Aryl triflates: useful coupling partners for the direct arylation of heteroaryl derivatives via Pd-catalyzed C-H activation-functionalization

Org Biomol Chem. 2008 Jan 7;6(1):169-74. doi: 10.1039/b715235c. Epub 2007 Nov 21.

Abstract

Aryl triflates were found to be suitable partners for the palladium catalyzed direct arylation of heteroaromatics via C-H activation-functionalization. The reaction conditions and the catalyst have a determining influence on the yields. The system combining PPh3 and Pd(OAc)2 using KOAc as base and DMF as solvent promotes the selective 2- or 5-arylations in moderate to high yields. Several heteroaromatics such as furan, thiophene, thiazole or oxazole derivatives have been employed successfully. The electronic properties of the aryl triflates also have a decisive influence on the yields of the coupling products. Electron-rich aryl triflates gave satisfactory results, whereas the electron-poor ones led to the formation of phenols.

MeSH terms

  • Catalysis
  • Furans / chemistry
  • Mesylates / chemistry*
  • Oxazoles / chemistry
  • Palladium / chemistry*
  • Thiazoles / chemistry
  • Thiophenes / chemistry

Substances

  • Furans
  • Mesylates
  • Oxazoles
  • Thiazoles
  • Thiophenes
  • methanesulfonic acid
  • Palladium
  • furan