Desymmetrization of a centrosymmetric diepoxide: efficient synthesis of a key intermediate in a total synthesis of hemibrevetoxin B

J Org Chem. 2003 Feb 7;68(3):747-53. doi: 10.1021/jo026456b.

Abstract

The preparation of an established intermediate in a total synthesis of hemibrevetoxin B is described. The acid-catalyzed cyclization of trans-4,5-epoxyoctane-2,7-dione exhibited a valuable mixture of kinetic and thermodynamic control: stereospecific epoxide opening was followed by equilibration of the products to provide the required trans-fused octahydropyrano[3,2-b]pyran ring system. Two-directional elaboration, by acetal substitution, ozonolysis, and sulfur ylide-mediated epoxidation, provided a centrosymmetric diepoxide. The key step of the synthesis was the first desymmetrization of a centrosymmetric molecule in natural product synthesis: Jacobsen asymmetric epoxide hydrolysis and acetonization provided the known synthetic intermediate in 97% yield and >95% ee over two steps. The exploitation of the center of symmetry of the AB ring system of the natural product contributed greatly to the efficiency (eight steps, 34% overall yield) of the synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Factors / analysis
  • Biological Factors / chemical synthesis
  • Catalysis
  • Chemistry, Organic / methods*
  • Cyclization
  • Heterocyclic Compounds, 4 or More Rings / analysis
  • Heterocyclic Compounds, 4 or More Rings / chemical synthesis*
  • Nuclear Magnetic Resonance, Biomolecular
  • Stereoisomerism

Substances

  • Biological Factors
  • Heterocyclic Compounds, 4 or More Rings
  • hemibrevetoxin B