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
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.
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.