CAS: 252663-47-1; (4-(Benzylcarbamoyl)Phenyl)Boronic Acid

该化合物是一种有机化合物,其特点是存在一种碳酸功能组,众所周知,该化合物能够与二醇形成可逆的共价结合,因而在各种化学反应中,特别是在铃木的组合反应中具有价值.该化合物的特征是代之以苯基环的苯基,以苯丙基氨基碳基组为替代,增强其溶性性和再活性.该碳酸混合物有助于其在药用化学中的潜在应用,特别是在制药和农用化学中.该化合物在室温中一般为固体,在极地溶剂中可能表现出中等溶性.其再活性可能受到碳基组的存在的影响,该碳基组可参与氢结合并影响分子的整体电子特性.此外,该化合物的结构允许与生物目标发生潜在互动,使其在药物设计和开发中成为一项感兴趣的主题.应当观测安全性和处理预防措施,因为丁酸具有潜在的再活性.

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4-(苯甲基氨酰基)苯硼酸频哪酯 N-Benzyl-4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Benzamide 1073353-57-7
4-羧基苯硼酸 4-Carboxyphenylboronic Acid 14047-29-1

合成工艺路线路线简述

    📜4-(苯甲基氨酰基)苯硼酸频哪酯置于盐酸,Sodium Periodate体系中,用 四氢呋喃,水 用作溶剂,化学反应生成4-(N-苄基甲酰氨)苯基硼酸
    参考文献:芳基硼酸作为双作用faah和trpv1配体
    标题:芳基硼酸作为双作用faah和trpv1配体
    摘要:制备了一系列基于药效团模型设计的31种芳基硼酸,用于各种trpv1拮抗剂,并在faah和trpv1通道上进行了测试.其中四个化合物,即化合物3C,4A,5A,B充当双重faah / Trpv1阻滞剂,Ic 50值在0.56至8.11μm之间,而其他十种化合物(化合物1C,F-I,2C-F,4B)则抑制faah和激活/脱敏的trpv1.
    Doi:10.1016/j.Bmcl.2016.01.071

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    专利信息


    专利号:US-6919382-B2
    优先权日:2000-08-31
    标 题 :Preparation and uses of conjugated solid supports for boronic acids
    发明人:HALL DENNIS G
    权利人:UNIV ALBERTA
    摘要:The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.1016/j.bmcl.2016.01.071
    摘要:Morera E, Di Marzo V, Monti L, Allarà M, Schiano Moriello A, Nalli M, Ortar G, De Petrocellis L. Arylboronic acids as dual-action FAAH and TRPV1 ligands. Bioorganic & Medicinal Chemistry Letters. 2016 Mar;26(5):1401–5. doi: 10.1016/j.bmcl.2016.01.071.
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