Synthesis of aza-, oxa-, and thiabicyclo[3.1.0]hexane heterocycles from a common synthetic intermediate

Org Lett. 2005 Jun 23;7(13):2627-30. doi: 10.1021/ol050730h.

Abstract

[reaction: see text] An efficient and stereospecific approach to the synthesis of structurally constrained aza-, oxa-, and thiabicyclo[3.1.0]hexane heterocycles has been achieved through application of the intramolecular cyclopropanation reaction of diazoacetates. The various constrained heterocycles (X = N, O, or S) are conveniently prepared from a common diol intermediate accessible from readily available cinnamyl alcohols. Application of the methodology to the synthesis of conformationally constrained oxazolidinone antibacterials is also discussed.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Aza Compounds / chemical synthesis
  • Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
  • Catalysis
  • Molecular Structure
  • Oxazolidinones / chemical synthesis
  • Oxazolidinones / pharmacology
  • Oxygen / chemistry
  • Propanols / chemistry*
  • Sulfur Compounds / chemical synthesis

Substances

  • Anti-Bacterial Agents
  • Aza Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Oxazolidinones
  • Propanols
  • Sulfur Compounds
  • Oxygen
  • cinnamyl alcohol