Synthesis of γ-monofluorinated goniothalamin analogues via regio- and stereoselective ring-opening hydrofluorination of epoxide

J Org Chem. 2011 Aug 19;76(16):6525-33. doi: 10.1021/jo200611w. Epub 2011 Jul 19.

Abstract

A stereoselective synthesis of the biologically interesting γ-monofluorinated goniothalamin analogue 2a was described. The features of the synthesis included regioselective reduction of the unprotected hydroxypropynyl moiety of compound 10 by Red-Al, asymmetric Sharpless epoxidation of allyl alcohol 11, and regio- and stereoselective ring-opening hydrofluorination of the hydroxypropynyl epoxide 14 with Et(3)N·3HF in high ee and dr. The chiral hydroxypropynyl fluorohydrin 15 was used as a valuable building block for preparation of a range of γ-monofluorinated α,β-unsaturated δ-lactones.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Epoxy Compounds / chemistry*
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Hydrocarbons, Fluorinated / chemistry
  • Lactones / chemical synthesis
  • Lactones / chemistry*
  • Molecular Structure
  • Pyrones / chemical synthesis*
  • Pyrones / chemistry
  • Stereoisomerism

Substances

  • Epoxy Compounds
  • Hydrocarbons, Fluorinated
  • Lactones
  • Pyrones
  • goniothalamin