Total synthesis of epothilone E and related side-chain modified analogues via a Stille coupling based strategy

Bioorg Med Chem. 1999 May;7(5):665-97. doi: 10.1016/s0968-0896(98)00153-9.

Abstract

A Stille coupling strategy has been utilized to complete a total synthesis of epothilone E from vinyl iodide 7 and thiazole-stannane 8h. The central core fragment 7 and its trans-isomer 11 were prepared from triene 15 using ring-closing metathesis (RCM), and were subsequently coupled to a variety of alternative stannanes to provide a library of epothilone analogues 18a-o and 19a-o. The Stille coupling approach was then used to prepare epothilone B analogues from the key macrolactone intermediate 24 which was itself synthesized by a macrolactonization based strategy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Chromatography, Thin Layer
  • Epothilones*
  • Epoxy Compounds / chemical synthesis*
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Models, Chemical
  • Thiazoles / chemical synthesis*

Substances

  • Epothilones
  • Epoxy Compounds
  • Thiazoles
  • epothilone E
  • epothilone B