Photoassisted diversity-oriented synthesis: accessing 2,6-epoxyazocane (oxamorphan) cores

J Org Chem. 2014 Nov 21;79(22):10956-71. doi: 10.1021/jo5019848. Epub 2014 Nov 5.

Abstract

The modular synthesis of photoprecursors and their photoinduced cyclization into substituted 1-benzazocanes of two distinct topologies is described. The key step producing an extended polyheterocyclic system involves the photogeneration of azaxylylenes and their subsequent intramolecular cycloaddition with furan-containing pendants tethered either via the aniline nitrogen or through the carbonyl group containing arm. The primary photoproducts-secondary or tertiary anilines which are not acylated at the nitrogen atom-undergo facile acid-catalyzed or spontaneous ring-opening-ring-closing rearrangement to yield fused polyheterocyclic structures possessing a 2,6-epoxyazocane (or oxamorphan) core.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Cycloaddition Reaction
  • Cycloheptanes / chemical synthesis*
  • Cycloheptanes / chemistry
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / chemistry
  • Molecular Structure
  • Photochemical Processes
  • Stereoisomerism

Substances

  • 2,6-epoxyazocane
  • Cycloheptanes
  • Heterocyclic Compounds