A Straightforward One-Pot Synthesis of 3,4-Dihydroquinazoline-2(1H)-thione Derivatives in Aqueous Organic Solvent

摘要

A novel and efficient method has been developed for the synthesis of a series of 3,4-dihydroquinazoline-2(1H)-thione derivatives in aqueous organic solvent starting from 3-(2-aminophenyl)acrylates with isothiocyanates via a tandem intermolecular nucleophilic addition/intramolecular Michael addition reaction under mild conditions. A broad substrate scope has been demonstrated, which shows wide functional group tolerance and chemical specialization. The efficiency of the methodology could make this process available on gram-scale.