WANG PEIYUAN,SOFIA MICHAEL JOSEPH,PAMULAPATI GANAPATI REDDY,ZHANG HAI-REN,CHUN BYOUNG-KWON,ROSS BRUCE S.,RACHAKONDA SUGUNA
申请号：
NZ70992610
公开号：
NZ709926A
申请日:
2010.05.20
申请国别(地区):
NZ
年份:
2016
代理人:
摘要：
Disclosed is a process for the synthesis of enantiomerically pure sofosbuvir (Sp-4) or its corresponding opposite phosphoramidate enantiomer (Rp-4), said process comprising reacting an enantiomerically purified isopropyl-alanylphosphoramidate of formula (C) (or C&rsquo； in the case of the preparation of Rp-4), with 2&rsquo；-deoxy-2&rsquo；-fluoro-2&rsquo；-C-methyluridine of formula (3) and a base, where LG&rsquo； is a suitable leaving group such as an aryloxide substituted with at least one electron withdrawing group (e.g. p-nitrophenoxide, p-chlorophenoxide, o-chlorophenoxide, 2,4-dinitrophenoxide, pentafluorophenoxide etc.), wherein Z is hydrogen or a protecting group, and optionally subsequently deprotecting the product as necessary.
