Sustainable access to benzothiophene derivatives bearing a trifluoromethyl group via a three-component domino reaction in water

Abstract

A catalyst-free three-component domino reaction was developed for the synthesis of benzothiophene fused pyrrolidones bearing a CF₃ group for the first time. The notable advantages of this strategy over the existing methods include the use of water as a solvent at room temperature, transition metal-free conditions, a broad substrate scope, and easy scale-up synthesis. More importantly, the benzothiophene derivatives have been found to show potent anticancer activities using the Cell Counting Kit-8 (CCK-8) assay.