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Updated: Apr 19, 2026

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
Cu-catalyzed aerobic oxidative cyclization of guanidylpyridines and derivatives
Björn Bartels1, Conor Gordon Bolas, Philipp Cueni
1Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, preclinical CMC, Process Research, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.
Abstract:
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.
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