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

Abstract

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.