N??[2??Methyl??5??(triazol??1??yl) phenyl] pyrimidin??2??amine as a Scaffold for the Synthesis of Inhibitors of Bcr??Abl

F Arioli, S Borrelli, F Colombo, F Falchi, I Filippi…

文献索引：Arioli, Federica; Borrelli, Stella; Colombo, Francesco; Falchi, Federico; Filippi, Irene; Crespan, Emmanuele; Naldini, Antonella; Scalia, Giusy; Silvani, Alessandra; Maga, Giovanni; Carraro, Fabio; Botta, Maurizio; Passarella, Daniele ChemMedChem, 2011 , vol. 6, # 11 p. 2009 - 2018

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被引用次数: 24

摘要

Abstract N-[2-Methyl-5-(triazol-1-yl) phenyl] pyrimidin-2-amine derivatives were synthesized and evaluated in vitro for their potential use as inhibitors of Bcr-Abl. The design is based on the bioisosterism between the 1, 2, 3-triazole ring and the amide group. The synthesis involves a copper (I)-catalyzed azide–alkyne cycloaddition (CuAAC) as the key step, with the exclusive production of anti-(1, 4)-triazole derivatives. One of the compounds obtained ...