A two-directional approach to enantiopure 1,4-difluoro-cyclohexenes: synthesis of difluorinated cyclitol analogues

Org Lett. 2008 Oct 2;10(19):4263-6. doi: 10.1021/ol8017402. Epub 2008 Sep 3.

Abstract

Enantiopure 1,4-difluoro-cyclohexenes were prepared from readily available acetonide-protected (3 S,4 S)-hexa-1,5-diene-3,4-diol. In a two-directional mode, a double cross-metathesis reaction using allyltrimethylsilane as the olefinic partner, followed by electrophilic fluorination, afforded diastereomeric acetonide-protected 3,6-difluoro-octa-1,7-diene-4,5-diols. These dienes were found to be suitable substrates for ring-closing metathesis, delivering cyclohexenes featuring fluorine atoms on the two allylic positions flanking the double bond. Upon dihydroxylation, novel difluorinated cyclitol analogues were formed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclitols / chemical synthesis*
  • Cyclitols / chemistry
  • Cyclohexenes / chemical synthesis*
  • Cyclohexenes / chemistry
  • Fluorine / chemistry*
  • Stereoisomerism

Substances

  • Cyclitols
  • Cyclohexenes
  • Fluorine