Facile synthesis of 3,5-diaryl-1,2,4-triazoles via copper-catalyzed domino nucleophilic substitution/oxidative cyclization using amidines or imidates as substrates

Kavitha Sudheendran, Dietmar Schmidt, Wolfgang Frey, Jürgen Conrad, Uwe Beifuss

Research output: Contribution to journalArticlepeer-review

33 Scopus citations

Abstract

Two methods for the synthesis of 3,5-diaryl-1,2,4-triazoles, both domino reactions, are reported. The first procedure, the Cu(OTf)2-catalyzed reaction between two amidines using NaHCO3 as a base, 1,10-phenanthroline as an additive and K3[Fe(CN)6]/ atmospheric oxygen as the oxidant, delivers 3,5-diaryl-1,2,4-triazoles with yields up to 68%. The second procedure for the synthesis of 3,5-diaryl-1,2,4- triazoles with yields up to 64% rests on the Cu(OTf)2-catalyzed reaction between two imidates and ammonium carbonate. This method features the formation of three bonds in a single synthetic step.

Original languageEnglish
Pages (from-to)1635-1645
Number of pages11
JournalTetrahedron
Volume70
Issue number8
DOIs
StatePublished - 25 Feb 2014
Externally publishedYes

Keywords

  • 1,2,4-Triazole
  • Amidine
  • Catalysis
  • Copper
  • Imidate

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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