CAS: 2022-78-8; 5-Fluoropyrimidin-2(1H)-One

该化合物是一种七环有机化合物,其特点是带有氟原子和碳基组,其分子结构具有六人芳香环,含有两个氮原子,有助于其基本性和潜在反应力.氟原子的存在会增加其亲脂性,影响其生物活动,使其对医药化学感兴趣,特别是药物的开发.该化合物一般是白色至白色的固体,在极地有机溶剂中可溶解.其化学特性允许其参与各种反应,包括核生殖替代和凝聚反应,这对合成有机化学具有价值.此外,5-Fluoro-2,1H)-pyridiminone可能因其结构上与核糖基相似而表现出生物活动,包括抗病毒或抗癌特性.正如许多化学物质一样,处理应谨慎处理,并遵循适当的安全议定书,以降低任何潜在危害.

结构式图片

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上下游产品

4-thio-5-fluorouracil Flucytosine 1-(4-Chlorobenzyloxy)methyl-5-fluoropyrimidin-2-one 1-Propargyl-5-fluor-pyrimid-2-on

合成工艺路线路线简述

    氟胞嘧啶置于bifidobacterium Longum Cytosine Deaminase体系中,用 Various Solvent(S) 用作溶剂,化学反应生成2-羟基-5-氟嘧啶
    参考文献:Cloned Cytosine Deaminase Gene Expression Ofbifidobacterium Longumand Application To Enzyme/pro-Drug Therapy Of Hypoxic Solid Tumors
    标题:Cloned Cytosine Deaminase Gene Expression Ofbifidobacterium Longumand Application To Enzyme/pro-Drug Therapy Of Hypoxic Solid Tumors
    摘要:长双歧杆菌是正常菌群中的一种非致病性厌氧细菌.最近,有报道称长双歧杆菌在缺氧实体瘤中积累.目的基因在实体瘤中通过穿梭载体 Pbles100 转染的长双歧杆菌中表达.在本报告中,我们构建了 Pbles100-S-Ecd,其中包含胞嘧啶脱氨酶基因.我们通过蛋白质印迹证实转染的长双歧杆菌产生胞嘧啶脱氨酶.此外,转染的长双歧杆菌产生胞嘧啶脱氨酶,将 5-氟胞嘧啶转化为 5-氟尿嘧啶.长双歧杆菌可用于缺氧实体瘤的酶/前药治疗.
    Doi:10.1271/bbb.66.2362

    专利信息


    专利号:US-11306041-B2
    优先权日:2017-03-30
    标 题:Catalytic synthesis of super linear alkenyl arenes using rhodium catalysts
    发明人:SCHINSKI WILLIAM; GOLDMAN ALAN; GUNNOE THOMAS B; WEBSTER-GARDINER MICHAEL S; SCHWARTZ NICHOLE
    权利人:UNIV VIRGINIA PATENT FOUNDATION
    摘要:Catalytic methods for synthesis of super linear alkenyl arenes and alkyl arenes are provided. The methods are capable of synthesizing super linear alkyl and alkenyl arenes from simple arene and olefin starting materials and with high selectivity for linear coupling. Methods are also provided for making a 2,6-dimethylnapthalene (DMN) or 2,6-methylethylnapthalene (MEN).

    专利号:WO-0231176-A1
    优先权日:2000-10-12
    标题:Process for producing nucleoside
    发明人:FUJIWARA JUNYA; KOMATSU HIRONORI; AWANO HIROKAZU; FUKAZAWA NOBUYUKI; ANDO TOMOYUKI; TSUCHIYA KATSUTOSHI; CHIBA KYOKO; UMETANI HIDEKI; ARAKI TADASHI; YAMAUCHI TAKAHIRO
    权利人:MITSUI CHEMICALS INC; FUJIWARA JUNYA; KOMATSU HIRONORI; AWANO HIROKAZU; FUKAZAWA NOBUYUKI; ANDO TOMOYUKI; TSUCHIYA KATSUTOSHI; CHIBA KYOKO; UMETANI HIDEKI; ARAKI TADASHI; YAMAUCHI TAKAHIRO
    摘要:An anomer mixture of a nonnatural 1-phosphorylated saccharide is reacted with a base by the action of phosphorylase activity, wherein the exchange reaction between the phosphate group of the 1-phosphorylated saccharide and the base is conducted anomer-selectively. Metal cations capable of forming a sparingly water-soluble salt with phosphate ions are caused to be present in the reaction mixture, whereby the phosphate ions which are a by-product of the reaction can be precipitated as a sparingly water-soluble salt and the reaction equilibrium can be shifted toward nucleoside synthesis. Thus, the yield of the target compound is heightened. By utilizing a difference in the rate of the exchange reaction, a mixture of optical isomers of the nucleoside can be obtained in which one of the isomers is contained in a higher proportion.

    专利号:EP-1179598-B1
    优先权日:1999-05-13
    标题 :Process for producing nucleoside compound
    发明人:NIKUMARU SEIYA; NAKAMURA TAKESHI
    权利人:MITSUI CHEMICALS INC
    摘要:In preparation of a nucleoside compound by reacting a pentose-1-phosphate and a nucleic acid base or its analogue in the presence of enzyme activity of nucleoside phosphorylase, a metal salt capable of forming a water-insoluble salt with phosphoric acid may be added to a reaction system to eliminate phosphoric acid, a byproduct, from the reaction system so that the equilibrium reaction can be shifted toward a direction for nucleoside synthesis, leading to an improved yield of the desired nucleoside compound.
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    主要参考文献

    [参考文献]: Patricia M Lorusso, Et Al. Phase I Clinical Trial Of 5-Fluoro-Pyrimidinone (5Fp), An Oral Prodrug Of 5-Fluorouracil (5Fu). Invest New Drugs. 2002 Feb;20(1):63-71.

    合成参考文献


    参考文献:10.1007/s10637-011-9688-3
    摘要:Schott S, Wallwiener M, Kootz B, Seeger H, Fehm T, Neubauer H. Cytotoxicity of the new antimetabolite-bisphosphonate (5-FdU-alendronate) in comparison to standard therapeutics on breast and ovarian cancer cell lines in the ATP tumor chemosensitivity assay. Invest New Drugs. 2012 Aug;30(4):1750–5. doi: 10.1007/s10637-011-9688-3.
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