2-溴-3-氨基-6-甲基吡啶置于盐酸,Sodium Nitrite,Hexafluorophosphoric Acid体系中,用 水 用作溶剂,化学反应 0.17H,以38%的收率获得2-溴-3-氟-6-甲基吡啶
参考文献:Synthesis And Biological Evaluation Of 5-(Fluoro-Substituted-6-Methylpyridin-2-yl)-4-([1,2,4]Triazolo[1,5-A]Pyridin-6-yl)Imidazoles As Inhibitors Of Transforming Growth Factor-β Type I Receptor Kinase
标题:Synthesis And Biological Evaluation Of 5-(Fluoro-Substituted-6-Methylpyridin-2-yl)-4-([1,2,4]Triazolo[1,5-A]Pyridin-6-yl)Imidazoles As Inhibitors Of Transforming Growth Factor-β Type I Receptor Kinase
摘要:To Further Optimize A Clinical Candidate 5 (Ew-7197),A Series Of 5-(3-,4-,Or 5-Fluoro-Substituted-6-Methylpyridin-2-yl)-4-([1,2,4]Triazolo[1,5-A]Pyridin-6-yl)Imidazoles 19A-L Have Been Synthesized And Evaluated For Their Tgf-Beta Type I Receptor Kinase (Alk5) And P38 Alpha Map Kinase Inhibitory Activity In An Enzyme Assay. The 5-(5-Fluoro-Substituted-6-Methylpyridin-2-yl)-4-([1,2,4] Triazolo[1,5-A] Pyridin-6-yl)Imidazoles 19H-1 Displayed The Similar Level Of Potency To That Of 5 Against Both Alk5 (Ic50 = 7.68-13.70 Nm) And P38 Alpha Map Kinase (Ic50 = 1240-3370 Nm). Among Them,19J Inhibited Alk5 With Ic50 Value Of 7.68 Nm In A Kinase Assay And Displayed 82% Inhibition At 100 Nm In A Luciferase Reporter Assay. (C) 2015 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2015.09.058