Base-mediated three-component system for the synthesis of S-substituted N-acyl ureas

Abstract

N-Acyl ureas are crucial intermediates in the synthesis of biologically active molecules, and their preparation traditionally relies on multi-step synthesis under reflux conditions. Here, we report a three-component system that combines widespread alkyl halides, thiourea and carbamoyl chlorides. Crucial to this strategy is the synthesis of specific S-substituted N-acyl ureas via the formation of the isothiouronium salt intermediates. This developed three-component system affords scalable and functional group-tolerant reactivity, furnishing the desired products in good to excellent yields under mild conditions.