CAS: 1074-41-5; 6-Amino-2-(Methylthio)Pyrimidin-4-Ol

该化合物是一种三环有机化合物,其基芯在6位置被氨基氨基中组取代,二位置为甲基硫烷.这一结构在合成应用中,特别是在制药和农用化学研究中具有多功能性,它作为发展核核素类比和生物活性分子的关键中间体.它的活性氨基和硫醚功能能够进一步衍生,促进更复杂的乙基循环的合成.化合物在标准条件下表现出稳定性,确保可靠的处理和储存.其定义明确的化学特性使它成为医药化学和材料科学应用的宝贵建筑.

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dimethyl sulfate methyl iodide 6-amino-2-thioxo-1,2-dihydro-4(3H)-pyrimidinone 6-Amino-2-thiouracil (9)-dihydro-purin-6-one2-methylsulfanyl-1,7(9)-dihydro-purin-6-one 4-amino-6-chloro-2-methylthiopyrimidine 6-amino-2-(morpholin-4'-yl)pyrimidin-4(3H)-one 6-amino-2-(4'-methylpiperazin-1'-yl)ptrimidin-4(3H)-one

合成工艺路线路线简述

    📜6-氨基-2-硫脲嘧啶置于potassium Carbonate体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应生成基巯基-4-氨基-6-羟基嘧啶
    参考文献:新型强效环丙沙星-尿嘧啶偶联物作为 Dna 促旋酶和拓扑异构酶 Iv 抑制剂,可对抗耐甲氧西林金黄色葡萄球菌
    标题:新型强效环丙沙星-尿嘧啶偶联物作为 Dna 促旋酶和拓扑异构酶 Iv 抑制剂,可对抗耐甲氧西林金黄色葡萄球菌
    摘要:合成了一系列环丙沙星-尿嘧啶偶联物5A-T,并通过1 H NMR,13 C NMR,质谱和元素分析进行了鉴定.抗菌结果表明,新衍生物对革兰氏阳性菌的活性优于革兰氏阴性菌;大多数目标化合物对金黄色葡萄球菌atcc 6538表现出非常好的活性.化合物5B和5G具有最高的活性,其 Mic 分别为 1.25 和 2.37 µm,比母体药物环丙沙星 Mic 为 7.58 µm 更有效.此外,它们还表现出对mrsa Aumc 261的强效活性mic 分别为 0.031 和 0.046 µm,高于 Mic 为 0.57 µm 的环丙沙星. 此外,与环丙沙星相比,化合物5B和5G显示出对 Dna 促旋酶 (Ic 50 = 1.72 和 5.72 µm) 和拓扑异构酶 Iv (4.36 和 7.77 µm) 的有效抑制活性,Ic 50值分别为 0.66 和 8.16 µm.分子对接研究表明化合物5B和5G
    Doi:10.1016/j.Bmc.2022.117004

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    专利信息


    专利号:US-6818633-B2
    优先权日:2001-06-29
    标题:Antiviral compounds and methods for synthesis and therapy
    发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN
    权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING
    摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

    专利号:US-2017275287-A1
    优先权日:2014-08-22
    标 题 :Novel n2, n4, n7, 6-tetrasubstituted pteridine-2,4,7-triamine and 2, 4, 6, 7-tetrasubstituted pteridine compounds and methods of synthesis and use thereof
    发明人:LIPFORD GRAYSON B; ZEPP CHARLES M
    权利人:JANUS BIOTHERAPEUTICS INC
    摘要:Compounds as immune system modulators bearing a pteridine core are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing autoimmunity disease using the same are described.

    专利号:US-5612468-A
    优先权日:1994-05-18
    标题:Pteridine nucletide analogs as fluorescent DNA probes
    发明人:HAWKINS MARY E; PFLEIDERER WOLFGANG; DAVIS MICHAEL D; BALIS FRANK
    权利人:US HEALTH
    摘要:The invention provides novel pteridine nucleotides which are highly fluorescent under physiological conditions and which may be used in the chemical synthesis of fluorescent oligonucleotides. The invention further provides for fluorescent oligonucleotides comprising one or more pteridine nucleotides. In addition the invention provides for pteridine nucleotide triphosphates which may be used as the constituent monomers in DNA amplification procedures.

    专利号:EP-3183251-A1
    优先权日:2014-08-22
    标题 :Novel n2, n4, n7, 6-tetrasubstituted pteridine-2,4,7-triamine and 2, 4, 6, 7-tetrasubstituted pteridine compounds and methods of synthesis and use thereof

    专利号:EP-3398948-A2
    优先权日:2014-08-22
    标题 :2,4,6,7-tetrasubstituted pteridine compounds and methods of synthesis and use thereof

    专利号:WO-2016029077-A1
    优先权日:2014-08-22
    标题:Novel n2, n4, n7, 6-tetrasubstituted pteridine-2,4,7-triamine and 2, 4, 6, 7-tetrasubstituted pteridine compounds and methods of synthesis and use thereof

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    合成参考文献


    摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2018) 3, 167.
    摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 318.
    摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 459.
    摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 460.
    摘要:Wang, X.; Hu, J., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2.
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