发明名称 A NOVEL ASYMMETRIC SYNTHESIS OF R AND S WARFARIN AND ITS ANALOGS
摘要 The present invention provides a novel process for making compounds of formu la (2a or 2b) or pharmaceutically acceptable salts thereof, wherein R1 is selected from the group consisting of phenyl and phen yl substituted with at least one group selected from NO2 and halogen, R2 is H; R3 is selected from the group consisting of C1-4 alkyl, phenyl, and benzyl; and, R4 is selected from the group consisting of H and halogen; which comprises the steps of: a) oxidizing a racemate of formula (2) or a salt thereof to form a dehydro-compound of formula (3), wherein R5 is selected from the group consisting of H, CH3, benzyl, C2-8 acyl, Na, Li and K; and, b) asymmetrically hydrogenating a compound of formula (3) in the presence of a chiral phosphin e catalyst to form a compound of formula (2a or 2b).
申请公布号 CA2226752(C) 申请公布日期 2002.02.19
申请号 CA19962226752 申请日期 1996.07.10
申请人 THE DUPONT MERCK PHARMACEUTICAL COMPANY 发明人 LI, HUI-YIN;ROBINSON, ANDREA JANE
分类号 B01J31/24;C07D311/56;(IPC1-7):C07D311/56 主分类号 B01J31/24
代理机构 代理人
主权项
地址
您可能感兴趣的专利