有机化学 ›› 2015, Vol. 35 ›› Issue (5): 1156-1160.DOI: 10.6023/cjoc201411040 上一篇    下一篇

研究简报

钯催化的基于C—H活化合成C-8位芳基取代嘌呤类似物

牛红英a, 苏凌云b, 张齐齐a, 张婉娜a, 付红岩a, 李建平b, 渠桂荣b, 郭海明b   

  1. a 河南科技学院化学化工学院 新乡 453003;
    b 河南师范大学化学与化工学院 新乡 453007
  • 收稿日期:2014-11-25 修回日期:2014-12-29 发布日期:2015-01-09
  • 通讯作者: 郭海明 E-mail:ghm@htu.cn
  • 基金资助:

    国家自然科学基金(Nos.21272059,21202039,21472037)、河南省高校科技创新人才支持计划(No.13HASTIT013)、国家大学生创新训练计划(No.201310467062)资助项目.

Pt Catalyzed C—H Activation of Purines and Aryl Boric Acids to 8-Aryl Purine Analogues

Niu Hongyinga, Su Lingyunb, Zhang Qiqia, Zhang Wannaa, Fu Hongyana, Li Jianpingb, Qu Guirongb, Guo Haimingb   

  1. a School of Chemistry and Chemical Engineering, Henan Institute of Science and Technology, Xinxiang 453003;
    b School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007
  • Received:2014-11-25 Revised:2014-12-29 Published:2015-01-09
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos.21272059, 21202039, 21472037), the Program for Science & Technology Innovation Talents in Universities of Henan Province (No.13HASTIT013), and the National Training Programs of Innovation for Undergraduates (No.201310467062).

以芳基硼酸为芳基化试剂, 以Pd(PPh3)4为催化剂, CuI为添加剂, 哌啶为碱, 在DMF中于125 ℃反应24 h, 通过C—H键的活化反应, 合成了系列C-8位芳基取代的嘌呤类似物, 为该类化合物的合成提供了新的合成路线.

关键词: 嘌呤, C—H键活化, 芳基硼酸, 芳基化

C-8 aryl substituted purine analogues were successfully synthesized by direct C—H activation of purines with aryl boric acids catalyzed by Pd(PPh3)4 in the presence of CuI and piperidine in DMF at 125 ℃ for 24 h, providing a new process for the syn-thesis of 8-aryl purines.

Key words: purine, C—H activation, aryl boric acid, arylation