Synthesis of (1,2,3-triazol-4-yl)methyl Phosphinates and (1,2,3-Triazol-4-yl)methyl Phosphates by Copper-Catalyzed Azide-Alkyne Cycloaddition

Molecules. 2019 May 31;24(11):2085. doi: 10.3390/molecules24112085.

Abstract

An efficient and practical method was developed for the synthesis of new (1,2,3triazol4yl)methyl phosphinates and (1,2,3-triazol-4-yl)methyl phosphates by the copper(I)catalyzed azide-alkyne cycloaddition (CuAAC) of organic azides and prop-2-ynyl phosphinate or prop-2-ynyl phosphate. The synthesis of (1benzyl-1H-1,2,3-triazol-4-yl)methyl diphenylphosphinate was optimized with respect to the reaction parameters, such as the temperature, reaction time, and catalyst loading. The approach was applied to a range of organic azides, which confirmed the wide scope and the substituent tolerance of the process. The method elaborated represents a novel approach for the synthesis of the target compounds.

Keywords: 1,2,3-triazol; click reaction; copper-catalyzed azide-alkyne cycloaddition; triazolylmethyl phosphate; triazolylmethyl phosphinate.

MeSH terms

  • Alkynes / chemistry*
  • Azides / chemistry*
  • Chemistry Techniques, Synthetic
  • Click Chemistry
  • Copper / chemistry*
  • Cycloaddition Reaction*
  • Magnetic Resonance Spectroscopy
  • Phosphates / chemical synthesis*
  • Phosphates / chemistry
  • Triazoles / chemistry*

Substances

  • Alkynes
  • Azides
  • Phosphates
  • Triazoles
  • Copper