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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.
Du et al. (2018) studied this question.