CAS: 84951-44-0; 2-Piperazin-1-Ylnicotinonitrile

该化合物是一种合成有机化合物,具有巨大的药用化学潜力,该化合物的特点是一个管子环和一个丙烯-3-碳三律核心,在药物设计方面提供了多种用途,其结构特征具有显著的优势,包括溶性得到改善,而且有可能加强药物目标相互作用,使其成为合成新药的宝贵中间体.

结构式图片

相似化合物

1185307-06-5 440100-15-2 374063-94-2

物理性质

MSDS等安全信息

欧盟法规

C&L通报

上下游产品

piperazine 2-chloro-3-pyridinecarbonitrile 2-(piperazin-1-yl)nicotinaldehyde 4-(3-Cyano-2-pyridinyl)-N-[4-(isopropyl)phenyl]-1-piperazinecarboxamide 2-[4-(3-cyano-2-pyridinyl)-1-piperazinyl]-N-(3-methylphenyl)acetamide

合成工艺路线路线简述

  • 6602-54-6 = 84951-44-0
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane; 4 - 5 H,Rt -> 110 °C
    标题:Structure Guided Design Of Potential Inhibitors Of Human Calcium-Calmodulin Dependent Protein Kinase Iv Containing Pyrimidine Scaffold
    作者:Naz,Huma; Jameel,Ehtesham; Hoda,Nasimul; Shandilya,Ashutosh; Khan,Parvez; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2016 卷标:26(3) 页码:782-788]

    6602-54-6 = 84951-44-0
    反应条件:1.1 Solvents: Methanol; Reflux
    标题:A Multifunctional Therapeutic Approach: Synthesis,Biological Evaluation,Crystal Structure And Molecular Docking Of Diversified 1H-Pyrazolo[3,4-B]Pyridine Derivatives Against Alzheimer'S Disease
    作者:Umar,Tarana; Shalini,Shruti; Raza,Kausar Md; Gusain,Siddharth; Kumar,Jitendra; Et Al
    参考文献:European Journal Of Medicinal Chemistry 日期:2019 卷标:175 页码:2-19]

    6602-54-6 = 84951-44-0
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane; 8 - 9 H,100 °C
    标题:Pyrimidine-Triazolopyrimidine And Pyrimidine-Pyridine Hybrids As Potential Acetylcholinesterase Inhibitors For Alzheimer'S Disease
    作者:Kumar,Jitendra; Gill,Asim; Shaikh,Marziya; Singh,Anju; Shandilya,Ashutosh; Et Al
    参考文献:Chemistryselect 日期:2018 卷标:3(2) 页码:736-747]

    6602-54-6 = 84951-44-0
    反应条件:1.1 Solvents: Ethanol-D; 16 H,Reflux
    标题:Novel D2/5-Ht Receptor Modulators Related To Cariprazine With Potential Implication To Schizophrenia Treatment
    作者:Juza,Radomir; Vojtechova,Iveta; Stefkova-Mazochova,Kristyna; Dehaen,Wim; Petrasek,Tomas; Et Al
    参考文献:European Journal Of Medicinal Chemistry 日期:2022 卷标:232]

    6602-54-6 = 84951-44-0
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane; 8 - 9 H,100 °C
    标题:Synthesis And Screening Of Triazolopyrimidine Scaffold As Multi-Functional Agents For Alzheimer'S Disease Therapies
    作者:Kumar,Jitendra; Meena,Poonam; Singh,Anju; Jameel,Ehtesham; Maqbool,Mudasir; Et Al
    参考文献:European Journal Of Medicinal Chemistry 日期:2016 卷标:119 页码:260-277]

    6602-54-6 = 84951-44-0
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane; 3 - 4 H,Reflux
    标题:Development Of Cyanopyridine-Triazine Hybrids As Lead Multitarget Anti-Alzheimer Agents
    作者:Maqbool,Mudasir; Manral,Apra; Jameel,Ehtesham; Kumar,Jitendra; Saini,Vikas; Et Al
    参考文献:Bioorganic & Medicinal Chemistry 日期:2016 卷标:24(12) 页码:2777-2788
📜哌嗪,2-氯-3-氰基吡啶 以 甲醇 作为反应溶剂,化学反应生成 2-哌嗪烟酰腈
参考文献:多功能治疗方法:多种抗阿尔茨海默氏病的1H-吡唑并[3,4-B]吡啶衍生物的合成,生物学评估,晶体结构和分子对接
标题:多功能治疗方法:多种抗阿尔茨海默氏病的1H-吡唑并[3,4-B]吡啶衍生物的合成,生物学评估,晶体结构和分子对接
摘要:2-(哌嗪-1-基)n-(1H-吡唑并[3,4-B]吡啶-3-基)乙酰胺被描述为一类新型的选择性和有效的乙酰胆碱酯酶(ache)抑制剂和淀粉样β聚集抑制剂.通过h 1 NMR,C 13 NMR,质谱和单晶x射线衍射研究证明了合成化合物(p1 P9)的形成.评价了所有化合物的乙酰胆碱酯酶和丁酰胆碱酯酶的抑制活性,自身介导的aβ聚集的抑制和cu(II)介导的aβ聚集的抑制.而且,进行的对接研究与体外结果一致.衍生物中最有效的分子表现出出色的抗ache活性(ic50 = 4.8 Nm).p3的动力学研究表明它是一种混合型抑制剂.体外研究表明,所有化合物均具有抑制自身诱导的β-淀粉样蛋白(aβ)聚集的能力,最高抑制率为81.65%.的效力p1和p3抑制自诱导aβ 1-42聚集通过tem分析确定.还评估了化合物的aβ分解,抗氧化,金属螯合活性.
DOI:10.1016/j.Ejmech.2019.04.038

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专利信息


专利号:US-9951088-B2
优先权日:2012-05-09
标题 :D2 receptor modulators and methods of use thereof in the treatment of diseases and disorders
发明人：JONES PHILIP G; LEW ROBERT; SPEAR KERRY L; XIE LINGHONG
权利人:SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.

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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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