2-甲氧基-4-甲基吡啶置于disodium Hydrogenphosphate,溴体系中,用 水 用作溶剂,化学反应 4.25H,以15.4 G的收率获得2-甲氧基-5-溴-6-甲基吡啶
参考文献:Synthesis And Structure−activity Relationships Of 8-(Pyrid-3-yl)Pyrazolo[1,5-A]-1,3,5-Triazines: Potent,Orally Bioavailable Corticotropin Releasing Factor Receptor-1 (Crf1) Antagonists
标题:Synthesis And Structure−activity Relationships Of 8-(Pyrid-3-yl)Pyrazolo[1,5-A]-1,3,5-Triazines: Potent,Orally Bioavailable Corticotropin Releasing Factor Receptor-1 (Crf1) Antagonists
摘要:This Report Describes The Syntheses And Structure-Activity Relationships Of 8-(Substituted Pyridyl)Pyrazolo[1,5-A]-1,3,5-Triazine Corticotropin Releasing Factor Receptor-1 (Crf1) Receptor Antagonists. These Crf1 Receptor Antagonists May Be Potential Anxiolytic Or Antidepressant Drugs. This Research Resulted In The Discovery Of Compound 13-15,Which Is A Potent,Selective Crf1 Antagonist (Hcrf(1) Ic50 = 6.1 +/-0.6 Nm) With Weak Affinity For The Crf-Binding Protein And Biogenic Amine Receptors. This Compound Also Has A Good Pharmacokinetic Profile In Dogs. Analogue 13-15 Is Orally Effective In Two Rat Models Of Anxiety: The Defensive Withdrawal (Situational Anxiety) Model And The Elevated Plus Maze Test. Analogue 13-15 Has Been Advanced To Clinical Trials.
Doi:10.1021/jm900025H