Synthesis and oxidative cyclization of 2-arylhydrazono-2-cyanoacetamidines to 5-amino-2-aryl-2H-[1,2,3]triazole-4-carbonitrile

Abstract

A general and convenient method for the synthesis of 2-arylhydrazono-2- cyanoacetamidines, containing either a cytisine or tryptamine moiety, or other secondary and primary amines was elaborated. A series of 5-amino-2-aryl-2H-[1,2, 3]-triazole-4-carbonitriles was successfully prepared by oxidation of these amidines with copper acetate in pyridine. The screening of the biological activity of the synthesized triazoles and amidines have shown that, some of these compounds possess fungicidal activity at concentrations of 50 μg/mL against some fungi tested. © ARKAT USA, Inc.