A simple and efficient synthesis of the valsartan  

作　　者：Chen Xi Zhang Guo Jun Zheng Fu Qiang Bi Yu Lin Li 

机构地区：[1]State Key Laboratory of Applied Organic Chemistry and Institute of Organic Chemistry, Lanzhou University, Lanzhou 730000, China

出　　处：《Chinese Chemical Letters》2008年第7期759-761,共3页中国化学快报（英文版）

基　　金：the National Natural Science Foundation of China (No.20272012);the Special Research Grant for Doctoral Sites in Chinese Universities (No.20010730001).

摘　　要：Valsartan 1, one of the most important agents used in antihypertensive therapy today, was synthesized starting from L-valin methyl ester hydrochloride 2 through four steps in an overall yield of 60%. The key step involves the palladium-catalyzed Suzuki coupling. This method overcomes many of the drawbacks associated with the previously reported syntheses and is more suitable for industrial production.Valsartan 1, one of the most important agents used in antihypertensive therapy today, was synthesized starting from L-valin methyl ester hydrochloride 2 through four steps in an overall yield of 60%. The key step involves the palladium-catalyzed Suzuki coupling. This method overcomes many of the drawbacks associated with the previously reported syntheses and is more suitable for industrial production.

关 键 词：VALSARTAN ANTIHYPERTENSIVE L-Valin methyl ester hydrochlofide SYNTHESIS Suzuki coupling 

分 类 号：TQ46[化学工程—制药化工] R972.4[医药卫生—药品]