Palladium-catalyzed intramolecular C-H acylation of indoles with thioester

A palladium-catalyzed intramolecular C-H acylation of indole with thioester is described, providing a direct and effective approach for the synthesis of the biologically active indole-indolone scaffolds. The method obviates the need for the prefunctionalized starting materials including organometallic reagents, alkyl halides, and NHP esters in previous metal-catalyzed cross-coupling reaction with thioester. Substrates bearing sensitive halo groups are compatible in the reaction, leaving a functional handle for further structural elaborations. (C) 2019 Elsevier Ltd. All rights reserved.