Highly efficient one-pot tandem Friedlander annulation and chemo-selective Csp3-H functionalization under calcium catalysis

Abstract

A highly efficient and regioselective Friedlander synthesis of 2-methyl-3-acyl quinolines is described, which occurs under solvent-free conditions and employs calcium triflate as a sustainable catalyst. For the first time in the literature, these 2-methyl-3-acyl quinolines undergo an in situ chemoselective Csp3-H functionalization to furnish structurally enriched quinoline heterocycles in high yields and with atom and step economy.