化学学报 ›› 2015, Vol. 73 ›› Issue (12): 1302-1306.DOI: 10.6023/A15040263 上一篇    下一篇

所属专题: 碳氢键官能团化

研究通讯

铜促进下腙的氧化胺化反应:1H-吲唑和1H-吡唑的合成

丁正伟a, 谭启涛a, 刘秉新a, 张可a, 许斌a,b,c   

  1. a 上海大学化学系 上海 200444;
    b 中国科学院上海有机化学研究所金属有机化学国家重点实验室 上海 200032;
    c 华东师范大学化学系上海市绿色化学与化工过程绿色化重点实验室 上海 200062
  • 收稿日期:2015-04-16 出版日期:2015-12-15 发布日期:2015-06-15
  • 通讯作者: 许斌, 谭启涛 E-mail:xubin@shu.edu.cn;qttan@shu.edu.cn
  • 基金资助:

    项目受国家自然科学基金(Nos.21272149,21302123),上海市教委科研创新重点项目(No.14ZZ094)以及上海市自然科学基金(No.13ZR1416400)资助.

Copper-Promoted Oxidative C-H Bond Amination of Hydrazones:Synthesis of 1H-Indazoles and 1H-Pyrazoles

Ding Zhengweia, Tan Qitaoa, Liu Bingxina, Zhang Keaa, Xu Bina,b,c   

  1. a Department of Chemistry, Shanghai University, Shanghai 200444;
    b State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032;
    c Shanghai Key Laboratory of Green Chemistry and Chemical Processes, Department of Chemistry, East China Normal University, Shanghai 200062
  • Received:2015-04-16 Online:2015-12-15 Published:2015-06-15
  • Supported by:

    Project supported by the National Natural Science Foundation of China(Nos. 21272149, 21302123), Innovation Program of Shanghai Municipal Education Commission(No. 14ZZ094) and Science and Technology Commission of Shanghai Municipality(No. 13ZR1416400).

吲唑和吡唑是两类重要的含氮杂环化合物,具有广泛的生物活性.发展了一类铜促进下腙的C(sp2)-H键氧化胺化反应,简便、高效地构建了一系列1H-吲唑和1H-吡唑衍生物.该反应条件温和,具有广泛的底物适用范围和较好的官能团兼容性.

关键词: 碳-氢键活化, 胺化, 吲唑, 含氮杂环, 吡唑

An efficient copper-promoted C(sp2)-H bond amination was developed to afford 1H-indazoles and 1H-pyrazoles in moderate to excellent yields from easily accessible hydrazones. This process tolerated a variety of functional groups and afforded the corresponding 1H-indazoles and 1H-pyrazoles under mild conditions.

Key words: C-H activation, amination, indazole, nitrogen heterocycles, pyrazole