Pd-Catalyzed C-H/C-C Cascade Activation for the Synthesis of γ-Lactams

This work establishes a palladium-catalyzed cascade reaction combining C(sp³)-H functionalization and C-C bond cleavage of cyclopropanes, enabling the direct and efficient construction of biologically relevant dihydro-2H-pyrrol-2-ones (γ-lactams) from readily accessible cyclopropanecarboxamides and diazo compounds. By introducing an α-substituent and directing group, this strategy facilitates the C-H activation of the cyclopropanes and the subsequent carbene migratory insertion, followed by directing group assisted β-carbon elimination enabling selective C-C cleavage. This method offers a concise and efficient approach to accessing γ-lactam-containing architectures of pharmaceutical interest.