One-Pot Functionalization of 8-Aminoquinolines through the Acylation and Regioselective C5-H Halogenation under Transition-Metal-Free Conditions

A mild and efficient functionalization of 8-aminoquinolines has been demonstrated through the acylation and regioselective C5-H halogenation in one pot under transition metal free conditions. This method enables the acyl halides acting as the donors of both acyl and halide atoms. Moremover, different type of acyl halides could be employed in this reaction and proceeded smoothly to afford the corresponding halogenated products in moderate to good yields. The protocol is operationally simple, facile, and might have potential application in synthesis of 5-halogenated quinoline scaffolds.