Rearrangement of 4-amino-3-halo-pyridines by nucleophilic aromatic substitution

J Org Chem. 2013 Jun 7;78(11):5705-10. doi: 10.1021/jo4003773. Epub 2013 May 23.

Abstract

The reaction of 3-halo-4-aminopyridines with acyl chlorides and triethylamine is described. The pyridin-4-yl α-substituted acetamide products were obtained in moderate to high yields. The presented rearrangement reaction, in which the presumed N-acylated intermediate reacts intramolecularly via nucleophilic aromatic substitution, results in a formal two-carbon insertion.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / chemical synthesis*
  • Acetamides / chemistry
  • Crystallography, X-Ray
  • Ethylamines / chemistry
  • Hydrocarbons, Chlorinated / chemistry*
  • Models, Molecular
  • Molecular Structure
  • Pyridines / chemistry*

Substances

  • Acetamides
  • Ethylamines
  • Hydrocarbons, Chlorinated
  • Pyridines
  • triethylamine