Hydrogen-free palladium-catalyzed intramolecular anti-Markovnikov hydroaminocarbonylation of 2-(1-methylvinyl)anilines.

The palladium-catalyzed intramolecular hydroaminocarbonylation of 2-(1-methylvinyl)aniline derivatives has been achieved using dppp (1,3-bis(diphenylphosphino)propane) as a ligand under hydrogen-free conditions. The reaction involves the generation of an active palladium hydride species with a catalytic amount of TsOH. This amide bond formation reaction was applied to the synthesis of various 4-substituted 3,4-dihydroquinolone derivatives with both high yield and regioselectivity.