EFFICIENT SYNTHESIS OF LOSARTAN, A NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONIST

被引：164

作者：

LARSEN, RD ^{[1
]}

KING, AO ^{[1
]}

CHEN, CY ^{[1
]}

CORLEY, EG ^{[1
]}

FOSTER, BS ^{[1
]}

ROBERTS, FE ^{[1
]}

YANG, CH ^{[1
]}

LIEBERMAN, DR ^{[1
]}

REAMER, RA ^{[1
]}

TSCHAEN, DM ^{[1
]}

VERHOEVEN, TR ^{[1
]}

REIDER, PJ ^{[1
]}

机构：

[1] DUPONT MERCK PHARMACEUT CO,CHAMBERS WORKS,DEEP WATER,NJ 08023

来源：

JOURNAL OF ORGANIC CHEMISTRY | 1994年 / 59卷 / 21期

关键词：

D O I：

10.1021/jo00100a048

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A highly efficient, convergent approach to the synthesis of the angiotensin II receptor antagonist losartan (1) is described. Directed ortho-metalation of 2-trityl-5-phenyltetraz ole provides the key boronic acid intermediate 10 for palladium-catalyzed biaryl coupling with bromide 5 obtained from the regioselective alkylation of the chloroimidazole 2. This methodology overcomes many of the drawbacks associated with previously reported syntheses.

引用

页码：6391 / 6394

页数：4

共 19 条

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