Asymmetric Synthesis of γ-Lactams Containing α,β-Contiguous Stereocenters via Pd(II)-Catalyzed Cascade Methylene C(sp3)-H Alkenylation/Aza-Wacker Cyclization

gamma-Lactam containing alpha,beta-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 alpha,beta-stereospecific gamma-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.

Automated summary

The paper describes an asymmetric C-H activation strategy for accessing alpha,beta-stereospecific gamma-lactams in good yields with high enantio- and diastereoselectivities, serving as an effective supplement to existing strategies.