📜哌嗪,2-氯-3-碘吡啶 以 正丁醇 作为反应溶剂,化学反应 18.0H,反应生成 1-(3-碘-2-吡啶基)哌嗪
参考文献:Pyridinylpiperazines,A New Class Of Selective .Alpha.2-Adrenoceptor Antagonists
标题:Pyridinylpiperazines,A New Class Of Selective .Alpha.2-Adrenoceptor Antagonists
摘要:A Series Of 1-(2-Pyridinyl)Piperazine Derivatives Was Synthesized And Evaluated For Adrenergic Activity. In Vitro Activity Was Assessed Through The Antagonism Of Clonidine'S Effect In The Rat,Isolated,Field-Stimulated Vas Deferens And By The Displacement Of [3H]Clonidine From Membrane Binding Sites Of Calf Cerebral Cortex. Antagonism Of Clonidine-Induced Mydriasis In The Rat Was Used As An In Vivo Assay. Several Members Of The Series Proved To Be Potent,Selective Alpha 2-Adrenoceptor Antagonists. 1-(3-Fluoro-2-Pyridinyl)Piperazine Was More Potent Than Either Yohimbine Or Rauwolscine In Displacement Of [3H]Clonidine And Had A Higher Affinity For This Binding Site (Alpha 2) Than For The [3H]Prazosin Site (Alpha 1). In Vivo,The 3-F Derivative Was More Potent Than The Reference Standards In Reversing Clonidine-Induced Mydriasis. None Of The Members Of This Series Was More Selective Or Potent Than Rauwolscine In Antagonizing Clonidine In The Rat Vas Deferens.
DOI:10.1021/jm00366A007