非马沙坦的合成

Synthesis of Fimasartan

以2-正丁基-5-乙氧基羰基甲基-4-羟基-6-甲基嘧啶为起始原料,经水解、酰化、N-烷基化、硫代酰胺化及脱保护基等反应合成了非马沙坦,结构经MS、~1HNMR表征。对关键步骤进行了工艺改进,总收率为45%。

Fimasartan was synthesized from 2-butyl-5-ethoxycarbonylmethyl-4-hydroxy-6-methylpyrimidine by a four-step reaction of hydrolysis,acylation,N-alkylation,thioamidation and deprotection. The structure was confirmed by MS and ~1HNMR. The critical process was optimized,the overall yield was about 45%.