Synthesis and biological evaluation of N-arylbenzo [b] thieno [3, 2-d] pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors

Y Loidreau, P Marchand, C Dubouilh-Benard…

Index: Loidreau, Yvonnick; Marchand, Pascal; Dubouilh-Benard, Carole; Nourrisson, Marie-Renee; Duflos, Muriel; Lozach, Olivier; Loaec, Nadege; Meijer, Laurent; Besson, Thierry European Journal of Medicinal Chemistry, 2012 , vol. 58, p. 171 - 183

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Citation Number: 24

Abstract

A useful and rapid access to libraries of N-arylbenzo [b] thieno [3, 2-d] pyrimidin-4-amines and their pyrido and pyrazino analogues was designed and optimized for the first time via microwave-accelerated condensation and Dimroth rearrangement of the starting anilines with N′-(2-cyanoaryl)-N, N-dimethylformimidamides obtained by reaction of thiophene precursors with dimethylformamide dimethylacetal. The inhibitory potency of the final ...