SYNTHESIS OF ALPHA-HYDROXY STATINE THROUGH A FACIALLY SELECTIVE OSMYLATION OF A CHIRAL ALPHA-AMIDO CROTONATE

被引：10

作者：

DEE, MF ^{[1
]}

ROSATI, RL ^{[1
]}

机构：

[1] PFIZER INC,DIV CENT RES,GROTON,CT 06340

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 09期

关键词：

D O I：

10.1016/0960-894X(95)00150-R

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

alpha-hydroxy statine 5 was synthesized by osmylation of amido crotonate 6 and incorporated into peptide framework 9, resulting in an active renin inhibitor; predicted stereochemical preferences for renin inhibition were confirmed by x-ray analysis and biochemical determinations. The facial selectivity of the osmylation is consistent with the Vedejs model.

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页码：949 / 952

页数：4

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