Palladium-Catalyzed Direct Oxidative C–H Activation/Annulation for Regioselective Construction of <i>N</i>‑Acylindoles

A Pd­(II)-catalyzed C­(sp3)–H/C­(sp2)–H coupling/annulation of anilides and α-dicarbonyl compounds for the synthesis of diverse N-acyl indoles is described. The reaction is achieved by cascade C–H activation, coupling, and intramolecular cyclization. This protocol provides a variety of indoles with high functional group tolerance and excellent regioselectivity. The utility of this protocol is demonstrated by transforming the synthesized compound into diversely functionalized analogues.