title: Cu-catalyzed aerobic oxidative cyclization of guanidylpyridines and derivatives.
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.
authors.affiliation: Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, preclinical CMC, Process Research, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.
authors.forename: Björn
authors.initials: B
authors.lastname: Bartels
authors.forename: Conor Gordon
authors.initials: CG
authors.lastname: Bolas
authors.forename: Philipp
authors.initials: P
authors.lastname: Cueni
authors.forename: Serena
authors.initials: S
authors.lastname: Fantasia
authors.forename: Nicolas
authors.initials: N
authors.lastname: Gaeng
authors.forename: Andrada Stefania
authors.initials: AS
authors.lastname: Trita
mesh_terms: D002384:Catalysis; D003300:Copper / Q000737:chemistry*; D003500:Cyclization; D019791:Guanidine / Q000031:analogs & derivatives / Q000737:chemistry*; D010084:Oxidation-Reduction; D011725:Pyridines / Q000737:chemistry*; D011743:Pyrimidines / Q000737:chemistry*; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D011725:Pyridines; D011743:Pyrimidines; D014230:Triazoles; D003300:Copper; D019791:Guanidine