右旋雷贝拉唑钠的合成

Synthesis of Dexrabeprazole Sodium

2-氯甲基-4-(3-甲氧基丙氧基)-3-甲基吡啶盐酸盐(化合物2)与2-巯基苯并咪唑(化合物3)经缩合反应制得2-[[[4-(3-甲氧基丙氧基)-3-甲基-2-吡啶基]甲基]硫代]-1H-苯并咪唑(化合物4),化合物4经不对称氧化、成钠盐制得右旋雷贝拉唑钠(化合物1),总收率为56%(以化合物2计),纯度99.91%,ee值99.96%。

Dexrabeprazole sodium(Compound 1) was synthesized from 2-(chloromethyl)-4-(3-methoxypropoxy)- 3-methylpyridine hydrochloride (Compound 2) and 2-mercaptobenzimidazole(Compound 3) by condensation to give 2-[[[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methyl]thio]-1H-benzimidazole (Compound 4), followed by asymmetric oxidation and salification with the yield of 56%(based on compound 2). The purity was 99.91%, and the ee value was 99.96%.