埃索美拉唑镁的合成工艺研究

The research on synthesis process of esomeprazole magnesium

本文以2-巯基-5-甲氧基苯并咪唑和2-(氯甲基)-4-甲氧基-3,5-二甲基吡啶盐酸盐为原料,依次经过缩合、不对称氧化、埃索美拉唑成钠盐、拆分和埃索美拉唑成镁盐这五步反应得到符合药典要求的埃索美拉唑镁,总收率达到73%。该路线操作简单,反应收率高,重复性好,适合工业化大生产。

The 2-mercapto-5-methoxy-benzimidazole and 2-（ chloromethyl ） -4-methoxy-3 , 5-dimethylpyridine hydrochloride were used as raw materials, followed by condensation, asymmetric oxidation, the formation of sodium salt of esomeprazole, resolution, and esomeprazole magnesium salt the five-step reaction to meet the requirements of the pharmacopoeia of esomeprazole magnesium. Fi- naly,and the total yield was 73%. The route was suitable for industrial production.