4.7 Article

Synthesis of N-(α-Fluorovinyl)azoles by the Reaction of Difluoroalkenes with Azoles

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 79, Issue 14, Pages 6395-6402

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jo5005845

Keywords

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Funding

  1. National Natural Science Foundation of China [21272070, 21072057]
  2. National Basic Research Program of China (973 Program) [2010CB126101]
  3. Twelfth Five-year Plan of China [2011BAE06B01-15]

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A mild and versatile method for the construction of C-N bonds by the reaction of (2,2-difluorovinyl)arenes with various N-H-containing heterocycles in the presence of K3PO4 has been developed. The reaction proceeded efficiently at room temperature (25 degrees C) affording the (E)-N-alpha-fluorovinyl derivatives of azoles 3 in good to excellent yields with relatively high stereoselectivity.

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