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Journal of Chinese Pharmaceutical Sciences ›› 2022, Vol. 31 ›› Issue (12): 938-945.DOI: 10.5246/jcps.2022.12.079

• Original articles • Previous Articles     Next Articles

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

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: