Palladium-catalyzed regioselective benzylation-annulation of pyridine N-oxides with toluene derivatives via multiple C-H bond activations: benzylation versus arylation

Org Lett. 2015 Feb 6;17(3):414-7. doi: 10.1021/ol503238a. Epub 2015 Jan 21.

Abstract

A palladium-catalyzed cross-dehydrogenative coupling (CDC) reaction of pyridine N-oxides with toluenes has been developed that operates under mild conditions. 2-Benzylpyridines can be obtained directly by this method via a CDC reaction between unactivated toluenes and pyridine N-oxides. In addition, azafluorene N-oxides, of value for future medicinal chemistry applications, can be obtained successfully by this procedure via four tandem C-H bond activations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzyl Compounds / chemistry
  • Catalysis
  • Molecular Structure
  • Palladium / chemistry*
  • Pyridines / chemical synthesis
  • Pyridines / chemistry*
  • Stereoisomerism
  • Toluene / chemistry

Substances

  • Benzyl Compounds
  • Pyridines
  • Toluene
  • Palladium
  • pyridine N-oxide
  • 2-benzylpyridine