非马沙坦的合成工艺改进

Improved Synthesis of Fimasartan

目的改进非马沙坦的合成工艺。方法以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,经过N-烷基化,脱保护,水解,酰胺缩合,硫羰基化5步反应合成了抗高血压药非马沙坦。结果目标产物结构经1H-NMR和ESI-MS确证。结论改进后的合成工艺操作简便,适合工业化生产。

Objective To improve the synthesis process of fimasartan. Methods Using 2-butyl-5-ethoxycarbonylmethyl-4- hydroxy-6-methylpyrimidine as starting material, fimasartan, an important antihypertensive drug, was synthesized by a5-step reaction including N-alkylation, deprotection, hydrolysis, condensation and thionylation. Results The structure of fimasartan was confirmed by 1H-NMR and ESI-MS. Conclusion The improved process has convenient operation and can be suitable for industrial production.