4.7 Article

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

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ORGANIC CHEMISTRY FRONTIERS
卷 8, 期 3, 页码 560-565

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ROYAL SOC CHEMISTRY
DOI: 10.1039/d0qo01323d

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  1. Program of High-level Talents of Nantong University [03083031]
  2. Large Instruments Open Foundation of Nantong University

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

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