4.8 Article

Palladium-Catalyzed Intramolecular C-H Difluoroalkylation: Synthesis of Substituted 3,3-Difluoro-2-oxindoles

期刊

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 54, 期 5, 页码 1646-1650

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201410471

关键词

C-H activation; cross-coupling; fluorine; heterocycles; palladium

资金

  1. National Institutes of Health [GM46059]
  2. JSPS

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The synthesis of 3,3-difluoro-2-oxindoles through a robust and efficient palladium-catalyzed C-H difluoroalkylation is described. This process generates a broad range of difluorooxindoles from readily prepared starting materials. The use of BrettPhos as the ligand was crucial for high efficiency. Preliminary mechanistic studies suggest that oxidative addition is the rate-determining step for this process.

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