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

来源：

TETRAHEDRON LETTERS | 1994年 / 35卷 / 41期

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).

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页码：7513 / 7516

页数：4

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