Azepine synthesis from alkyl azide and propargylic ester via gold catalysis

J Org Chem. 2012 Jun 1;77(11):5184-90. doi: 10.1021/jo300667a. Epub 2012 May 17.

Abstract

An efficient new method was developed to synthesize multisubstituted 4,5-dihydro-1H-azepine derivatives through the gold-catalyzed reaction of two molecules of propargylic esters with one molecule of alkyl azide. It was proposed that vinyl gold carbenoid, in situ generated from propargylic ester through gold-catalyzed 1,2-rearrangement, was trapped by alkyl azide to give vinyl imine intermediate. These, in turn, could undergo a formal [4 + 3] cycloaddition with another molecule of vinyl gold carbenoid to afford the desired azepine product.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Azepines / chemical synthesis*
  • Azepines / chemistry*
  • Azides / chemistry*
  • Catalysis
  • Cyclization
  • Esters
  • Gold / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Azepines
  • Azides
  • Esters
  • Gold