Heteroaryldifluoromethylation of organoborons catalyzed by palladium: facile access to aryl(heteroaryl)difluoromethanes

Org Lett. 2014 Sep 19;16(18):4822-5. doi: 10.1021/ol502121m. Epub 2014 Sep 5.

Abstract

A first example of Pd-catalyzed heteroaryldifluoromethylation of organoborons with bromodifluoromethylated heteroarenes has been described. The use of phosphine ligand PAd2(n-Bu)·HI is critical for the reaction efficiency. With use of this ligand, a wide range of aryl(heteroaryl)difluoromethanes were obtained with high efficiency. The notable features of this reaction are its broad substrate scope and excellent functional group compatibility, thus providing a facile protocol for application in drug discovery and development.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Drug Discovery
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Hydrocarbons, Fluorinated / chemistry
  • Ligands
  • Molecular Structure
  • Palladium / chemistry*
  • Phosphines / chemistry

Substances

  • Hydrocarbons, Fluorinated
  • Ligands
  • Phosphines
  • Palladium
  • difluoromethane
  • phosphine