Synthesis of polysubstituted quinolines via copper(ii)-catalyzed annulation of 2-aminoaryl ketones with alkynoates

Abstract

Copper triflate catalyzed annulation of 2-aminoaryl ketones with internal alkynes has been developed for the synthesis of polysubstituted quinolines in high yields under solvent-free conditions. Phenyl propiolic acid afforded the 3-unsubstituted quinolines via decarboxylation. The protocol is compatible with various internal alkynes and is expected to find wide applications due to its operational simplicity.