Selective synthesis of acylated caprolactam via sequential Michael addition/palladium-catalyzed alpha-arylation of ketones

A formal [6 + 1] annulation reaction through sequential Michael addition/palladium-catalyzed alpha-arylation of ketones has been developed. This approach provides an efficient route enabling rapid access to diverse acylated caprolactams by the double C-C bond formation of the same site from methyl ketones. In addition, the reaction features a broad substrate scope, good functional group tolerance, easy scale-up of reaction and useful transformations of the products.