Palladium-Catalyzed C8-H Acylation of 1-Naphthylamines with Acyl Chlorides

A facile and efficient protocol for palladium-catalyzed regioselective C8-H acylation of 1-naphthylamine derivatives with acyl chlorides has been developed. The reaction exhibits broad functional group tolerance, and both aromatic and alpha,beta-unsaturated acyl chlorides can be effectively coupled with 1-naphthylamines. Moreover, the picolinamide moiety as a bidentate directing likely plays a key role in this regioselective transformation.