One-Pot Synthesis of 5-Amino-2,5-dihydro-1-benzoxepines: Access to Pharmacologically Active Heterocyclic Scaffolds

J Org Chem. 2015 May 1;80(9):4683-96. doi: 10.1021/acs.joc.5b00583. Epub 2015 Apr 13.

Abstract

A one-pot multibond-forming process involving a thermally mediated Overman rearrangement and a ring closing metathesis reaction of allylic trichloroacetimidates bearing a 2-allyloxyaryl group has been developed for the synthesis of 5-amino-substituted 2,5-dihydro-1-benzoxepines. Chemoselective reduction and functionalization of these compounds allowed access to a range of pharmacologically active 5-amino-2,3,4,5-tetrahydro-1-benzoxepine scaffolds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzoxepins / chemical synthesis*
  • Benzoxepins / chemistry
  • Cyclization
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / chemistry
  • Molecular Structure

Substances

  • 5-amino-2,5-dihydro-1-benzoxepine
  • Benzoxepins
  • Heterocyclic Compounds