标题:
拉唑类药物中间体硫醚化合物的合成Synthesis of the Sulfoether Intermediates of Prazole Compounds
作者:
刘善和, 范芳芳, 方红新, 张千峰
关键字:
质子泵抑制剂, 新药研发, 合成, 硫醚化合物Proton Pump Inhibitors (PPIs), Drug Development, Synthesis, Sulfoether Compounds
期刊名称:
《Journal of Organic Chemistry Research》, Vol.2 No.2, 2014-06-20
摘要:
通过质子泵抑制剂作用机理设计了四种具有潜在治疗消化性疾病疗效的质子泵抑制剂衍生物，该类化合物可作为新药筛选的候选药物，为新药研发提供参考。采用的2-氯甲基-4-烷氧基-甲基吡啶盐酸盐、硫醇和甲醇钠的摩尔配比为1:1.1:2.5，高效地合成了该类化合物的硫醚中间体，硫醚产率基本在80%以上，反应条件温和，操作简单。
Four derivatives of proton pump inhibitors which have potential therapeutic efficacy of digestive diseases were designed based on the mechanism of action of proton pump inhibitor. These com- pounds can be used as new drug candidates and provide a reference for new drug development. Finally, these sulfoether intermediates were efficiently synthesized by using 2-chloro-4-alkoxy- methylpyridine hydrochloride, mercaptan and sodium methoxide, and the molar ratio of the three ingredients is 1:1.1:2.5. The yields of them are mostly above 80%. The reaction has the advantage of mild conditions and simple operation.