Palladium-catalyzed C-H ethoxycarbonyldifluoromethylation of electron-rich heteroarenes

Org Lett. 2015 Jun 5;17(11):2652-5. doi: 10.1021/acs.orglett.5b01024. Epub 2015 May 12.

Abstract

The first Pd-catalyzed C-H ethoxycarbonyldifluoromethylation with BrCF2CO2Et has been developed. The use of a bidentate phosphine ligand (Xantphos) is critical for the reaction to occur. A variety of electron-rich heteroarenes, including indoles, furans, thiophenes, and pyrroles, can be ethoxycarbonyldifluoromethylated in moderate to excellent yields. The reactions take place at the C-H bonds adjacent to the heteroatoms with high regioselectivity. This method provides a new protocol for the introduction of difuoroalkyl groups into electron-rich heteroarenes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Electrons*
  • Furans / chemical synthesis*
  • Furans / chemistry
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Methylation
  • Molecular Structure
  • Palladium / chemistry*
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry
  • Stereoisomerism
  • Thiophenes / chemical synthesis*
  • Thiophenes / chemistry

Substances

  • Furans
  • Indoles
  • Pyrroles
  • Thiophenes
  • Palladium