Palladium‐Catalyzed Intermolecular Carboamidation of Alkenes with Alkynamides for the Assembly of Structurally Diverse γ‐Lactams

Comprehensive Summary γ‐Lactam is one of the most prevalent heterocyclic building blocks in organic synthesis and pharmaceutical chemistry. However, the direct use of alkynamides as the synthon for the preparation of structurally diverse γ‐lactams has remained much underexplored so far. Herein, we presented the first palladium‐catalyzed intermolecular carboamidation of alkenes with alkynamides for constructing polyfunctionalized α‐methylene‐γ‐lactams under aerobic oxidative conditions. More importantly, this protocol features broad substrate scope, good functional group tolerance, and good step‐ and atom‐economy. Remarkably, the synthetic value of this synthetic strategy is further demonstrated by applications in the gram‐scale synthesis and the late‐stage diversification of pharmaceuticals molecules.