4.8 Article

Nickel-Catalyzed α-Arylation of Zinc Enolates with Polyfluoroarenes via C-F Bond Activation under Neutral Conditions

Journal

ORGANIC LETTERS
Volume 16, Issue 21, Pages 5544-5547

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol502499q

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Funding

  1. National Key Technologies RD Program [2011BAE06B05]
  2. National Natural Science Foundation of China [21172245/21172244/21372247]
  3. SIOC

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The first nickel-catalyzed alpha-arylation of 2-(polyfluorophenyl) pyridine with zinc enolates of esters or amides via C-F bond activation under neutral conditions is described. A variety of functional groups such as ester, amide, ether, and amine were tolerated. This method provides a simple and useful tool to synthesize fluorinated a-aryl carboxylic acids and a-aryl amides that are important intermediates for drug discovery

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