有机化学 ›› 2018, Vol. 38 ›› Issue (8): 1940-1948.DOI: 10.6023/cjoc201804004 上一篇    下一篇

所属专题: 碳氢活化合辑2018-2019

综述与进展

基于C-H键官能团化合成芳香伯胺的研究进展

徐琳琳a, 徐辉c, 林海霞a, 戴辉雄b   

  1. a 上海大学化学系 上海大学创新药物研究中心 上海 200444;
    b 中国科学院上海药物研究所 药物化学研究室 上海 201203;
    c 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
  • 收稿日期:2018-04-02 修回日期:2018-04-23 发布日期:2018-05-03
  • 通讯作者: 林海霞, 戴辉雄 E-mail:haixialin@staff.shu.edu.cn;hxdai@sioc.ac.cn
  • 基金资助:

    国家自然科学基金委基金(No.21772211)和中国科学院青年创新促进会(No.2014229)资助项目.

Progress in the Synthesis of Primary Anilines via C-H Bond Functionalization

Xu Linlina, Xu Huic, Lin Haixiaa, Dai Huixiongb   

  1. a Department of Chemistry, Innovative Drug Research Center, Shanghai University, Shanghai 200444;
    bDepartment of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203;
    c State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032
  • Received:2018-04-02 Revised:2018-04-23 Published:2018-05-03
  • Contact: 10.6023/cjoc201804004 E-mail:haixialin@staff.shu.edu.cn;hxdai@sioc.ac.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21772211) and the Youth Innovation Promotion Association of Chinese Academy of Sciences (No. 2014229).

芳香伯胺类化合物在医药、农药以及材料化学中都有着广泛的应用.近年来,通过发展绿色高效C-N键构建方法引入伯胺是化学合成领域研究的热点之一.直接C-H键官能团化向目标分子中引入伯胺的策略因其高效实用的优点受到了化学家们的广泛关注.主要总结最近几年芳香C(sp2)-H伯胺化反应的研究进展,并对该领域所面临的挑战及发展前景做了总结和展望.

关键词: 氨基化, C-H键官能团化, 伯胺, 过渡金属催化

Primary anilines are widely used in pharmaceutical, agrochemicals and material chemistry. In recent years, the green and efficient methods for constructing carbon-nitrogen (C-N) bonds to introduce primary amines has been one of the hottest topics in chemical synthesis. The direct C-H primary amination of aromatic compounds have received considerable attention due to its high efficiency and practicality. The recent progress in the C-H primary amination of aromatic compounds reactions is reviewed. Furthermore, the synthetic challenge and prospect in the future development for the synthesis of primary anilines through direct C-H amination are summarized.

Key words: amination, C-H bond functionalization, primary anilines, transition-metal catalyzed