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METHOD FOR PREPARING (5Z,9Z)-5,9-DOCOSADIENOIC ACID EXHIBITING INHIBITORY ACTION ON HUMAN TOPOISOMERASE I

机译：制备对人拓扑异构酶I具有抑制作用的（5Z，9Z）-5,9-二十二碳二烯酸的方法

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FIELD: chemistry.;SUBSTANCE: invention refers to preparing (5Z,9Z)-5,9-docosadienoic acid of formula (1) exhibiting the inhibitory action on human topoisomerase I. (5Z,9Z)-5,9-Docosadienoic acid is prospective as a drug preparation possessing antitumour, antiviral and antibacterial action. Substance of the method consists in the fact that tetrahydropyrane ester of 5,6-heptadien-1-ole (4) and 1,2-pentadecadiene (5) interacts with Grignard reagent RMgX (R = Me, Et, Pr, Bu, Oct; X = Cl, Br, I) in diethyl ester in the presence of metal Mg (powder) and catalyst titanocendichloride Cp₂TiCl₂, in molar ratio (4):(5) : RMgX : Mg : Cp₂TiCl₂=10:12:(30-50):32:(0.4-0.6), in the argon atmosphere at temperature 0-35°C at atmospheric pressure over 6-10 h; the reaction mixture is processed with 5% aqueous HCl to prepare 2-[(5Z,9Z)-5,9-docosadien-l-yloxy]tetrahydro-2H-pyrane (6), which is oxidised by Jones reagent.;EFFECT: improving the properties.;2 cl, 1 dwg, 1 tbl, 15 ex

机译：技术领域：本发明涉及制备式（1）的（5Z，9Z）-5，9-二十二碳二烯酸<图像文件=“ 00000001.GIF” he =“ 17” imgContent =“ undefined” imgFormat =“表现出对人拓扑异构酶I的抑制作用的GIF“ wi ＝” 154” />。（5Z，9Z）-5，9-二十二碳二烯酸有望作为具有抗肿瘤，抗病毒和抗菌作用的药物制剂。该方法的实质在于5,6-庚二烯-1-烯烃（4）和1,2-十五碳二烯（5）的四氢吡喃酯与格氏试剂RMgX相互作用（R = Me，Et，Pr，Bu，Oct ; X = Cl，Br，I），在金属镁（粉末）和催化剂二茂钛二氯化物Cp _{2 TiCl _{2 存在下的二乙酯中，摩尔比为（4）：（5）：RMgX：Mg：Cp _{2 TiCl _{2 = 10：12：（30-50）：32：（0.4-0.6），在氩气中温度为0-35°C，大气压下持续6-10 h;反应混合物用5％HCl水溶液处理，制备2-[（（5Z，9Z）-5,9-二十二碳杂-1-基氧基]四氢-2H-吡喃（6），其经Jones试剂氧化。改善性能。; 2 cl，1 dwg，1 tbl，15 ex}}}}

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公开/公告号RU2541795C1

专利类型
公开/公告日2015-02-20

原文格式PDF
申请/专利权人 FEDERALNOE GOSUDARSTVENNOE BJUDZHETNOE UCHREZHDENIE NAUKI INSTITUT NEFTEKHIMII I KATALIZA ROSSIJSKOJ AKADEMII NAUK;FEDERALNOE GOSUDARSTVENNOE BJUDZHETNOE UCHREZHDENIE NAUKI INSTITUT BIOKHIMII I GENETIKI UFIMSKOGO NAUCHNOGO TSENTRA ROSSIJSKOJ AKADEMII NAUK;
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申请/专利号RU20130136785
发明设计人 MAKAROV ALEKSEJ ALEKSANDROVICH;DZHEMILEVA LILJA USEINOVNA;MAKAROVA EHLINA KHAMZINOVNA;KHUSNUTDINOVA EHLZA KAMILEVNA;DZHEMILEV USEIN MEMETOVICH;DJAKONOV VLADIMIR ANATOLEVICH;
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申请日2013-08-06
分类号C07C57/03;C07C51/31;A61K31/19;A61P31/00;A61P35/00;
国家 RU
入库时间 2022-08-21 14:56:32

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