Asymmetric Synthesis of γ‑Lactams Containing α,β-Contiguous Stereocenters via Pd(II)-Catalyzed Cascade Methylene C(sp3)–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 enan...
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Veröffentlicht in: | Organic letters 2021-03, Vol.23 (6), p.2048-2051 |
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Hauptverfasser: | , , , |
Format: | Artikel |
Sprache: | eng |
Online-Zugang: | Volltext |
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Zusammenfassung: | 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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ISSN: | 1523-7060 1523-7052 |
DOI: | 10.1021/acs.orglett.1c00204 |