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.