CAS: 61-68-7; 2-((2,3-Dimethylphenyl)Amino)Benzoic Acid

该化合物是一种非类固醇抗炎药物(NSAID),属于胎儿类,主要用于其止痛,抗炎和抗苯性特性,其作用是抑制环氧酶(COX)酶,从而减少丙烯酸合成.该化合物在控制轻度至中度疼痛方面特别有效,包括痢疾,肌肉骨骼状况和手术后不适状态.它的迅速行动和有利的生物利用率使它成为短期疼痛缓解的实用选择.口服配方中可以使用甲基乙酸,并适合病人的个别需要.对胃肠或心血管风险因素的病人,如其他非国家行为者一样,给予谨慎.其选择性和功效凸显了其在临床环境中的效用.

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CAS号13481-67-9 2-[(2,3-dimethy... | CAS号87-59-2 2,3-二甲基苯胺 | CAS号118-91-2 邻氯苯甲酸 | CAS号1488-42-2 二苯基碘-2-羧酸内盐 | CAS号88-67-5 邻碘苯甲酸 | CAS号55591-34-9 N-(2,3-dimethyl... | CAS号873-32-5 邻氯苯腈 | CAS号1804-54-2 1-(1',2'-dimeth... | CAS号137488-33-6 1-(1',2'-dimeth... | CAS号10457-97-3 2,3-dihydroxypr... | CAS号106724-32-7 3-pyridin-4-ylp... | CAS号20723-85-7 (2-methoxypheny... | CAS号1804-47-3 Benzoic acid, 2... | CAS号29098-16-6 ethoxymethyl 2-... | CAS号137488-42-7 1-(2,3-dimethyl... | CAS号1618-52-6 2-(2,3-dimethyl... | CAS号1222-42-0 2-[(2,3-Dimethy... | CAS号59338-12-4 1-(2,3-dimethyl...

合成工艺路线路线简述

    2-[(2,3-二甲基苯基)氨基]苯甲腈置于水,Potassium Hydroxide体系中,用 乙醇 作为反应溶剂,化学反应 20.0H,以161 Mg的收率获得产物扑湿痛
    参考文献:Piii/pv=o催化下硝基芳烃和硼酸的分子间还原c-N交叉偶联
    标题:Piii/pv=o催化下硝基芳烃和硼酸的分子间还原c-N交叉偶联
    摘要:报道了一种通过分子间 Cn 偶联合成芳基和杂芳基胺的主要基团催化方法.该方法采用基于小环有机磷的催化剂(1,2,2,3,4,4-六甲基膦烷)和末端氢硅烷还原剂(苯基硅烷)来驱动硝基(杂)芳烃与硼酸的还原性分子间偶联.展示了在构建 Csp2-N(来自芳基硼酸)和 Csp3-N 键(来自烷基硼酸)中的应用;该反应在 Csp3-N 键形成方面是立体有择的.该方法构成了一条从现成的构件到有价值的含氮产品的新途径,与现有催化 Cn 偶联方法在范围和化学选择性方面具有互补性.
    DOI:10.1021/jacs.8B10769

    海关参考信息

    专利信息


    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: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.

    专利号:US-12264143-B2
    优先权日:2020-12-17
    标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use
    发明人:SAMMIS GLENN M; ROGGEN MARKUS
    权利人:NALU BIO INC
    摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.

    专利号:US-10975069-B2
    优先权日:2014-04-01
    标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
    发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
    权利人:UNIV WASHINGTON
    摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

    专利号:US-2008287407-A1
    优先权日:2003-12-10
    标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
    发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
    权利人:NITROMED INC
    摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, 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 at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

    专利号:US-8304409-B2
    优先权日:2002-07-03
    标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
    发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
    权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA
    摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
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    主要参考文献


    1: Shabbir A, Arshad HM, Shahzad M, Shamsi S, Ashraf MI. Immunomodulatory activity of mefenamic acid in mice models of cell-mediated and humoral immunity. Indian J Pharmacol. 2016 Mar-Apr;48(2):172-8. doi: 10.4103/0253-7613.178837.
    2: Nurhikmah W, Sumirtapura YC, Pamudji JS. Dissolution Profile of Mefenamic Acid Solid Dosage Forms in Two Compendial and Biorelevant (FaSSIF) Media. Sci Pharm. 2016 Feb 14;84(1):181-90. doi: 10.3797/scipharm.ISP.2015.09. eCollection 2016.
    3: Adira Wan Khalit WN, Tay KS. Aqueous chlorination of mefenamic acid: kinetics, transformation by-products and ecotoxicity assessment. Environ Sci Process Impacts. 2016 Apr 9. [Epub ahead of print] doi: 10.1016/j.ctcp.2015.09.003. Epub 2015 Sep 25. doi: 10.1016/j.antiviral.2016.01.006. Epub 2016 Jan 18. doi: 10.1002/prot.24985. Epub 2016 Feb 3. doi: 10.1016/j.jenvman.2015.11.029. doi: 10.1515/acph-2015-0035. doi: 10.1016/j.ejpb.2015.11.011. Epub 2015 Nov 22. doi: 10.3857/roj.2015.33.3.256. Epub 2015 Sep 30.

    合成参考文献


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    摘要:Tjandrawinata RR, Nofiarny D, Susanto LW, Hendri P, Clarissa A. Symptomatic treatment of premenstrual syndrome and/or primary dysmenorrhea with DLBS1442, a bioactive extract of Phaleria macrocarpa. Int J Gen Med. 2011;4():465–76.
    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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