Total synthesis of (+)-boronolide, (+)-deacetylboronolide, and (+)-dideacetylboronolide

J Org Chem. 2003 May 16;68(10):4039-45. doi: 10.1021/jo0269058.

Abstract

Total synthesis of (+)-boronolide, (+)-deacetylboronolide, and (+)-dideacetylboronolide has been achieved from a single intermediate 26, which was synthesized in 11 steps from a d-mannitol-derived intermediate 8 in an overall yield of 10%. The key steps in the synthesis are inversion of a chiral center by taking an advantage of the inherent mechanism involved in the ring closing to an epoxide via intramolecular S(N)2 reaction and lactonization of a diol using Fetizons reagent. The strategy is amenable to preparation of analogues of (+)-boronolide in sufficient amount for further screening of biological activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Combinatorial Chemistry Techniques*
  • Cyclization
  • Indicators and Reagents
  • Lactones / analysis
  • Lactones / chemical synthesis*
  • Lamiaceae / chemistry
  • Mannitol / chemistry*
  • Molecular Structure
  • Nuclear Magnetic Resonance, Biomolecular
  • Stereoisomerism

Substances

  • Indicators and Reagents
  • Lactones
  • boronolide
  • deacetylboronolide
  • dideacetylboronolide
  • Mannitol