CAS: 247564-72-3; 2,4,5-Trifluorophenylboronic Acid

该化合物是一种氟化丙烯酸衍生物,广泛用作铃木-米亚乌拉交叉相交反应的关键中间体,其电子脱衣三氟联苯组增强反应性,促进双ary化合物合成过程中高效的C-C债券形成;该化合物在标准条件下具有良好稳定性,在普通有机溶剂中可溶解,适合多种催化用途;其高纯度和一贯性能确保制药和农用化学研究取得可靠成果,特别是在建造复合氟化松片方面;氟原子的存在还具有独特的电子和消毒特性,使先进的合成途径能够选择性地发挥作用.

结构式图片

欧盟法规

C&L通报

上下游产品

1-bromo-2,4,5-trifluorobenzene 2-chloro-4-fluoro-6-(2,4,5-trifluorophenyl)pyrimidine

合成工艺路线路线简述

    2,4,5-三氟溴苯置于正丁基锂,硼酸三甲酯体系中,用 正己烷 用作溶剂,化学反应 1.0H,以70%的收率获得2,4,5-三氟苯硼酸
    参考文献:多氟联苯的合成;推动铃木-宫浦交叉耦合与电子贫乏基板的边界
    标题:多氟联苯的合成;推动铃木-宫浦交叉耦合与电子贫乏基板的边界
    摘要:多氟联苯是许多不同应用中令人感兴趣且有希望的基材.不幸的是,目前用于合成这些化合物的所有方法仅适用于充满分子的手或仅在非常特殊的情况下.因此,迄今仍无法获得许多这些化合物.在这里,我们报告了合成各种高度氟化联苯的一般策略.在我们的研究中,我们研究了关键参数,例如不同的膦配体以及具有不同氟化度的各种亲核试剂和亲电试剂的影响.这些结果将已经非常通用的suzuki-Miyaura反应的范围扩展到了电子贫乏产品的合成上,使这些产品更容易获得.
    Doi:10.1021/acs.Joc.7B02267

    专利信息


    专利号:US-2025304580-A1
    优先权日:2021-11-09
    标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
    发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN
    权利人:VIGIL NEUROSCIENCE INC
    摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

    专利号:US-12319691-B2
    优先权日:2020-05-04
    标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
    发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI
    权利人:AMGEN INC; VIGIL NEUROSCIENCE INC
    摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

    专利号:US-12428425-B2
    优先权日:2020-05-04
    标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
    发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; PANTELEEV JANE; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN
    权利人:AMGEN INC; VIGIL NEUROSCIENCE INC
    摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

    专利号:CN-117486916-A
    优先权日:2023-12-29
    标题:A kind of synthesis method of 3,4,5-trifluorobenzene boric acid

    专利号:CN-115819260-B
    优先权日:2022-11-28
    标 题:A kind of synthesis process of sitagliptin intermediate

    专利号:CN-117486916-B
    优先权日:2023-12-29
    标题:A kind of synthesis method of 3,4,5-trifluorophenylboric acid
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    主要参考文献

    参考标题:A Rapid And Efficient Catalysis System For The Synthesis Of 4-Vinylbiphenyl Derivatives
    作者:Xiaowei Ma,Yan Liu,Ping Liu,Jianwei Xie,Bin Dai,Zhiyong Liu |发布日期:2013.12
    摘要:A Series Of 4‐vinylbiphenyl Derivatives Were Synthesized By Pd(Oac)2/pcy3‐catalyzed Suzuki-Miyaura Reaction In The Presence Of K3Po4.3H2O As Base In Toluene At 80°C For Only 10-30 Min, And The Corresponding Products Achieved 65-98% Yields. According To This Efficient C―c Bond‐forming Method, The Obtained Yields Of 4‐vinylbiphenyl Liquid Crystal Compounds Were Up To 92-96%. Copyright © 2013 John Wiley

    合成参考文献

    参考DOI号:10.1021/acs.j°C.7b02267
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