CAS: 72420-38-3; 5-Methyl-4-Oxo-5-Phenyl-4,5-Dihydrofuran-2-Carboxylic Acid

该化合物是主要因其在制药领域应用而得到承认的一种化学化合物,被归类为非类固醇抗炎药物(NSAID),以其止痛和抗炎特性而著称.Acifran功能通过抑制环氧酶(COX)酶(Coifran),在合成 prostraglandins(可调节发炎和疼痛的化合物)方面发挥着关键作用.该物质一般是白色的脱白晶粉,在有机溶剂中可溶解.其药理学特征表明,它可能有效治疗关节炎和其他炎性疾病等疾病.然而,像许多NASSID一样,Acifran可能与副作用有关,包括胃肠问题和潜在的心血管风险,需要认真考虑其在临床环境中的使用情况.与任何制药化合物一样,它对于遵守管制准则和进行彻底研究以确保安全和功效至关重要.

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Methyl 4,5-Dihydro-5-Methyl-4-Oxo-5-Phenyl-2-Furancarboxylate 72429-82-4

合成工艺路线路线简述

    📜苯乙酮置于甲醇,Lithium Hydroxide,正丁基锂,Mercury(II) Perchlorate,Sodium Hydride体系中,用 四氢呋喃,甲醇,正己烷 作为反应溶剂,化学反应生成 阿西弗兰
    参考文献:Analogues Of Acifran: Agonists Of The High And Low Affinity Niacin Receptors,Gpr109A And Gpr109B
    标题:Analogues Of Acifran: Agonists Of The High And Low Affinity Niacin Receptors,Gpr109A And Gpr109B
    摘要:Recently Identified Gpcrs,Gpr109A And Gpr109B,The High And Low Affinity Receptors For Niacin,May Represent Good Targets For The Development Of Hdl Elevating Drugs For The Treatment Of Atherosclerosis. Acifran,An Agonist Of Both Receptors,Has Been Tested In Human Subjects,Yet Until Recently Very Few Analogs Had Been Reported. We Describe A Series Of Acifran Analogs Prepared Using Newly Developed Synthetic Pathways And Evaluated As Agonists For Gpr109A And Gpr109B,Resulting In Identification Of Compounds With Improved Activity At These Receptors.
    DOI:10.1021/jm070022X

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-7956214-B2
    优先权日:2001-11-02
    标题 :Process for the preparation of aniline-derived thyroid receptor ligands
    发明人:CHIDAMBARAM RAMAKRISHNAN; KANT JOYDEEP; WEAVER RAYMOND E; YU JURONG; GHOSH ARUN
    权利人:KAROBIO AB; BRISTOL MYERS SQUIBB CO
    摘要:Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

    专利号:US-10968192-B2
    优先权日:2018-09-26
    标题:Crystalline solid forms of N-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)benzyl)phenyl)butanamide and methods of their synthesis
    发明人:BEDNARZ MARK STEPHEN; Dai Kuangchu; ECKERT JEFFREY MANNING; LIM NGIAP-KIE; SIROIS LAUREN; WU WENXUE; ZHAO MATTHEW MANGZHU
    权利人:LEXICON PHARMACEUTICALS INC
    摘要:Methods of preparing, and solid forms of N-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)benzyl)phenyl)butanamide, and salts, solvates and cocrystals thereof, are disclosed.

    专利号:KR-101513003-B1
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy compositions and applications

    专利号:US-10814013-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:AU-2007308022-A2
    优先权日:2006-10-05
    标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Adepu KK, Kachhap S, Bhandari D, Anishkin A, Chintapalli SV. Computational insights on molecular interactions of acifran with GPR109A and GPR109B. J Mol Model. 2022 Jul 28;28(8):237. doi: 10.1007/s00894-022-05233-5. 16(3):251-63. doi: 10.3109/00498258609043528. 38(3):313-7. doi: 10.1038/clpt.1985.177. 340(2):482-90. doi: 10.1016/j.bbrc.2005.12.022. Epub 2005 Dec 19. 50(7):1445-8. doi: 10.1021/jm070022x. Epub 2007 Mar 15. 14(6):338-50. 47(1):50-6. doi: 10.1038/clpt.1990.7. 237(2):696-704. doi: 10.1016/j.atherosclerosis.2014.10.090. Epub 2014 Oct 28. 126(12):2637-46. doi: 10.1038/sj.jid.5700586. Epub 2006 Sep 28. 71(5):646-56. doi: 10.1016/j.bcp.2005.11.019. Epub 2006 Jan 18. Erratum in: Biochem Pharmacol. 2006 May 28;71(11):1662. Te Poole, Robert [corrected to te Poele, Robert H]. 23(23):14778. doi: 10.3390/ijms232314778.
    12: Pike NB, Wise A. Identification of a nicotinic acid receptor: is this the molecular target for the oldest lipid-lowering drug? Curr Opin Investig Drugs. 2004 Mar;5(3):271-5. 45(3):267-79. doi: 10.1016/0021-9150(82)90228-3. 45(3):281-90. doi: 10.1016/0021-9150(82)90229-5. 278(11):9869-74. doi: 10.1074/jbc.M210695200. Epub 2003 Jan 9.
    770:70-7. doi: 10.1016/j.ejphar.2015.11.052. Epub 2015 Dec 4. 48(3):240-4. doi: 10.1111/j.2042-7158.1996.tb05909.x. 16(4):244-8. doi: 10.1016/s0009-9120(83)90112-1. 173(3):367-71. doi: 10.3181/00379727-173-41658.

    合成参考文献


    摘要:Journal of Medicinal Chemistry., 25(1154), 1982
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