伊贝沙坦的合成工艺改进

An Improvement on the Synthetic Technology of Irbesartan

参照文献报道 ,试验了以 2 丁基 1 ,3 二氮杂螺环〔4 4〕壬 1 烯 4 酮 (2 )为原料经两条不同路线合成伊贝沙坦的工业生产方法。路线一以化合物 2与 4 溴甲基 2′ 氰基联苯 (3)经取代、四氮唑化两步反应合成伊贝沙坦 ,总收率 63% ,路线二以化合物 2与四氮唑环上带保护基的化合物 5经取代、脱保护得伊贝沙坦 ,总收率 85%。所得目标化合物及其中间体的结构经1H NMR、MS确证。

Two methods for synthesizing irbesartan were reported.From 2 n butyl 1,3 diazaspiro〔4 4〕 non 1 en 4 one(2) and 4 bromomethyl 2′ cyanobiphenyl(3),irbesartan was prepared by substitution and cyclization with a good yield of 63%.It can also be obtained from 2 and N protected 5 through substitution and deprotection.The overall yield was 85%.The structure was confirmed by 1H NMR and MS.