CAS: 60547-97-9; 6,7-Dimethoxy-2-(Piperazin-1-yl)Quinazolin-4-Amine

该化合物是五甲酰衍生物,具有显著的药用化学和药物研究潜力,其结构在四级的2位置和氨基功能上有一个管道状替代体,在六位和七位位置上还有角状氧基组,这增强了其对某些生物目标的结合性和选择性.这一复合物对于它作为流动酶抑制剂的脚手架的作用,特别是在发展针对癌症和炎性疾病的治疗器方面,具有意义.其定义明确的合成途径和可变核心结构使它成为进一步衍生的多用途中间体,有助于探索药物发现中的结构性活动关系.

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CAS号110-85-0 哌嗪 | CAS号23680-84-4 4-氨基-2-氯-6, 7-二氧基喹唑啉 | CAS号107021-36-3 普拉佐宾德 | CAS号74191-85-8 多沙唑嗪 | CAS号19237-84-4 盐酸哌唑嗪 | CAS号19216-56-9 哌唑嗪 | CAS号79221-43-5 1-Piperazinecar...

合成工艺路线路线简述

    2-氯-4-氨基-6,7-二甲氧基喹唑啉置于macroporous Polymer-Supported Carbonate,Macroporous Polymer-Supported-Tsoh体系中,用 二氯甲烷,二甲基亚砜 作为反应溶剂,化学反应生成 2-哌嗪基-4-氨基-6,7-二甲氧基喹唑啉
    参考文献:Parallel Synthesis Of N-Arylpiperazines Using Polymer-Assisted Reactions
    标题:Parallel Synthesis Of N-Arylpiperazines Using Polymer-Assisted Reactions
    摘要:A Series Of N-Arylpiperazines Were Prepared In A Parallel Fashion Using Palladium-Catalyzed Cross-Coupling,Or Nucleophilic Aromatic Displacement Chemistries,And Polymer-Assisted Sequestration And Purification Techniques As Key Steps. (C) 2006 Elsevier Ltd. All Rights Reserved.
    DOI:10.1016/j.Tetlet.2006.02.047

    海关参考信息

    专利信息


    专利号:US-6469065-B1
    优先权日:1996-02-02
    标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
    发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

    专利号:US-2005187222-A1
    优先权日:1996-02-02
    标题:Nitrosated and nitrosylated alpha-adrenergic receptor antagonist compounds
    发明人:GARVEY DAVID S; DE TEJADA INIGO S; GASTON RICKY D; KHANAPURE SUBHASH P; SHELEKHIN TATIANA E; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.
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    主要参考文献


    1: Zhou G, Wang L, Ma Y, Wang L, Zhang Y, Jiang W. Synthesis of a quinazoline derivative: a new α₁-adrenoceptor ligand for conjugation to quantum dots to study α₁-adrenoceptors in living cells. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5905-9. doi: 10.1016/j.bmcl.2011.07.122. Epub 2011 Aug 10. Russian.

    合成参考文献


    参考文献:10.1021/jm9805337
    摘要:Leonardi A, Motta G, Boi C, Testa R, Poggesi E, De Benedetti PG, Menziani MC. Synthesis, pharmacological evaluation, and structure-activity relationship and quantitative structure-activity relationship studies on novel derivatives of 2,4-diamino-6,7-dimethoxyquinazoline alpha1-adrenoceptor antagonists. J Med Chem. 1999 Feb 11;42(3):427–37. doi: 10.1021/jm9805337.
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