CAS: 530-78-9; 2-((3-(Trifluoromethyl)Phenyl)Amino)Benzoic Acid

该化合物是一种属于胎儿类化合物的非类固醇抗炎药物(NSAID),主要用于其止痛和抗炎特性,通常用于治疗与各种条件有关的疼痛和炎症;氟虫酸的化学结构具有2-苯基氨基苯并呋喃酸脊椎的化学特征,有助于其药理活动;其特点是能够抑制环氧酶酶酶,从而减少作为炎症和疼痛媒介的蛋白质合成;氟虫酸通常用于口服,并因其相对高的亲食性而闻名,这可能影响其吸收和在体内的分布;虽然有效,它也可能与胃肠侧效应和其他不良反应有关,与其他非氨基甲酸基乙酰胺相似;在临床环境中,它的使用经常受到监测,以降低潜在风险,特别是在有前状况的病人中.

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CAS号2765-91-5 methyl 2-[3-(tr... | CAS号98-16-8 间三氟甲苯胺 | CAS号118-91-2 邻氯苯甲酸 | CAS号17763-70-1 Benzoic acid, 2... | CAS号1977-00-0 sodium 2-[[3-(t... | CAS号32509-03-8 1-[3-(trifluoro... | CAS号137488-39-2 1-(3'-trifluoro... | CAS号92-30-8 2-三氟甲基吩噻嗪 | CAS号29098-19-9 acetyloxymethyl... | CAS号29261-37-8 benzoyloxymethy... | CAS号2765-91-5 methyl 2-[3-(tr... | CAS号32509-03-8 1-[3-(trifluoro...

合成工艺路线路线简述

  • 合成目标产物 Flufenamic Acid 主要起始原料 Benzoic Acid,2-[[3-(Trifluoromethyl)Phenyl]Amino]-, Methyl Ester
  • (文献来源)合成步骤主要原料 Benzoic Acid,2-[[3-(Trifluoromethyl)Phenyl]Amino]-, Methyl Ester
2-(3-三氟甲基苯基氨基)-苯甲腈置于potassium Hydroxide体系中,用 乙醇,水 作为反应溶剂,化学反应 20.0H,以98%的收率获得产物氟灭酸
参考文献:硝基化合物对钼酸的还原钼催化直接胺化
标题:硝基化合物对钼酸的还原钼催化直接胺化
摘要:在广泛的化学领域中,芳族胺的合成至关重要.我们报道了硼酸与硝基化合物的直接胺化反应,反应生成(杂)芳基胺.二氧钼(vi)催化剂和三苯膦作为廉价的还原剂的新颖组合已显示出实现这种新的c-N偶联的决定性作用.我们的方法论已被证明是可扩展的,耐空气和湿气的,高度化学选择性的,并且可以同时结合脂肪族和芳香族硝基化合物.此外,这种芳香族仲胺的一般且分步经济的合成方法可耐受芳基卤化物和羰基化合物,因此与其他芳香族胺合成物具有正交性.
DOI:10.1002/anie.201812806

海关参考信息

专利信息


专利号:US-2024287520-A1
优先权日:2021-06-30
标题:Method for synthesis of linkage modified oligomeric compounds
发明人:RODRIGUEZ ANDREW A
权利人:IONIS PHARMACEUTICALS INC
摘要:The present disclosure provides methods of synthesizing modified oligonucletodies and oligomeric compounds (including oligomeric compounds that are antisense agents or portions thereof) comprising a modified oligonucleotide having at least one modified internucleoside linking group. In certain embodiments, the present disclosure provides stabilized formulations of certain sulfonyl azides for use in the synthesis of olignonucleotides comprising one or more sulfonyl phosphoramidate linkages. Some embodiments provide stabilized compositions of high energy reagents that may be used in the synthesis of modified oligonucleotides, allowing for safe process scale preparation thereof.

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:WO-2004011474-A1
优先权日:2002-07-31
标题:Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-6653468-B1
优先权日:2002-07-31
标 题 :Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
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主要参考文献


1: Hendriks CM, Penning TM, Zang T, Wiemuth D, Gründer S, Sanhueza IA, Schoenebeck F, Bolm C. Pentafluorosulfanyl-containing flufenamic acid analogs: Syntheses, properties and biological activities. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4437-40. doi: 10.1016/j.bmcl.2015.09.012. Epub 2015 Sep 8.
2: Hoppel M, Ettl H, Holper E, Valenta C. Influence of the composition of monoacyl phosphatidylcholine based microemulsions on the dermal delivery of flufenamic acid. Int J Pharm. 2014 Nov 20;475(1-2):156-62. doi: 10.1016/j.ijpharm.2014.08.058. Epub 2014 Aug 29. doi: 10.1016/j.ijpharm.2015.05.056. Epub 2015 May 26. doi: 10.1016/j.ijpharm.2014.12.048. Epub 2014 Dec 24. doi: 10.1016/j.ejphar.2015.09.014. Epub 2015 Sep 16. doi: 10.1021/jp5125519. Epub 2015 Mar 23. doi: 10.1016/j.pharmthera.2013.01.012. Epub 2013 Jan 25. Review.
8: Guo M, Wang K, Hamill N, Lorimer K, Li M. Investigating the Influence of Polymers on Supersaturated Flufenamic Acid Cocrystal Solutions. Mol Pharm. 2016 Sep 6;13(9):3292-307. doi: 10.1021/acs.molpharmaceut.6b00612. Epub 2016 Aug 15. doi: 10.1016/j.ijantimicag.2013.08.018. Epub 2013 Oct 1.

合成参考文献


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参考文献:10.1152/jn.00025.2011
摘要:Wang S, Zhang A, Kurada L, Matsui T, Lei S. Cholecystokinin facilitates neuronal excitability in the entorhinal cortex via activation of TRPC-like channels. Journal of Neurophysiology. 2011 Sep;106(3):1515–24. doi: 10.1152/jn.00025.2011.
参考文献:10.1124/jpet.111.183020
摘要:Chi Y, Li K, Yan Q, Koizumi S, Shi L, Takahashi S, Zhu Y, Matsue H, Takeda M, Kitamura M, Yao J. Nonsteroidal Anti-Inflammatory Drug Flufenamic Acid Is a Potent Activator of AMP-Activated Protein Kinase. The Journal of Pharmacology and Experimental Therapeutics. 2011 Oct;339(1):257–66. doi: 10.1124/jpet.111.183020.
参考文献:10.3389/fphys.2011.00029
摘要:Lees-Green R, Du P, O'Grady G, Beyder A, Farrugia G, Pullan AJ. Biophysically based modeling of the interstitial cells of cajal: current status and future perspectives. Front Physiol. 2011;2():29.
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