The rearrangement of 2,3-epoxysulfonates and its application to natural products syntheses: formal synthesis of (-)-aphanorphine and total syntheses of (-)-alpha-herbertenol and (-)-herbertenediol

J Org Chem. 2003 Jul 25;68(15):5917-24. doi: 10.1021/jo034573g.

Abstract

The Lewis acid treatment of 2,3-epoxysulfonates with 2,3-dialkyl substituents or 2-alkyl-3-aryl substituents produced the rearrangement products via C3-cleavage of the oxirane ring in high yields. On the other hand, 2-aryl-3-alkyl-2,3-epoxysulfonates produced the products via C2-cleavage of the oxirane ring. The sulfonyloxy groups of the alpha-sulfonyloxy ketones, having a chiral benzylic quaternary carbon center obtained by the rearrangement of 2-alkyl-3-aryl-2,3-epoxysulfonates, were reductively eliminated to give the ketones with a chiral benzylic quaternary carbon center. The method was applied to the formal synthesis of (-)-aphanorphine and total syntheses of (-)-alpha-herbertenol and (-)-herbertenediol.

MeSH terms

  • Alkaloids / chemical synthesis
  • Biological Products / chemical synthesis*
  • Bridged-Ring Compounds / chemical synthesis*
  • Cyclopentanes / chemical synthesis*
  • Cyclopentanes / chemistry
  • Epoxy Compounds / chemistry*
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Molecular Conformation
  • Phenols / chemical synthesis*
  • Phenols / chemistry
  • Pyrroles / chemical synthesis*
  • Sulfonic Acids / chemistry*

Substances

  • Alkaloids
  • Biological Products
  • Bridged-Ring Compounds
  • Cyclopentanes
  • Epoxy Compounds
  • Indicators and Reagents
  • Phenols
  • Pyrroles
  • Sulfonic Acids
  • aphanorphine
  • herbertenediol
  • herbertenol