Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors

被引:29
作者
McKittrick, BA [1 ]
Ma, K [1 ]
Dugar, S [1 ]
Clader, JW [1 ]
Davis, H [1 ]
Czarniecki, M [1 ]
McPhail, AT [1 ]
机构
[1] DUKE UNIV,DEPT CHEM,DURHAM,NC 27708
关键词
D O I
10.1016/0960-894X(96)00347-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The C-3 sidechain of azetidinones related to SCH 48461 was modified by introducing a hydroxyl group at the 1' position. This led to the discovery of the cis azetidinone 2c, which had improved CAI activity. Compound 2c was prepared using a selective reduction and silane mediated debromination to control the relative stereochemistry of the three centers. Copyright (C) 1996 Elsevier Science Ltd
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页码:1947 / 1950
页数:4
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