Palladium(II)-Catalyzed Direct C7-Acyloxylation of Indoles

We report a palladium-catalyzed C-H acyloxylation of indoles that achieves excellent regioselectivity at the C7 position. The synergistic combination of a methylsulfonyl directing group and a pyridone-based ligand was crucial to overriding the inherent preference for functionalization at the C3 position. The reaction features a broad substrate scope and good functional group tolerance and provides direct access to valuable 7-acyloxylated indole derivatives.