CAS: 39718-89-3; 2-(4-((2-Methylallyl)Amino)Phenyl)Propanoic Acid

该化合物是一种主要用于其止痛和抗炎特性的非类固醇抗炎药物(NSAID),被归类为一种丙基酸衍生物,并因其能抑制环氧氧基酶(COX)酶而闻名,该酶在将参与炎症和疼痛信号的蛋白质合成中起着关键作用.Alminoproprofen通常以口服形式施用,用于治疗关节炎,肌肉疼痛和其他炎症候等症状.该物质在有机溶剂中表现出中等至高溶性,而其在水中的溶性则相对较低,这可能影响其生物利用率.Alminoproprofen的血清反应涉及吸收,分布,新陈代谢和排泄过程,而这些过程对于其治疗效果至关重要.与其他非氨ID一样,潜在的副作用可能包括胃肠道不适,心血管疼痛和其他炎障碍等症状.该物质需要仔细考虑病人病史和同时进行治疗.

结构式图片

上下游产品

2-(4-cyano-phenyl)-propionic acid

合成工艺路线路线简述

    📜2-(4-氰基苯基)丙酸置于羟胺,Potassium Carbonate,Sodium Hydroxide,三甲基硅烷化重氮甲烷体系中,用 乙醇,水,乙二醇,甲苯 用作溶剂,化学反应 22.0H,反应生成阿明洛芬
    参考文献:苄基 C-Oh 键的硼基自由基活化:通过光氧化还原催化实现游离醇和 Co2 的跨电偶联
    标题:苄基 C-Oh 键的硼基自由基活化:通过光氧化还原催化实现游离醇和 Co2 的跨电偶联
    摘要:通过在温和的可见光光氧化还原条件下用四苯基硼酸钠产生的中性二苯基硼基自由基活化游离醇,开发了一种直接裂解 C(Sp 3 )-Oh 键的新策略.该策略已通过游离醇和二氧化碳的交叉亲电偶联来合成羧酸得到验证.已经实现了将一系列伯,仲和叔苯甲醇直接转化为酸.对照实验和计算研究表明,用中性硼基自由基活化醇会发生 C(Sp 3 )-Oh 键的均裂,从而产生烷基自由基.在光氧化还原条件下将烷基自由基还原成碳阴离子后,用co进行以下羧化2提供耦合产品.
    Doi:10.1021/jacs.1C12463

    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-2012029226-A1
    优先权日:2009-02-06
    标题:Method for the synthesis of chiral alpha-aryl propionic acid derivatives
    发明人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE
    权利人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE
    摘要:The present invention provides a method for the synthesis of optically pure α-aryl propionic acid derivatives comprising subjecting the corresponding racemic α-aryl propionic acid derivatives to high sheer or impact forces, such as grinding.

    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-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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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Hanada S, Fujioka K, Futamura Y, Manabe N, Hoshino A, Yamamoto K. Evaluation of anti-inflammatory drug-conjugated silicon quantum dots: their cytotoxicity and biological effect. Int J Mol Sci. 2013 Jan 10;14(1):1323-34. doi: 10.3390/ijms14011323.
    2: Syed NI, Zehra F, Syed AA, Karim S, Khan FZ. Comparing the effects of salts of diclofenac and alminoprofen with aspirin on serum electrolytes, creatinine and urea levels in rabbits. Pak J Pharm Sci. 2012 Oct;25(4):777-82. Japanese. Japanese. French. Japanese. Japanese. Japanese. French. doi: 10.1016/j.jpba.2013.08.023. Epub 2013 Aug 29. Japanese.

    合成参考文献


    摘要:Yakuri to Chiryo. Pharmacology and Therapeutics., 14(2093), 1986
    摘要:Drugs of the Future., 9(165), 1984
    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).
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