CAS: 819849-20-2; 2-Fluoro-5-Nitrophenylboronic Acid

该化合物是一种多用途的boron酸衍生物,通常用于铃木-米亚乌拉的交叉相交反应,原因是其反应性boronic酸功能组和电排的硝基和氟替代成分,硝基组的存在提高了催化变异的回活动性,而氟替代成分则有可能进一步功能化.该化合物在制药和材料科学研究中特别有用,用于建造复杂的双aryl结构.在标准处理条件下,该化合物具有良好的稳定性,通常作为白色的向离白晶体固体供应.该产品定义明确的再活动剖面图使其成为合成氟化和硝基替代芳香化合物的宝贵中间体.

结构式图片

欧盟法规

C&L通报

上下游产品

2-氟-5-硝基苯硼酸频哪醇酯 2-(2-Fluoro-5-Nitrophenyl)-4,4,5,5-Tetramethyl-1,3,2-Dioxaborolane 425378-68-3

合成工艺路线路线简述

    📜2-氟-5-硝基苯硼酸频哪醇酯置于sodium Periodate,水体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 2-氟-5-硝基苯硼酸
    参考文献:一种2-氟-5-硝基苯甲醚的合成方法
    标题:一种2-氟-5-硝基苯甲醚的合成方法
    摘要:本发明公开了一种2‑氟‑5‑硝基苯甲醚的合成方法,包括:步骤1,利用3‑溴‑4‑氟硝基苯和联硼酸频哪醇酯发生偶联反应,反应生成2‑氟‑5‑硝基苯硼酸频哪醇酯;步骤2,利用2‑氟‑5‑硝基苯硼酸频哪醇酯和高碘酸钠发生氧化水解反应,反应生成2‑氟‑5‑硝基苯硼酸;步骤3,利用2‑氟‑5‑硝基苯硼酸和双氧水发生氧化反应,反应生成2‑氟‑5‑硝基苯酚;步骤4,利用2‑氟‑5‑硝基苯酚和硫酸二甲酯发生甲基化反应,得到2‑氟‑5‑硝基苯甲醚.本发明2‑氟‑5‑硝基苯甲醚的合成方法,不但提供了一种在芳香环上引入羟基的新思路,而且产品具有较高的纯度和收率;此外,各步骤属于操作常规,所用设备常规,且原料便宜易得,适合工业化扩大生产.

    专利信息


    专利号:US-2023212216-A1
    优先权日:2019-12-20
    标 题:Synthesis of lactone derivatives and their use in the modification of proteins
    发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH
    权利人:GENIE BIOTECH UK LTD
    摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.

    专利号:AU-2020409711-A1
    优先权日:2019-12-20
    标题 :Synthesis of lactone derivatives and their use in the modification of proteins

    专利号:EP-4076533-A1
    优先权日:2019-12-20
    标 题:Synthesis of lactone derivatives and their use in the modification of proteins

    专利号:CA-3164962-A1
    优先权日:2019-12-20
    标题 :Synthesis of lactone derivatives and their use in the modification of proteins

    专利号:WO-2021123229-A1
    优先权日:2019-12-20
    标题:Synthesis of lactone derivatives and their use in the modification of proteins

    专利号:CN-116768729-A
    优先权日:2022-01-20
    标题 :A kind of synthesis method of 2-fluoro-5-nitroanisole

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.1016/j.ejmech.2022.114571
    摘要:Zhou J, Stapleton P, Xavier-Junior FH, Schatzlein A, Haider S, Healy J, Wells G. Triazole-substituted phenylboronic acids as tunable lead inhibitors of KPC-2 antibiotic resistance. European Journal of Medicinal Chemistry. 2022 Oct;240():114571. doi: 10.1016/j.ejmech.2022.114571.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知