PRACTICAL SYNTHESES OF A NOVEL TRICYCLIC DIPEPTIDE MIMETIC BASED ON A [6H]-AZEPINO INDOLINE NUCLEUS - APPLICATION TO ANGIOTENSIN-CONVERTING ENZYME-INHIBITION

被引:35
作者
DELOMBAERT, S
BLANCHARD, L
STAMFORD, LB
SPERBECK, DM
GRIM, MD
JENSON, TM
RODRIGUEZ, HR
机构
[1] Research Department, Pharmaceuticals Division, CIBA-GEIGY Corporation, Summit, NJ 07901
关键词
D O I
10.1016/S0040-4039(00)78331-6
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Two stereocontrolled synthetic approaches towards 5-(S)-amino-1,2,4,5,6,7-hexahydro-azepino [3,2,1-hi] indole-4-one-2-(S)-carboxylic acid 1, based on intramolecular Friedel-Crafts acylations, are reported. This conformationally restricted tricyclic dipeptidomimetic has been applied a the design of a potent and orally active inhibitor of angiotensin-converting enzyme (ACE).
引用
收藏
页码:7513 / 7516
页数:4
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