Cu-catalyzed aerobic oxidative cyclization of guanidylpyridines and derivatives.

J Org Chem

Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, preclinical CMC, Process Research, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.

Published: January 2015

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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http://dx.doi.org/10.1021/jo502536tDOI Listing

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