Microwave-assisted or Cu-NHC-catalyzed cycloaddition of azido-disubstituted alkynes: bifurcation of reaction pathways

J Org Chem. 2014 Oct 17;79(20):9818-25. doi: 10.1021/jo5011262. Epub 2014 Oct 6.

Abstract

Microwave irradiation promoted the intramolecular cycloaddition of 2-azidoacetamides derived from α-chiral propargylic amines, affording 1,4,5-trisubstituted triazoles 4 bearing a chiral aminomethyl side chain at C5. In contrast, for the same substrates 3a-k, Cu(I)-NHC complexes catalyzed the intermolecular cycloaddition in an unexpected desilylative fashion, leading to 1,4-disubstituted triazoles 5. This demonstrates that 1-silyl alkynes can be employed as substrates for CuAAC with a suitable coupling partner.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemistry*
  • Amines / chemistry*
  • Azides / chemical synthesis*
  • Azides / chemistry
  • Catalysis
  • Copper / chemistry
  • Cycloaddition Reaction
  • Microwaves
  • Molecular Structure
  • Pargyline / analogs & derivatives
  • Pargyline / chemistry
  • Triazoles / chemistry*

Substances

  • Alkynes
  • Amines
  • Azides
  • Triazoles
  • Copper
  • Pargyline