📜4-甲氧基-3-硝基吡啶置于叔丁基过氧化氢,Potassium Tert-Butylate,三氯氧磷体系中,用 四氢呋喃,癸烷,氨,甲苯 作为反应溶剂,化学反应 8.0H,反应生成 2,4-二甲氧基-5-硝基吡啶
参考文献:Discovery Of Aminofurazan-Azabenzimidazoles As Inhibitors Of Rho-Kinase With High Kinase Selectivity And Antihypertensive Activity
标题:Discovery Of Aminofurazan-Azabenzimidazoles As Inhibitors Of Rho-Kinase With High Kinase Selectivity And Antihypertensive Activity
摘要:The Discovery,Proposed Binding Mode,And Optimization Of A Novel Class Of Rho-Kinase Inhibitors Are Presented. Appropriate Substitution On The 6-Position Of The Azabenzimidazole Core Provided Subnanomolar Enzyme Potency In Vitro While Dramatically Improving Selectivity Over A Panel Of Other Kinases. Pharmacokinetic Data Was Obtained For The Most Potent And Selective Examples And One (6N) Has Been Shown To Lower Blood Pressure In A Rat Model Of Hypertension.
DOI:10.1021/jm060873P