A highly efficient tandem [3 + 2] "click" cycloaddition/6-exo-cyclization strategy for the construction of triazole fused pyrazines

Abstract

The pharmaceutically important tetrahydro-[1,2,3]triazolopyrazine heterocyclic architecture has been synthesized via a concise tandem "click"/6-exo-dig cyclization strategy in mixed aqueous-organic media. The generality of this mild method was expanded to various amino acid based substrates. The scopes and limitations of this method are discussed in the paper.