Thermolysis of isomigrastatin and its congeners via [3,3]-sigmatropic rearrangement: a new route to the synthesis of migrastatin and its analogues

Org Lett. 2006 Dec 7;8(25):5865-8. doi: 10.1021/ol062470p.

Abstract

Thermolysis of isomigrastatin (1) under neat heating conditions afforded migrastatin (1a). The reaction is proposed to proceed via a concerted [3,3]-sigmatropic rearrangement by which ring expansion is achieved regio- and enantiospecifically. The general applicability of this reaction was demonstrated with six additional isomigrastatin congeners (3-8), providing a new route to the synthesis of migrastatin analogues (3a-8a). [reaction: see text]

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Chromatography, High Pressure Liquid
  • Hot Temperature
  • Isomerism
  • Lactones / chemical synthesis*
  • Lactones / chemistry*
  • Macrolides / chemical synthesis*
  • Macrolides / chemistry*
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Piperidones / chemical synthesis*
  • Piperidones / chemistry*
  • Stereoisomerism

Substances

  • Lactones
  • Macrolides
  • Piperidones
  • isomigrastatin
  • migrastatin