Pd(II)-Catalyzed Csp2–H Carbonylative Amidation of Groebke–Blackburn–Bienaymé Reaction Products: Access to Imidazo[1,2-a]pyridine-Fused δ-Lactams
The Groebke–Blackburn–Bienaymé (GBB) reaction provides efficient access to imidazole-fused heterocycles, yet it is inevitably endowed with an isocyanide-derived secondary amino group in products. Herein, we report a Pd(II)-catalyzed sp2 C–H carbonylative amidation strategy using Co2(CO)8 as a safe CO surrogate. Leveraging the native aryl amino group as a directing motif, this protocol enables direct conversion of GBB adducts into pharmaceutically relevant imidazo[1,2-a]pyridine-fused δ-lactams with up to 86% yield. The method demonstrates exceptional functional group tolerance and eliminates prefunctionalization requirements, offering a streamlined approach to access complex nitrogen-rich architectures.
研究领域:
有机化学
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药物化学
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杂环化学
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转化医学
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分子药理学
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）