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尿嘧啶类化合物碘代方法的研究

李立, 覃华, 张亮, 王孝伟, 刘俊义*

  

  1. 1. 北京大学医学部 天然药物及仿生药物国家重点实验室, 北京 100191
    2. 北京大学医学部 药学院 化学生物学系, 北京 100191

  • 收稿日期:2009-11-16 修回日期:2010-02-20 出版日期:2010-03-15 发布日期:2010-03-15
  • 通讯作者: 刘俊义*

Study on the iodination of uracil derivatives

Li Li, Hua Qin, Liang Zhang, Xiao-Wei Wang, Jun-Yi Liu*

  

  1. 1. State Key Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing 100191, China
    2. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China

  • Received:2009-11-16 Revised:2010-02-20 Online:2010-03-15 Published:2010-03-15
  • Contact: Jun-Yi Liu*

摘要: 5-碘尿嘧啶类化合物具有很好的生物学活性, 并且是重要医药中间体, 方便在5位引入多种基团。为了寻找一个简便有效的嘧啶环5位的碘代方法, 我们尝试了碘/二氧化铅, 碘/硝酸铈胺和一氯化碘三种方法来进行实验, 并对其结果进行了比较, 为不同取代类型的尿嘧啶和2-硫尿嘧啶衍生物的碘代方法提供了很好的选择依据。

关键词: 尿嘧啶, 2-硫尿嘧啶, 碘代, 二氧化铅, 硝酸铈胺, 一氯化碘

Abstract: 5-Iodouracil derivatives have interesting biological activities and can serve as important substrates for the metal-catalyzed cross-coupling reactions to introduce alkyl, alkenyl, and alkynyl groups to the C-5 position of uracil derivatives. In order to find a good method to iodinate directly the C-5 of uracil derivatives, we investigated three methods, which included iodine/lead (IV) dioxide, iodine/ammonium hexanitratocerate (CAN) and iodine chloride, and examined their reactivity to different types of uracil and thiouracil derivatives.

Key words: Iodination, Lead (IV) dioxide, Ammonium hexanitratocerate, Iodine chloride, Uracil, 2-Thiouracil

中图分类号: 

Supporting:

Foundation items: National Natural Science Foundation of China (Grant No. 20172007; 20672008).
*Corresponding author. Tel.: 86-10-82805203