Synthesis of substituted quinolines via allylic amination and intramolecular Heck-coupling

Org Biomol Chem. 2014 Dec 7;12(45):9133-8. doi: 10.1039/c4ob01614a.

Abstract

A new catalytic approach for the synthesis of substituted quinolines via C-N and C-C bond formation using 2-haloaryl hydroxylamines and allylic C-H substrates is described. Fe-catalyzed allylic C-H amination followed by Pd-catalyzed intramolecular Heck-coupling and aerobic dehydrogenation deliver the valuable quinoline and naphthyridine heterocycles in good to excellent overall yields. In this process, Pd(OAc)2 plays a dual role in catalyzing Heck coupling as well as aerobic dehydrogenation of dihydroquinolines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allyl Compounds / chemistry*
  • Amination
  • Catalysis
  • Iron / chemistry
  • Molecular Structure
  • Oxidation-Reduction
  • Oxygen / chemistry
  • Palladium / chemistry
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry

Substances

  • Allyl Compounds
  • Quinolines
  • Palladium
  • Iron
  • quinoline
  • Oxygen