Asymmetric Synthesis of γ-Lactams Containing α,β-Contiguous Stereocenters via Pd(II)-Catalyzed Cascade Methylene C(sp)-H Alkenylation/Aza-Wacker Cyclization.

γ-Lactam containing α,β-contiguous stereogenic centers stands out as a pivotal motif in various bioactive compounds, while its efficient synthesis still needs to be enhanced. Herein, an asymmetric C-H activation strategy for accessing α,β-stereospecific γ-lactams in good yields (≤79%) with high enantio- and diastereoselectivities (≤96% ee and >20:1 dr) was described, which serves as an effective supplement to the existing strategies.