CAS: 85386-98-7; 1-(3-Iodopyridin-2-yl)Piperazine

该化合物是具有重要合成用途的多用途七环化合物,具有极佳稳定性,可用于各种有机转化,其主要优势在于能够促进形成C-N债券,使其成为生物活性分子和药物合成中的宝贵中间体.该化合物的活性碘替代成分提供了与多种核素高效结合的机会.

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219635-89-9 34803-66-2 1201643-59-5

上下游产品

piperazine 2-chloro-3-iodopyridine 1-(3-phenyl-2-pyridinyl)piperazine

合成工艺路线路线简述

  • 合成目标产物 1-(3-Iodo-Pyridin-2-yl)-Piperazine 主要起始原料 Piperazine And 2-Chloro-3-Iodopyridine
  • 78607-36-0 = 85386-98-7
    反应条件:1.1 Reagents: N-Methyl-2-Pyrrolidone,Diisopropylethylamine; 60 Min,240 °C
    标题:Design Of Potent,Orally Available Antagonists Of The Transient Receptor Potential Vanilloid 1. Structure-Activity Relationships Of 2-Piperazin-1-Yl-1H-Benzimidazoles
    作者:Ognyanov,Vassil I.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2006 卷标:49(12) 页码:3719-3742
📜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

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✅ COA系统入驻 | 共享模式

合成参考文献


参考文献:10.1021/jm00366a007
摘要:Saari WS, Halczenko W, King SW, Huff JR, Guare JP, Hunt CA, Randall WC, Anderson PS, Lotti VJ, Taylor DA. Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists. J Med Chem. 1983 Dec;26(12):1696–701. doi: 10.1021/jm00366a007.
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