)AMINO)PROPANOATE
专利权人:
GILEAD PHARMASSET LLC
发明人:
ROSS, Bruce S.,SOFIA, Michael Joseph,PAMULAPATI, Ganapati Reddy,RACHAKONDA, Suguna,ZHANG, Hai-Ren,CHUN, Byoung-Kwon,WANG, Peiyuan,CHUN
申请号:
RSP20150788
公开号:
RS54368B1
申请日:
2011.03.31
申请国别(地区):
RS
年份:
2016
代理人:
摘要:
Refers to a process for preparing a composition comprising a Phosphorus containing Active or diastereomericamente enantiomerically enriched Salt or Salt thereof of formula (i), which comprises: a) reacting a protected or not protected with a basic Reagent such as pyridine, co Lina, among others, to form a Salt of the assetThen REACT with a compound or Salt diastereomericamente enantiomerically enriched formula (ii) where W is aryl or - (CH2) NSC (o) C (CH3) 3 (m CH2OH) - m; n is 2 or 3; M is 0, 1, 2 or 3; LG is a leaving Group such like Halogen, tosylate, among others, is a radical Group that includes a Amina as benzylamine.Among others; b) optionally Unprotect The Compound obtained in Step a); and c) optionally subjecting The Compound obtained in Step a) or the compound obtained in STEP (b) chromatography, Extraction and Crystallization to obtain the desired Compound.Said composition is useful for the prophylaxis and / or treatment of a viral Agent such as herpes Type 2, hepatitis C virus, rhinovirus, EbolaKristalni (S)-izopropil 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-diokso-3,4-dihidropirimidin-1(2H)-il)-4-fluoro-3-hidroksi-4-metiltetrahidrofuran-2-il)metoksi)(fenoksi)fosforil)amino)propanoat predstavljen formulom Sp-4:koji ima XRPD 20-refleksije (°) od oko: 6.1, 8.2, 10.4, 12.7, 17.2, 17.7, 18.0, 18.8, 19.4, 19.8, 20.1, 20.8, 21.8 i 23.3.Prijava sadrži još 18 patentnih zahteva.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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