Nickel-catalyzed α-arylation of zinc enolates with polyfluoroarenes via C-F bond activation under neutral conditions.

Journal: Organic Letters
Published:
Abstract

The first nickel-catalyzed α-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 α-aryl carboxylic acids and α-aryl amides that are important intermediates for drug discovery.

Authors
Daohong Yu, Chang-sheng Wang, Cheng Yao, Qilong Shen, Long Lu