Efficient One-Pot Synthesis of 2,3-Dihydropyrimidinthiones via Multicomponent Coupling of Terminal Alkynes, Elemental Sulfur, and Carbodiimides

摘要

Multicomponent reactions (MCRs) have become very useful for fast and efficient construction of important molecules. Utilization of common and readily available chemicals as their components and involvement of selective cleavage of chemical bonds such as C=N double bonds and C-H bonds should make an MCR much more attractive both fundamentally and synthetically. Herein we report a novel organolithium-promoted MCR involving terminal alkynes, sulfur, and carbodiimides (Scheme 1) that affords 2,3-dihydropyrimidinthiones via C=N double bond cleavage and sp C-H bond functionalization of the carbodiimide molecule.