CAS: 101477-55-8; 1-(Bis(4-Fluorophenyl)Methyl)-4-(2,3,4-Trimethoxybenzyl)Piperazine

该化合物是一种复杂的有机分子,其特征是中管子环,由两个含有氟原子(准位置)的苯基组和一个含有三种甲基氧(2,3,4 的位置)的苯基组替代.具体替代模式允许在管状动物的周围有针对性地具有静态和电子特性.这一结构设计有可能在特定化学环境中促成有针对性的互动或功能,在这些环境中,这种精确的替代组合有利于选择需要调制的氢疏漏或氢联结能力的应用,这些应用需要调制的氢疏漏或氢联结能力,来自芳香环和甲基氧组.

结构式图片

欧盟法规

C&L通报

上下游产品

曲美他嗪 1-(2,3,4-Trimethoxybenzyl)Piperazine 5011-34-7
N-[(2,3,4-Trimethoxyphenyl)Methyl]-N'-Thioformylpiperazine 1172580-43-6
4,4'-二氟苯甲哌嗪 1-(4-Fluorophenyl)Methyl-Piperazine 27469-60-9

合成工艺路线路线简述

    2,3,4-三甲氧基氯苄置于甲醇,三乙胺,Sodium Hydroxide体系中,用 甲醇 用作溶剂,化学反应 16.0H,反应生成洛美利嗪
    参考文献:一种盐酸洛美利嗪的合成方法
    标题:一种盐酸洛美利嗪的合成方法
    摘要:本发明属于药物制备技术领域,涉及一种盐酸洛美利嗪的合成方法.所述合成方法具体步骤为:1)2,3,4‑三甲氧基苯氯苄和1‑boc‑哌嗪在碱性条件下,加热至40oc反应4H,然后加入盐酸得到1‑(2,3,4‑三甲氧基苄基)哌嗪;2)1‑(2,3,4‑三甲氧基苄基)哌嗪和4,4'‑二氟二苯甲基氯在三乙胺的条件下得到1‑(二(4‑氟苯基)甲基)‑4‑(2,3,4‑三甲氧基苄基)哌嗪;3)1‑(二(4‑氟苯基)甲基)‑4‑(2,3,4‑三甲氧基苄基)哌嗪在盐酸的条件下用乙醇和甲基叔丁基醚重结晶得到盐酸洛美利嗪.与现有技术相比,本发明所述的盐酸洛美利嗪的合成方法原料便宜,来源广泛,条件温和,且收率较高,化学纯度较高,处理简单,不需要精制.

    专利信息


    专利号:US-2008287407-A1
    优先权日:2003-12-10
    标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
    发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
    权利人:NITROMED INC
    摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    专利号:CA-2555219-A1
    优先权日:2004-02-03
    标 题 :Synthesis of cyanoimino-benzoimidazoles

    专利号:US-9751877-B2
    优先权日:2012-09-21
    标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
    发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
    权利人:PFIZER
    摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:WO-2005075459-A1
    优先权日:2004-02-03
    标题:Synthesis of cyanoimino-benzoimidazoles

    专利号:EP-1711484-A4
    优先权日:2004-02-03
    标题:SYNTHESIS OF CYANOIMINO-BENZOIMIDAZOLES
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    主要参考文献


    1: Ren Y, Liu T, Song G, Hu Y, Liang J. Determination of lomerizine in human plasma by liquid chromatography/tandem mass spectrometry and its application to a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Feb 1;947-948:96-102. doi: 10.1016/j.jchromb.2013.12.026. Epub 2013 Dec 26. doi: 10.1111/jnc.12738. Epub 2014 May 9. doi: 10.1159/000357209. Epub 2014 Feb 5. doi: 10.1016/j.jns.2013.09.007. Epub 2013 Sep 12. Epub 2013 Apr 2.
    7: Okano M, Thevis M, Sato M, Kageyama S. Analytical detection of trimetazidine produced by metabolic conversion of lomerizine in doping control analysis. Drug Test Anal. 2016 Aug;8(8):869-74. doi: 10.1002/dta.1893. Epub 2015 Nov 11. doi: 10.1007/s11010-011-0913-3. Epub 2011 Jun 9. Japanese. doi: 10.1111/j.1755-5949.2009.00081.x. Epub 2009 Sep 24. Epub 2009 Sep 26. Brain Res Bull. 2010 Mar 16;81(4-5):467-71. doi: 10.1016/j.brainresbull.2009.11.004. Epub 2009 Nov 11. doi: 10.1016/j.expneurol.2008.11.026. Epub 2008 Dec 11.

    合成参考文献


    摘要:Nakayama M, Aihara M, Chen YN, Araie M, Tomita-Yokotani K, Iwashina T. Neuroprotective effects of flavonoids on hypoxia-, glutamate-, and oxidative stress-induced retinal ganglion cell death. Mol Vis. 2011;17():1784–93.
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