拉唑类药物中间体硫醚化合物的合成
Synthesis of the Sulfoether Intermediates of Prazole Compounds
DOI: 10.12677/JOCR.2014.22004, PDF, HTML, 下载: 2,570  浏览: 9,132  科研立项经费支持
作者: 刘善和, 方红新, 张千峰:安徽国星生物化学有限公司,马鞍山;范芳芳:安徽工业大学分子工程与应用化学研究所,马鞍山
关键词: 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
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。
Abstract: 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.
文章引用:刘善和, 范芳芳, 方红新, 张千峰. 拉唑类药物中间体硫醚化合物的合成[J]. 有机化学研究, 2014, 2(2): 22-27. http://dx.doi.org/10.12677/JOCR.2014.22004

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