CAS: 31462-55-2; 4-Fluoropyrimidine

该化合物是一种强效抑制物,是甲状腺合成酶,使其成为癌症研究的宝贵工具. 它具有高度选择性和特殊性,在定向药物开发中具有优势. 它独特的结构特征有助于它有效抑制肿瘤细胞扩散,成为抗乳癌治疗的有前途的候选者.

结构式图片

合成工艺路线路线简述

    📜4-嘧啶甲酸置于tetrakis(Acetonitrile)Copper(I)Tetrafluoroborate,1-Fluoro-2,4,6-Trimethylpyridin-1-Ium Tetrafluoroborate体系中,用 乙腈 作为反应溶剂,化学反应 24.0H,以56%的收率获得产物4-氟嘧啶
    参考文献:(杂)芳基羧酸脱羧卤化的统一方法
    标题:(杂)芳基羧酸脱羧卤化的统一方法
    摘要:芳基卤化物是合成化学中的基本基序,在金属介导的交叉偶联反应中起着关键作用,并在药物发现中充当重要的支架.尽管芳基羧酸的热脱羧官能化已得到广泛探索,但现有的卤代脱羧方法的范围仍然有限,并且目前不存在提供从芳基羧酸前体获得任何类型的芳基卤化物的统一策略.在此,我们报告了一种通过配体到金属电荷转移对(杂)芳基羧酸进行直接脱羧卤化的通用催化方法.该策略适用于极其广泛的底物范围.我们利用芳基自由基中间体实现不同的功能化途径:(1) 原子转移以获取溴代或碘代(杂)芳烃或(2)自由基被铜捕获并随后还原消除以反应生成氯代或氟代(杂)芳烃.所提出的配体到金属的电荷转移机制得到了一系列光谱研究的支持.
    DOI:10.1021/jacs.2C02392

    专利信息


    专利号:EP-0029960-A1
    优先权日:1979-11-30
    标 题 :Concentrated aqueous preparations of reactive dyestuffs free of solvents, and process for their preparation
    发明人:KOLL JOCHEN ING-GRAD; MOELLS HANS-HEINZ DR; BLECK WOLF-ECKHARD DR; HOERNLE REINHOLD DR; HILDEBRAND DIETRICH DR; NONN KONRAD DR
    权利人:BAYER AG
    摘要:Concentrated aqueous solutions of reactive dyes with alkylsulfonylpyrimidinyl-dichloroquinoxalinyl, monofluorotriazinyl or fluoropyrimidinyl reactive groups, which are distinguished by high storage stability and resistance to hydrolysis, are obtained by directly concentrating the reaction solutions of the last synthesis step by means of a membrane separation process, preferably by a membrane separation process.

    专利号:US-7189831-B2
    优先权日:2001-10-08
    标 题 :Organic compounds
    发明人:GISLER MARKUS
    权利人:CLARIANT FINANCE BVI LTD
    摘要:Fibre-reactive trisazo compounds of the formula (I) n nbearing halogenated pyrimidine reactive moieties and where the substituents are each as defined in the claims, and also the associated synthesis, the use of the compounds for dyeing or printing hydroxyl-containing or nitrogenous organic substrates, the use of the compounds as a component in an inkjet printing ink and also the dyed or printed substrates.

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    合成参考文献


    参考文献:10.1055/s-0039-1690248
    摘要:Liu F, Zhang X, Qian Q, Yang C. A Concise and Efficient Approach to 2,6-Disubstituted 4-Fluoropyrimidines from α-CF3 Aryl Ketones. Synthesis. 2019 Nov 06;52(02):273–80. doi: 10.1055/s-0039-1690248.
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