Efficient synthesis of valsartan, a nonpeptide angiotensin II receptor antagonist

被引：17

作者：

Zhang, C

Zheng, GJ

Fang, LJ

Li, YL ^{[1
]}

机构：

[1] Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China

[2] Lanzhou Univ, Inst Organ Chem, Lanzhou 730000, Peoples R China

[3] Zhejiang Hisun Pharmaceut Co Ltd, Taizhou 318000, Peoples R China

来源：

SYNLETT | 2006年 / 03期

关键词：

valsartan; antihypertensive therapy; directed orthometalation; palladium-catalyzed Suzuki coupling; methyl ester saponification;

D O I：

10.1055/s-2006-926234

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A highly efficient and convergent approach to the synthesis of the angiotensin II receptor antagonist valsartan (1), one of the most important agents used in anti h yperten sive therapy today, is described. Directed ortho-metalation of 4-bromotoluene provides the key boronic acid intermediate II which was subjected to palladium-catalyzed Suzuki coupling. This method overcomes many of the drawbacks associated with the previously reported syntheses. The saponification of the methyl ester in valsartan was realized in a convenient and economical manner, which is more suitable for industrial production.

引用

页码：475 / 477

页数：3

共 22 条

[1] SEQUENTIAL DIRECTED ORTHO METALATION BORONIC ACID CROSS-COUPLING REACTIONS - A GENERAL REGIOSPECIFIC ROUTE TO OXYGENATED DIBENZO[B,D]PYRAN-6-ONES RELATED TO ELLAGIC ACID [J].