A concise synthesis of silanediol-based transition-state isostere inhibitors of proteases

被引：19
|
作者：
Organ, MG
Buon, C
Decicco, CP
Combs, AP
机构：
[1] York Univ, Dept Chem, N York, ON M3J 1P3, Canada
[2] Bristol Myers Squibb Co, Discovery Chem, Expt Stn, Wilmington, DE 19880 USA
来源：
ORGANIC LETTERS | 2002年 / 4卷 / 16期
关键词：
D O I：
10.1021/ol026195s
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
[GRAPHICS] An efficient synthesis of silanediol-based transition-state inhibitors of proteases is described. A new convergent synthesis has been optimized by using a two-step sequence of hydrosilylation followed by the addition of a silyllithio species to an imine. The method should be applicable to the synthesis of a wide variety of silanediol isosteres to probe the utility of this unique transition-state isostere.
引用
收藏
页码：2683 / 2685
页数：3
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