奥美沙坦酯关键中间体的合成工艺改进

Improved synthesis of the key intermediate of olmesartan medoxomil

目的优化奥美沙坦酯关键中间体的合成工艺。方法以4-(1-羟基-1-甲基乙基)-2-丙基咪唑-5-羧酸乙酯为原料,与4-[2-(2-三苯甲基四唑-5-基)苯基]苄基溴缩合合成关键中间体4-(1-羟基-1-甲基乙基)-2-丙基-1-[2'-(三苯甲基四唑-5-基)联苯基-4-基甲基]咪唑-5-羧酸乙酯。结果与结论该优化的合成方法操作简便,制备的中间体收率为55%,质量较好。

Objective To improve synthetic method of the key intermediate of olmesartan medoxomil. Methods 4 - （ 1 - hydroxy - 1 - methyl - ethyl ） - 2 - propyl - 1 - [ 2 - （ triphenylmethyl tetrazole - 5 - yl ） biphenyl - 4 - methyl ] imidazole - 5 - carboxylic acid ethyl ester was synthesized from 4 - （ 1 - hydroxy - 1 - methyl - ethyl ） - 2 - propylimidazole - 5 - earboxylate ethyl ester through condensation with 4 - [ 2 - （ 2 - （ triphenylmethyl ） tetrazole - 5 - yl ） phenyl ] benzyl bromide. Results and Conclusion The optimized synthesis method was simple with 55% yield of the intermediate and the quality was good.