CAS: 162607-15-0; (4-Methylthiophen-2-yl)Boronic Acid

该化合物是一种环乙酸激素衍生物,广泛用作铃木-米亚鲁交叉相交反应的关键中间体,其硫苯基和碳酸功能组可有效形成碳-碳结,特别是在合成药品,农用化学品和先进材料方面.甲基替代成分可增强消毒和电子特性,提高混合反应的选择性.该化合物在标准条件下具有良好的稳定性,并表现出对卤化亚胺的高度再活性,因此对建设复杂的分子结构很有价值.它与各种反应条件和功能组的兼容性进一步强调了其在有机合成和药用化学研究中的实用性.

结构式图片

相似化合物

635305-48-5 177735-09-0 6165-68-0

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上下游产品

3-Methylthiophene 2-bromo-4-methylthiophene 1,1-dimethylethyl ((1S)-2-{[3-({[2-chloro-4-(4-methyl-2-thienyl)phenyl]sulfonyl}amino)-4-(methyloxy)phenyl]amino}-1-methyl-2-oxoethyl)methylcarbamate 4,4,5,5-tetramethyl-2-(4-methylthiophen-2-yl)[1,3,2]dioxaborolane 2-amino-5-(4-methyl-thiophen-2-yl)-benzonitrile 2-chloro-4-(4-methylthiophen-2-yl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine

合成工艺路线路线简述

    2-溴-4-甲基噻吩置于盐酸,仲丁基锂体系中,用 四氢呋喃,水 用作溶剂,化学反应 5.08H,反应生成4-甲基-2-噻吩硼酸
    参考文献:一种单杂环硼酸的制备方法
    标题:一种单杂环硼酸的制备方法
    摘要:本发明提供了一种单杂环硼酸的制备方法,所述制备方法包括以下步骤:(1)将式i所示化合物与烷基硼酸酯溶于溶剂a中,得到a溶液,将有机锂试剂溶于溶剂b中,得到b溶液,将a溶液与b溶液连续加料反应,流出反应管后终止反应得到中间体;(2)将步骤(1)得到的中间体经水解反应后得到所述单杂环硼酸;本发明所提供的制备方法能够提高反应收率,最高可达到95%以上,减少反应时间,可在5‑60Min中内完成反应,并且可以使反应温度提高,降低了低温反应的能耗,温度可控,安全性提高,压力控制方便,自动化程度提高,有利于生产操作,成本降低,提升经济效益.

    专利信息


    专利号:US-6825185-B2
    优先权日:2000-12-21
    标题:Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use
    发明人:KHANAPURE SUBHASH P; GARVEY DAVID S; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GASTON RICKY D
    权利人:NITROMED INC
    摘要:The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B 4 (LTB 4 ) receptor antagonists, leukotriene A 4 (LTA 4 ) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H 2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

    专利号:US-2009137557-A1
    优先权日:2005-11-22
    标题 :Calcilytic Compounds
    发明人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S
    权利人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S
    摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.

    专利号:WO-2010039922-A1
    优先权日:2008-10-03
    标 题:Calcilytic compounds
    发明人:CASILLAS LINDA N; CHARNLEY ADAM KENNETH; DEMARTINO MICHAEL P; DONG XIAOYANG; HARRIS PHILIP ANTHONY; MARQUIS ROBERT W JR; RAMANJULU JOSHI M; TROUT ROBERT
    权利人:GLAXOSMITHKLINE LLC; CASILLAS LINDA N; CHARNLEY ADAM KENNETH; DEMARTINO MICHAEL P; DONG XIAOYANG; HARRIS PHILIP ANTHONY; MARQUIS ROBERT W JR; RAMANJULU JOSHI M; TROUT ROBERT
    摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.

    专利号:WO-2010065383-A1
    优先权日:2008-11-25
    标 题 :Calcilytic compounds
    发明人:CASILLAS LINDA N; CHARNLEY ADAM KENNETH; HARRIS PHILIP ANTHONY; JEONG JAE U; MARQUIS ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT
    权利人:GLAXOSMITHKLINE LLC; CASILLAS LINDA N; CHARNLEY ADAM KENNETH; HARRIS PHILIP ANTHONY; JEONG JAE U; MARQUIS ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT
    摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.

    专利号:CN-112679292-B
    优先权日:2020-12-25
    标 题 :Synthesis method of secondary sulfonamide compound
    上海常丰生物医药科技有限公司
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    合成参考文献


    参考文献:10.1021/jm980343w
    摘要:Weston GS, Blázquez J, Baquero F, Shoichet BK. Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase. J Med Chem. 1998 Nov 05;41(23):4577–86. doi: 10.1021/jm980343w.
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