Selective C-arylation of free (NH)-heteroarenes via catalytic C-H bond functionalization

J Am Chem Soc. 2003 May 7;125(18):5274-5. doi: 10.1021/ja034848+.

Abstract

A new system for palladium-catalyzed arylation of a broad spectrum of free (NH)-heteroarenes has been developed (indole, pyrrole, pyrazole, 2-phenylimidazole, imidazole, benzimidazole, and purine). Remarkable selectivity has been achieved in the presence of MgO base, providing single C-arylation products, while no N-arylation and no bis-arylation products have been detected. In the case of free imidazole, exclusive C-4 arylation may be switched to exclusive 2-arylation by the addition of CuI to the Pd/Ph3P/MgO system. When free aryl-(NH)-azoles are desired, direct arylation eliminates three steps in comparison to standard methods, including N-protection, stoichiometric metalation or halogenation, and N-deprotection.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.
  • Retracted Publication

MeSH terms

  • Azoles / chemical synthesis
  • Azoles / chemistry*
  • Catalysis
  • Hydrocarbons, Aromatic / chemical synthesis
  • Hydrocarbons, Aromatic / chemistry*
  • Magnesium Oxide / chemistry
  • Palladium / chemistry

Substances

  • Azoles
  • Hydrocarbons, Aromatic
  • Magnesium Oxide
  • Palladium