Copper-Catalyzed One-Pot N-Acylation and C5–H Halogenation of 8-Aminoquinolines: The Dual Role of Acyl Halides

摘要

The synthesis of N -acyl-5-halo-8-aminoquinolines has been realized by directly employing 8-aminoquinolines and acyl halides (Cl, Br, I) with copper catalysis. The construction of the target products involves domino N -acylation and C5–H halogenations of the 8-aminoquinoline, wherein the acyl halides act as the donors of both acyl and halide atoms, which enables the first access to the step efficient synthesis of 5-halogenated N -acyl quinlolines.