A study of the scope and regioselectivity of the ruthenium-catalyzed [3 + 2]-cycloaddition of azides with internal alkynes

J Org Chem. 2006 Oct 27;71(22):8680-3. doi: 10.1021/jo061688m.

Abstract

[3 + 2]-Cycloadditions of alkyl azides with various unsymmetrical internal alkynes in the presence of CpRuCl(PPh3)2 as catalyst in refluxing benzene have been examined, leading to 1,4,5-trisubstituted-1,2,3-triazoles. Whereas alkyl phenyl and dialkyl acetylenes undergo cycloadditions to afford mixtures of regioisomeric 1,2,3-triazoles, acyl-substituted internal alkynes react with complete regioselectivity. In addition, propargyl alcohols and propargyl amines were found to react with azides to afford single regioisomeric products.

Publication types

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

MeSH terms

  • Alkynes / chemistry*
  • Azides / chemistry*
  • Catalysis
  • Cyclization
  • Molecular Structure
  • Ruthenium / chemistry*
  • Stereoisomerism

Substances

  • Alkynes
  • Azides
  • Ruthenium