CAS: 58-32-2; 2,2',2'',2'''-((4,8-Di(Piperidin-1-yl)Pyrimido[5,4-D]Pyrimidine-2,6-Diyl)Bis(Azanetriyl))Tetrakis(Ethan-1-Ol)

该化合物是一种有选择性地抑制板块中磷化酶的强效抗塑剂,从而减少了板块的聚集和粘合. 其药理学剖面可以提高功效,同时尽可能减少系统性副作用,从而成为防止不同临床环境血栓事件的有吸引力的选择.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

2,6-dichloro-4,8-bis(piperidin-1-yl)pyrimido[5,4-d]pyrimidine 2,2'-iminobis[ethanol] piperidine 2,4,6,8-Tetrachloro-pyrimido[5,4-d]pyrimidinedipyridamole di-p-toluenesulfonate

合成工艺路线路线简述

    乳清酸置于盐酸,Copper(L) Iodide,氯化亚砜,铜,Caesium Carbonate,Sodium Hydroxide体系中,用 1,4-二氧六环,水,硝基苯 作为反应溶剂,化学反应 45.5H,反应生成 双嘧达莫
    参考文献:一种引入催化剂优化合成双嘧达莫的制备方 法
    标题:一种引入催化剂优化合成双嘧达莫的制备方 法
    摘要:一种引入催化剂优化合成双嘧达莫的制备方法,其属于医药中间体技术领域.该方法在6‑甲基尿嘧啶中甲基氧化为甲酸中,引入co催化体系,将反应产率提高到90%‑95%;在硝基乳清酸中硝基还原为氨基一步中,采用铜粉做催化剂,产率高达85%以上;在取代羟基变为取代氯的步骤中,引入socl2和n,N‑二甲基甲酰胺,降低了环境污染和后处理的难度;在步骤(4)中引入cui催化体系,反应产率达到95%,且操作容易,处理简单.该工艺提高了产率,降低了成本,保证了安全性,节省了能源,符合绿色反应的现代化工生产要求.

    海关参考信息

    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-7122693-B2
    优先权日:1988-04-11
    标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof
    发明人:BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE
    权利人:SHIRE BIOCHEM INC
    摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.

    专利号:US-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    专利号:US-6730790-B2
    优先权日:2002-03-01
    标 题:Chlorinated heterocyclic compounds and methods of synthesis
    发明人:KWIATKOWSKI STEFAN; GOLINSKI MIROSLAW
    权利人:R T ALAMO VENTURES I LLC
    摘要:Compositions of the present invention comprise chlorinated heterocyclic compounds, including racemic monochloroflosequinan, purified enantiomers of monochloroflosequinan and the sulfone derivative of monochloroflosequinan. The methods of the present invention comprise the synthesis of racemic monochloroflosequinan and derivatives thereof, including the sulfone derivative. Intermediates in the synthesis are also provided. The methods further comprise the synthesis of enantiomers of monochloroflosequinan.

    专利号:WO-9925699-A1
    优先权日:1997-11-19
    标 题:Salts of 5,5'-arylidenebisbarbituric and 5,5'-arylidenebis(2-thiobarbituric) acids and 5,5'-arylidenebis(2-thiobarbituric) acids having an antibacterial, anti-chlamydial, antiviral and immuno-modulating activity
    发明人:ASHKINAZI RIMMA ILIINICHNA
    权利人:TETS VIKTOR VENIAMINOICH; ASHKINAZI RIMMA ILIINICHNA
    摘要:The present invention relates to the production of new chemical substances having an anti-microbial, antiviral, immuno-modulating and anti-tumoral activity. This invention more precisely relates to the synthesis of new substances consisting of 5,5'-arylidenebis(2-thiobarbituric) acids and in salts of 5,5'-arylidenebisbarbituric and 5,5'-arylidenebis(2-thiobarbituric) acids of general formula (I) where X is oxygen or sulphur. R1 is hydrogen, a nitro group or an alkoxy group, R2 is hydrogen, a nitro group, an alkoxy group or halogen and Cat+ is a proton or a pyridin- or 2-hydroxyethylammonium-cation. In the preferred embodiments of these substances, the following conditions are observed: X=O, Cat+ is pyridine, R1=H and R2=Cl (I); X=O, Cat+ is pyridine, R1=H and R2=NO2 (II); X=O, Cat+ is H3N+CH2CH2OH, R1=H and R2=NO2 (III); X=S, Cat+ is pyridine, R1=H and R2=Cl (IV); X=S, Cat+ is pyridine, R1=H and R2=OH (V); X=S, Cat+ is pyridine, R1=NO2 and R2=H (VI); X=S, Cat+ is pyridine and R1=R2=MeO (VII); X=O, Cat+ is pyridine, R1=H and R2=Br (VIII); X=O, Cat?+ is H+, R1¿=H and R2=Cl (IX); X=O, Cat?+ is H+, R1¿=H and R2=NO2 (X). This invention also relates to eight synthesis instances of these substances, to three tables representing the chemical and physical characteristics of the substances thus obtained and to the results of five series of experiments. These synthesis instances, tables and results demonstrate the biological properties of these substances on myco-bacteria, on herpes viruses and on Chlamydia trachomatis as well as their interferon-inducing activity and the absence of acute toxicity.

    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.
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    主要参考文献


    1: Ciacciarelli M, Zerbinati C, Violi F, Iuliano L. Dipyridamole: a drug with unrecognized antioxidant activity. Curr Top Med Chem. 2015;15(9):822-9. Review. doi: 10.1016/j.phrs.2014.05.008. Epub 2014 May 24. Review. doi: 10.1177/0036933013496926. Review. doi: 10.1016/j.jclinepi.2012.01.019. Review. doi: 10.1159/000338053. Epub 2012 Aug 9. Review. doi: 10.3310/hta15310. Review. doi: 10.1111/j.1749-6632.2010.05732.x. Review. doi: 10.1111/j.1749-6632.2010.05737.x. Review.
    9: d'Esterre CD, Lee TY. Effect of dipyridamole during acute stroke: exploring antithrombosis and neuroprotective benefits. Ann N Y Acad Sci. 2010 Oct;1207:71-5. doi: 10.1111/j.1749-6632.2010.05801.x. Review. doi: 10.2146/ajhp080645. Review. doi: 10.3233/CH-2010-1274. Review. doi: 10.1002/ccd.22030. Review. doi: 10.1586/14737175.8.11.1661. Review. Review. doi: 10.1161/ATVBAHA.107.160226. Epub 2008 Jan 3. Review.
    16: Halkes PH, Algra A. Anticoagulants, aspirin and dipyridamole in the secondary prevention of cerebral ischaemia: which is the best for which patient? Cerebrovasc Dis. 2007;24 Suppl

    合成参考文献


    参考文献:10.1007/s00259-005-1965-y
    摘要:Schuijf JD, Poldermans D, Shaw LJ, Jukema JW, Lamb HJ, de Roos A, Wijns W, van der Wall EE, Bax JJ. Diagnostic and prognostic value of non-invasive imaging in known or suspected coronary artery disease. European Journal of Nuclear Medicine and Molecular Imaging. 2005 Nov 30;33(1):93–104. doi: 10.1007/s00259-005-1965-y.
    参考文献:10.1161/01.res.26.6.743
    摘要:Afonso S. Inhibition of coronary vasodilating action of dipyridamole and adenosine by aminophylline in the dog. Circ Res. 1970 Jun;26(6):743–52. doi: 10.1161/01.res.26.6.743.
    参考文献:10.1155/2011/687624
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