Preparation of benzotriazine inhibitors of kinases.

Abstract

The title compds. I [each of A and each of B = CH0-1, N, NH, O, S; R0 = H, alkyl; L = a bond, alkyl, alkenyl, alkynyl; R1 = hydroxy, alkoxy, (un)substituted NH2, etc.; R2 = Me, Et, OH, etc.; R3 = H, alkyl, alkoxy, etc.; n = 0-5; with provisions] which are capable of inhibiting kinases, such as members of the Src kinase family, and various other specific receptor and non-receptor kinases, were prepd. E.g., a multi-step synthesis of II, starting from 7-bromobenzo[1,2,4]triazin-3-ylamine-1-oxide and 2,6-dimethylphenylboronic acid, was given. II possesses an IC50 value of 15 nM for Src kinase. Pharmaceutical compns. comprising the compd. I are disclosed. [on SciFinder(R)]