A new method for the straightforward synthesis of 2-amino-[1,2,4]triazolo[1,5-a]pyridines and derivatives is presented. The target products are synthesized in high yields from guanidylpyridines and analogues via copper-catalyzed N-N coupling. The present methodology shows a wide scope, tolerating not only different substituents on the pyridine ring but also different heterocylic rings such as pyrazines, pyrimidines, and pyridazines.

amino-[1,2,4]triazolo[1,5-a]pyridine structures and analogues such as (X) and (XII). A wide scope is possible where a broad spectrum of substrates is tolerated. Whereas the chloro-substituted substrates (III) react without any problem, no conversion is observed with the bromo compounds. If an iodine substituent is present [cf. (V)], CuI has to be used instead of CuBr. -(BARTELS*, B.; BOLAS, C. G.; CUENI, P.; FANTASIA, S.; GAENG, N.; TRITA, A. S.; J.