应用化学 ›› 2019, Vol. 36 ›› Issue (2): 182-187.DOI: 10.11944/j.issn.1000-0518.2019.02.180094

• 研究论文 • 上一篇    下一篇

微波辅助铜合成2-(N,N-二甲氨基)苯并噁唑衍生物

林晨a,林小燕a,张鹏a,许贻文a,许建华ab,柯方ab*()   

  1. 福建医科大学 a药学院
    b新药研究所 福州 350004
  • 收稿日期:2018-03-30 出版日期:2019-02-01 发布日期:2019-01-31
  • 通讯作者: 柯方
  • 基金资助:
    福建省科技厅研究基金项目(2016J01686,2016J01372,2016Y9051,2017J01820)福建医科大学苗圃基金(2015MP008)资助

Copper-catalyzed Microwave-Assisted Synthesis of N,N-Dimethyl-2-benzoxazolamine Derivatives

LIN Chena,LIN Xiaoyana,ZHANG Penga,XU Yiwena,XU Jianhuaab,KE Fangab*()   

  1. aDepartment of Pharmacy,Fujian Medical University,Fuzhou 350004,China
    bInstitute of Materia Medica,Fujian Medical University,Fuzhou 350004,China
  • Received:2018-03-30 Published:2019-02-01 Online:2019-01-31
  • Contact: KE Fang
  • Supported by:
    Supported by the Department of Fujian Province Natural Science and Technology Foundation(No.2016J01686, No.2016J01372, No.2016Y9051, No.2017J01820), the Fund of Fujian Medical University(No.2015MP008)

摘要:

建立了一种简单实用、经济高效的以取代2-碘芳胺和N,N-二甲基氨基硫代甲酰氯为原料,以碘化亚铜为催化剂,吡啶为溶剂,100 ℃条件下,串联合成2-(N,N-二甲氨基)苯并噁唑衍生物的微波催化体系,合成了一系列中等至良好产率的2-(N,N-二甲氨基)苯并噁唑衍生物,最高产率达90%。

关键词: 微波辅助合成, 2-(N,N-二甲氨基)苯并噁唑, 碘化亚铜

Abstract:

Microwave-assisted one-pot synthesis of a variety of N,N-dimethyl-2-benzoxazolamine derivatives were achieved by the cascade reaction of substituted 2-iodoanilines with dimethylcarbamothioic chloride in pyridine in the presence of CuI at 100 ℃ with moderate to good yields(up to 90%).

Key words: microwave-assisted synthesis, N,N-dimethyl-2-benzoxazolamines, 2-iodoanilines