THE SYNTHESIS OF NOVEL MACROCYCLIC INHIBITORS OF HUMAN RENIN

被引：17

作者：

RIVERO, RA

GREENLEE, WJ

机构：

[1] Department of Exploratory Chemistry Merck Sharp, Dohme Research Laboratories, Rahway, NJ 07065

来源：

TETRAHEDRON LETTERS | 1991年 / 32卷 / 22期

关键词：

D O I：

10.1016/S0040-4039(00)74351-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

As part of an effort to develop human renin inhibitors with improved bioavailability, macrocyclic renin inhibitors 1 and 2 were prepared. These macrocycles were constructed from an analog of ''ACHPA'' ((3S, 4S)-4-amino-5-cyclohexyl-3-hydroxypentanoic acid)1 which incorporates a 2(S)-4-butenyl chain. A key step in the assembly of these macrocycles was the stereoselective synthesis of the 2(S)-substituted ACHPA derivative 3, utilizing the Evans chiral oxazolidone aldol protocol.2

引用

页码：2453 / 2456

页数：4

共 26 条

[1]

Antonaccio M J, 1987, Prog Drug Res, V31, P161

[2]

BAYLEY H, 1978, TETRAHEDRON LETT, V39, P3633

[3] CLINICAL GOAL IN SIGHT FOR SMALL MOLECULE RENIN INHIBITORS [J].