Synthesis of (±)-4,5-dia-Parthenolide, an Unnatural Parthenolide Stereoisomer

J Org Chem. 2016 Nov 18;81(22):11009-11016. doi: 10.1021/acs.joc.6b01985. Epub 2016 Oct 21.

Abstract

A short total synthesis of the novel unnatural parthenolide diastereomer (±)-4,5-dia-parthenolide was accomplished in 13 steps and an overall yield of 1.75% starting from commercially available (E,E)-farnesol. The challenging isopropenyl side chain oxidation was regioselectively achieved via a newly developed stepwise dihydroxylation procedure, employing a Bartlett-Smith iodocarbonate cyclization followed by iodide substitution and catalytic transesterification.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Carbon-13 Magnetic Resonance Spectroscopy
  • Catalysis
  • Chromatography, High Pressure Liquid
  • Cyclization
  • Esterification
  • Hydroxylation
  • Proton Magnetic Resonance Spectroscopy
  • Sesquiterpenes / chemical synthesis*
  • Sesquiterpenes / chemistry
  • Spectrometry, Mass, Electrospray Ionization
  • Stereoisomerism

Substances

  • Sesquiterpenes
  • parthenolide