Pd-Catalyzed Three-Component Coupling of Aryl Bromides, Alkynes, and Anthranils To Access <i>ortho</i> Carbonyl N-Aryl Indoles

A palladium-catalyzed three-component coupling of aryl bromides, alkynes, and anthranils has been developed for the direct and efficient synthesis of <i>ortho</i> carbonyl-substituted N-aryl indoles featuring a C-N chiral axis. Anthranil serves as an aryl nitrene precursor in this reaction, facilitating the expedient conversion of C,C-palladacycles into N-aryl indoles through sequential C-N bond formation. The <i>in situ</i> generated <i>ortho</i> carbonyl group within the product structure can be conveniently transformed into other functionalities, thereby enhancing the synthetic utility of this methodology.