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Palladium-catalyzed intramolecular C H acylation of indoles with thioester

Abstract 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… Click to show full abstract

Abstract 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.

Keywords: intramolecular acylation; acylation indoles; indoles thioester; palladium catalyzed; catalyzed intramolecular

Journal Title: Tetrahedron Letters
Year Published: 2019

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