Palladium-catalyzed mono- and double-carbonylation of indoles with amines controllably leading to amides and α-ketoamides.

A novel and efficient double-carbonylation of indoles with primary or secondary amines to yield indole-3-α-ketoamides has been developed and bioactive molecules could be one-pot synthesized using the current methodology, which could also be selectively switched to mono-carbonylation to afford indole-3-amides only by a slight modification of reaction conditions.