Michael addition-elimination reactions of chiral enolates with ethyl 3-halopropenoates

Org Lett. 2008 Jan 3;10(1):65-8. doi: 10.1021/ol702632m. Epub 2007 Dec 11.

Abstract

Key dienoic or dienal substructures of cytotoxic macrolides amphidinolide E and dictyostatin have been prepared via a Michael addition (followed by elimination of X-) of chiral enolates on beta-halo derivatives of ethyl acrylate, with full retention of the initial E or Z configuration. Evans oxazolidin-2-ones and our related thiazolidin-2-ones, as well as a fine-tuning of the reaction conditions, have been essential. Many chiral building blocks are accessible from these adducts.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
  • Bridged Bicyclo Compounds, Heterocyclic / chemistry
  • Catalysis
  • Macrolides / chemical synthesis*
  • Macrolides / chemistry
  • Molecular Structure
  • Propane / analogs & derivatives
  • Propane / chemistry*
  • Stereoisomerism

Substances

  • Bridged Bicyclo Compounds, Heterocyclic
  • Macrolides
  • amphidinolide E
  • dictyostatin
  • Propane