ENANTIOSELECTIVE SYNTHESIS OF THE (SYN,ANTI)-1-AMINO-2,3-DIOL SUBUNIT OF RENIN INHIBITORS BY REACTION OF BETA-LACTAMS WITH A GRIGNARD-REAGENT

被引:21
作者
SPERO, DM
KAPADIA, S
FARINA, V
机构
[1] Department of Process Research, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, CT 06877
关键词
D O I
10.1016/0040-4039(95)00824-V
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new approach to the BOC-protected amino diol la via the opening of 3,4-cis-disubstitute beta-lactam 3 with isobutylmagnesium chloride is described. Nonracemic beta-lactam 3 could be obtained by enzymatic resolution of the 3-acetoxy-beta-lactam 4 or from a chiral precursor, methyl (R)-(-)-mandelate.
引用
收藏
页码:4543 / 4546
页数:4
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