Catalytic decarboxylative fluorination for the synthesis of tri- and difluoromethyl arenes

Org Lett. 2013 Jun 7;15(11):2648-51. doi: 10.1021/ol4009377. Epub 2013 May 20.

Abstract

Treatment of readily available α,α-difluoro- and α-fluoroarylacetic acids with Selectfluor under Ag(I) catalysis led to decarboxylative fluorination. This operationally simple reaction gave access to tri- and difluoromethylarenes applying a late-stage fluorination strategy. Translation to [(18)F]labeling is demonstrated using [(18)F]Selectfluor bis(triflate), a reagent affording [(18)F]tri- and [(18)F]difluoromethylarenes not within reach with [(18)F]F2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Diazonium Compounds / chemistry*
  • Fluorine Radioisotopes
  • Halogenation
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Hydrocarbons, Fluorinated / chemistry
  • Indicators and Reagents / chemistry*
  • Molecular Structure
  • Silver / chemistry

Substances

  • Diazonium Compounds
  • Fluorine Radioisotopes
  • Hydrocarbons, Fluorinated
  • Indicators and Reagents
  • Silver
  • selectfluor