Electrochemical Difluoromethylarylation of Alkynes

J Am Chem Soc. 2018 Feb 21;140(7):2460-2464. doi: 10.1021/jacs.8b00391. Epub 2018 Feb 9.

Abstract

An unprecedented radical difluoromethylarylation reaction of alkynes has been developed by discovering a new difluoromethylation reagent, CF2HSO2NHNHBoc. This air-stable and solid reagent can be prepared in one step from commercially available reagents CF2HSO2Cl and NH2NHBoc. The CF2H radical, generated through ferrocene-mediated electrochemical oxidation, participates in an unexplored alkyne addition reaction followed by a challenging 7-membered ring-forming homolytic aromatic substitution step to afford fluorinated dibenzazepines.

Publication types

  • Research Support, Non-U.S. Gov't