【摘要】 目的为了完善与强化对原料药雷贝拉唑钠的质量控制,合成雷贝拉唑钠有关物质。方法以2-巯基-1H-苯并咪唑和2-氯甲基-4-(3-甲氧基丙氧基)-3-甲基吡啶盐酸盐为原料,合成2-[[[4-(3-甲氧基丙氧基)-3-甲基吡啶-2-基]甲基]硫代]-1H-苯并咪唑(1)和2-[[[4-(3-甲氧基丙氧基)-3-甲基-1-氧代吡啶-2-基]甲基]磺酰基]-1H-苯并咪唑(3);以雷贝拉唑为原料,合成2-[[[4-(3-甲氧基丙氧基)-3-甲基-2-吡啶基]甲基]磺酰基]-1H-苯并咪唑(2)。结果与结论目标化合物的结构经核磁、质谱确证,纯度均大于99.8%,可作为质量控制的标准品。本实验反应条件温和、生成副产物较少、操作简单,并且采用双氧水为氧化剂,降低了成本、减少了环境污染。更多还原

【Abstract】 Rabeprazole sodium is a new generation of proton pump inhibitor drugs. To enhance the quality control of rabeprazole sodium,three related substances( 1,2,3) were synthesized. The target compounds were synthesized from 2-chloromethyl-3-methyl-4-( 3-methoxypropoxy) pyridine hydrochloride and 2-mercaptobenzimidazole and rabeprazole. Their structures were confirmed by MS,~1H-NMR. The three impurities can be used in the quality control of rabeprazole sodium. This synthetic route is simple,raw materials are cheap and easy to obtain and reaction conditions are mild. This method has the advantages of environmental protection and reducing the cost of production.更多还原