右旋雷贝拉唑钠的合成  

Synthesis of Dexrabeprazole Sodium

作　　者：唐尧[1] 潘迅 卜凡友 Tang Yao;Pan Xun;Bu Fan-you(Jiangsu Aosaikang Pharmaceutical Co., Ltd., Jiangsu Nanjing 211112)

机构地区：[1]江苏奥赛康药业有限公司

出　　处：《生物化工》2019年第4期119-120,140,共3页Biological Chemical Engineering

摘　　要：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%.

关 键 词：右旋雷贝拉唑钠 新型质子泵抑制剂 抗溃疡药 不对称氧化 合成 

分 类 号：TQ460.6[化学工程—制药化工]