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中国药学(英文版) ›› 2022, Vol. 31 ›› Issue (12): 938-945.DOI: 10.5246/jcps.2022.12.079

• 【研究论文】 • 上一篇    下一篇

利用连续流动反应一锅法合成不对称芳香脲的Curtius重排反应

佟盟, 詹威, 牛铖铖, 葛泽梅, 李润涛*(), 王欣*()   

  1. 北京大学 药学院, 北京 100191
  • 收稿日期:2022-10-12 修回日期:2022-10-26 接受日期:2022-11-15 出版日期:2022-12-27 发布日期:2022-12-28
  • 通讯作者: 李润涛, 王欣
  • 作者简介:
    + Tel.: +86-10-82805553, E-mail:
  • 基金资助:
    National Natural Science Foundation of China (Grant No. 21877005).

Continuous-flow, one-pot synthesis of asymmetrical aromatic ureas from acids and amines via curtius rearrangement

Meng Tong, Wei Zhan, Chengcheng Niu, Zemei Ge, Runtao Li*(), Xin Wang*()   

  1. School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
  • Received:2022-10-12 Revised:2022-10-26 Accepted:2022-11-15 Online:2022-12-27 Published:2022-12-28
  • Contact: Runtao Li, Xin Wang

摘要:

利用连续流动反应一锅法完成Curtius重排, 通过胺和异氰酸酯的亲核加成反应合成不对称脲。本方法的优点是底物范围广、产率高、反应快速、方法简单、安全性高及易规模化合成。

关键词: 连续流动反应, 不对称脲, Curtius反应, 安全性

Abstract:

In the present study, we described a continuous-flow, one-pot synthesis of asymmetrical ureas using nucleophilic addition reaction of amines to isocyanates derived from acids’ Curtius rearrangement. The advantages of this method included broad substrate scope, high yields, rapid reaction, simplicity, extraordinary safety, and easy scale-up.

Key words: Continuous-flow reaction, Asymmetrical urea, Curtius reaction, Safety

Supporting: