Stereoselective synthesis of styrene oxides via a Mitsunobu cyclodehydration

Org Lett. 2001 Aug 9;3(16):2513-5. doi: 10.1021/ol016167u.

Abstract

[reaction: see text] The Mitsunobu cyclodehydration of chiral phenethane-1,2-diols (4), readily accessed from the styrene derivative (5), has been demonstrated to provide the corresponding styrene oxides (2) with high levels of stereoretention (up to 99%). Optimized reaction conditions are described, from which the combination of tricyclohexylphosphine (Chx(3)P) and diisopropylazodicarboxylate (DIAD) in THF and R = EWG provides the best results.

MeSH terms

  • Cyclization
  • Epoxy Compounds / chemical synthesis*
  • Epoxy Compounds / chemistry
  • Epoxy Compounds / pharmacology
  • Indicators and Reagents
  • Neurokinin-1 Receptor Antagonists
  • Phosphines / chemistry
  • Substance P / antagonists & inhibitors

Substances

  • Epoxy Compounds
  • Indicators and Reagents
  • Neurokinin-1 Receptor Antagonists
  • Phosphines
  • Substance P
  • styrene oxide