CAS: 17969-20-9; 2-(2-(4-Chlorophenyl)Thiazol-4-yl)Acetic Acid

该化合物是一种属于箱状酸类别的化学化合物,其特点是分子结构,包括一个苯基组和一个箱状酸功能组,有助于其酸性;众所周知,芬可乐酸用于各种应用,特别是在制药和农用化学领域;在有机溶剂中表现出中等溶性,水溶性有限,这是许多有机酸的典型特征;该化合物还可能显示生物活动,使其对药用化学感兴趣;在标准条件下,其稳定性允许其在各种配方中使用,尽管它可能敏感地注意极高的pH水平或反应剂;与许多化学物质一样,在处理和储存准则方面,以及接触的潜在危险方面,应参考安全数据表.

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2-(2-(4-氯苯基)噻唑-4-基)乙酸乙酯 Ethyl 2-(2-(4-Chlorophenyl)Thiazol-4-yl)Acetate 20287-70-1
2-(2-(4-Chlorophenyl)Thiazol-4-yl)Ethan-1-Ol 27473-03-6

合成工艺路线路线简述

    📜2-(2-(4-Chlorophenyl)Thiazol-4-yl)Ethan-1-Ol置于penicillium Duclauxi体系中,用 水 用作溶剂,化学反应 76.0H,反应生成氯苯噻唑乙酸
    参考文献:微生物对2-(4-氯苯基)噻唑-4-基乙酸(芬氯酸)及相关化合物的代谢
    标题:微生物对2-(4-氯苯基)噻唑-4-基乙酸(芬氯酸)及相关化合物的代谢
    摘要:
    Doi:10.1021/jm00280A012

    海关参考信息

    专利信息


    专利号:US-5847150-A
    优先权日:1996-04-24
    标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles
    发明人:DORWALD FLORENCIO ZARAGOZA
    权利人:NOVO NORDISK AS
    摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

    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-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.

    专利号:US-2024287041-A1
    优先权日:2021-05-20
    标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
    发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

    专利号:AU-2022276509-A1
    优先权日:2021-05-20
    标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

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    主要参考文献


    1: Ekdahl A, Weidolf L, Baginski M, Morikawa Y, Thompson RA, Wilson ID. The metabolic fate of fenclozic acid in chimeric mice with a humanized liver. Arch Toxicol. 2018 Sep;92(9):2819-2828. doi: 10.1007/s00204-018-2274-0. Epub 2018 Aug 9.
    2: Fenclozic acid. Lancet. 1970 Mar 28;1(7648):662-3. 91(7):2643-2653. doi: 10.1007/s00204-016-1894-5. Epub 2016 Nov 28.
    4: Pickup K, Wills J, Rodrigues A, Jones HB, Page C, Martin S, Sarda S, Wilson I. The metabolic fate of [14C]-fenclozic acid in the hepatic reductase null (HRN) mouse. Xenobiotica. 2014 Jan;44(2):164-73. doi: 10.3109/00498254.2013.866299. Epub 2013 Dec 10. 86(22):11281-9. doi: 10.1021/ac502943d. Epub 2014 Oct 31. 6(1):81-88. doi: 10.1039/c6tx00376a.

    合成参考文献


    参考文献:10.1016/j.drudis.2011.05.007
    摘要:Chen M, Vijay V, Shi Q, Liu Z, Fang H, Tong W. FDA-approved drug labeling for the study of drug-induced liver injury. Drug Discov Today. 2011 Aug;16(15-16):697–703. doi: 10.1016/j.drudis.2011.05.007.
    摘要:Nature., 221(582), 1969
    摘要:Farmaco, Edizione Scientifica., 40(875), 1985 []
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