Copper(II)‐Catalyzed Aerobic Oxidative Coupling between Chalcone and 2‐Aminopyridine via CH Amination: An Expedient Synthesis of 3‐Aroylimidazo[1,2‐a]pyridines

A simple and efficient protocol has been developed for the synthesis of 3‐aroylimidazopyridines via copper(II) acetate‐catalyzed aerobic oxidative amination. A library of 3‐aroylimidazopyridines was synthesized from readily accessible chalcones and 2‐aminopyridines with high yields and regioselectivity. The reaction proceeds through a tandem Michael addition followed by an intramolecular oxidative amination. The successful application of this methodology for a gram‐scale reaction indicates its potential for bulk synthesis. magnified image