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Synlett 1997; 1997(2): 193-195
DOI: 10.1055/s-1997-739
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The Synthesis of Novel Trans-Oxabicyclo[3,3,0]octane Systems as Potential Inhibitors of HIV Protease

Mikael E. Mahler, Michael J. Palmer*
  • *Discovery Chemistry, Pfizer Central Research, Sandwich, Kent, England, CT13 9NJ
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Publication Date:
31 December 2000 (online)

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The novel trans-3-oxabicyclo[3,3,0]octan-7-one system has been prepared by intramolecular ring closure of the corresponding cyclopentane diol. Peralkylation and benzylidene substitution of the octanone has allowed the preparation of tetra-alkylated potential inhibitors of HIV protease. Weak activity against HIV protease (IC50's 70-100μM) was observed.

trans-3-oxabicyclo[3,3,0]octan-7-ol derivatives - intramolecular ring closure - peralkylation - differential substitution