Palladium-catalyzed amination of aryl nonaflates

J Org Chem. 2003 Dec 12;68(25):9563-73. doi: 10.1021/jo034962a.

Abstract

The first detailed study of the palladium-catalyzed amination of aryl nonaflates is reported. Use of ligands 2-4 and 6 allows for the catalytic amination of electron-rich and -neutral aryl nonaflates with both primary and secondary amines. With use of Xantphos 5, the catalytic amination of a variety of functionalized aryl nonaflates resulted in excellent yields of anilines; even 2-carboxymethyl aryl nonaflate is effectively coupled with a primary alkylamine. Moderate yields were obtained when coupling halo-aryl nonaflates with a variety of amines, where in most cases the aryl nonaflate reacted in preference to the aryl halide. Overall, aryl nonaflates are an effective alternative to triflates in palladium-catalyzed C-N bond-forming processes due to their increased stability under the reaction conditions.

Publication types

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

MeSH terms

  • Alkylation
  • Amination
  • Amines / chemistry*
  • Aniline Compounds / chemical synthesis*
  • Catalysis
  • Hydrocarbons, Aromatic / chemistry*
  • Ligands
  • Mesylates / chemistry*
  • Molecular Structure
  • Palladium / chemistry*
  • Phenols / chemistry

Substances

  • Amines
  • Aniline Compounds
  • Hydrocarbons, Aromatic
  • Ligands
  • Mesylates
  • Phenols
  • Palladium
  • trifluoromethanesulfonic acid