Asymmetric Synthesis of γ-Lactams Containing α,β-Contiguous Stereocenters via Pd(II)-Catalyzed Cascade Methylene C(sp³)–H Alkenylation/Aza-Wacker Cyclization
2021
Wu, Le-Song | Ding, Yi | Han, Ye-Qiang | Shi, Bing-Feng
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.
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