Synthesis of 1-Cyanoalkynes and Their Ruthenium(II)-Catalyzed Cycloaddition with Organic Azides to Afford 4-Cyano-1,2,3-triazoles

J Org Chem. 2018 May 4;83(9):5092-5103. doi: 10.1021/acs.joc.8b00424. Epub 2018 Apr 13.

Abstract

A new method to convert terminal alkynes under relatively mild conditions to 1-cyanoalkynes using in situ formed cyanogen is described. 1-Cyanoalkynes have a higher reactivity than terminal alkynes in the ruthenium(II)-catalyzed regiospecific azide-alkyne cycloaddition to afford 4-cyano-1,2,3-triazoles. A mechanistic proposal different from the one that terminal alkynes adopt under the same reaction conditions is proposed. This work provides a new and convenient two-step sequence to prepare 4-cyano-1,2,3-triazoles from terminal alkynes and organic azides.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Alkynes / chemistry*
  • Azides / chemical synthesis*
  • Azides / chemistry*
  • Cycloaddition Reaction
  • Nitriles / chemistry*
  • Ruthenium / chemistry*
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry*

Substances

  • Alkynes
  • Azides
  • Nitriles
  • Triazoles
  • Ruthenium