CAS: 20028-68-6; 2,4,6-Trichloroquinazoline

该化合物是一种氯化的五氯硝基苯衍生物,广泛用作有机合成和制药研究的多用途中间体,其活性三氯甲基组是制作更为复杂的五氯基化合物(包括潜在的药物候选物和农用化学品)的宝贵前体.该化合物在核循环替代反应中表现出高度的反活性,使得在2,4和6个位置能够有选择地发挥功能.在标准储存条件和记录良好的合成路线下,其稳定性进一步提高其在实验室和工业应用中的效用.研究人员在开发具有潜在生物活动的七环化框架时,其作用的价值为2,4,6-三氯五氯基苯基.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    2,2,2-Trifluoro-N-(2-Iodo-4-Chlorophenyl)Acetamide置于potassium Carbonate体系中,用 甲醇,N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 24.5H,反应生成2,4,6-三氯喹唑啉
    参考文献:乙腈介导的 2-乙炔苯胺合成 2,4-二氯喹啉和邻氨基苯甲腈合成 2,4-二氯喹唑啉
    标题:乙腈介导的 2-乙炔苯胺合成 2,4-二氯喹啉和邻氨基苯甲腈合成 2,4-二氯喹唑啉
    摘要:2,4-二氯喹啉和 2,4-二氯喹唑啉分别由 2-乙炔基苯胺和邻氨基苯甲腈合成,在乙腈中使用双光气并在 130 oc 或 150 oc 下加热 12 小时.该反应用于合成 4,6-二氯吡唑并[3,4-D]嘧啶(二氯-9H-异嘌呤).还描述了假定的机制.
    Doi:10.1055/s-2005-922790

    海关参考信息

    专利信息


    专利号:US-6930113-B2
    优先权日:1996-11-01
    标题 :Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
    发明人:GARVEY DAVID S; DE TEJADA INIGO SAENZ; EARL RICHARD A; KHANAPURE SUBHASH P
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, 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 is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, 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 diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).

    专利号:US-2003158184-A1
    优先权日:2001-12-21
    标 题 :Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses
    发明人:GARVEY DAVID S; DE TEJADA INIGO SAENZ
    摘要:The invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or release nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.

    专利号:US-6472425-B1
    优先权日:1997-10-31
    标 题:Methods for treating female sexual dysfunctions
    发明人:GARVEY DAVID S; SAENZ DE TEJADA INIGO
    权利人:NITROMED INC
    摘要:The present invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or releases nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.
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    合成参考文献


    摘要:Kang, F.-A.; Yang, S.-M., Science of Synthesis Knowledge Updates, (2015) 2, 210.
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