CAS: 77671-31-9; 4-Methyl-5-(4-(Methylthio)Benzoyl)-1H-Imidazol-2(3H)-One

该化合物是一种药剂,被归类为磷柴油酶抑制剂,具体针对III类磷柴油酶(PDE3),主要用于其积极的非热带效应,这种效应会增加心肌萎缩性,有利于治疗心脏衰竭. 苯丙胺通过增加细胞内循环过敏性单磷酸酯(cAMP)的浓度,导致心肌功能和血管变异作用的改善.该物质通常静脉注射,其半衰期相对较短,需要在治疗期间进行仔细监测.其化学结构包括一个丙烯环和一氯酮组,有助于其生物活动.

结构式图片

上下游产品

CAS号1192-34-3 4-甲基-1,3-二氢咪唑-2-酮 | CAS号13205-48-6 4-甲硫基苯甲酸 | CAS号1442-06-4 4-(甲硫基)苯甲酰氯 | CAS号403-42-9 对氟苯乙酮 | CAS号1778-09-2 4-甲硫基苯乙酮

合成工艺路线路线简述

    📜Diethyl 1-(3-Amino-1-(4-(Methylthio)Phenyl)-1-Oxobut-2-En-2-yl)Hydrazine-1,2-Dicarboxylate置于盐酸,水,Potassium Hydroxide,Sodium Hydroxide,Sodium Nitrite体系中,用 乙醇,水 作为反应溶剂,化学反应 68.67H,反应生成 依诺昔酮
    参考文献:通过烯胺酮从芳基甲基酮简单合成 4-Aroyl-5-Methyl-1H-Imidazol-2(3H)-One 衍生物(enoxymone 类似物)
    标题:通过烯胺酮从芳基甲基酮简单合成 4-Aroyl-5-Methyl-1H-Imidazol-2(3H)-One 衍生物(enoxymone 类似物)
    摘要:芳基甲基酮 1A-E 与 N,N-二甲基乙酰胺二甲基乙缩醛 (Dmadma) (E)-1Aryl-3-(二甲氨基)-But-2-En-1-Ones 2A-E 一起得到.在与乙酸铵的反应中取代 N,N-(二甲氨基) 基团得到相应的 (Z)-3-氨基-1-芳基-丁-2-烯-1 酮 3A-E.在 3A-E 与偶氮二羧酸二乙酯的反应中,形成了中间体 4A-E,在大多数情况下,它们无需分离就环化为乙基(5-芳酰基-4-甲基-2-氧代-2,3-二氢-1H-咪唑-1-基)氨基甲酸酯5A-E.酯基水解,然后中间体 6A-C,E 脱羧和脱氨基,反应生成 4-Aroyl-5-Methyl-1 Himidazol-2(3H)-Ones 7A-C,E.
    DOI:10.3998/ark.5550190.P008.236

    海关参考信息

    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-6030613-A
    优先权日:1995-01-17
    标题:Receptor specific transepithelial transport of therapeutics
    发明人:BLUMBERG RICHARD S; SIMISTER NEIL E; LENCER WAYNE I
    权利人:BRIGHAM & WOMENS HOSPITAL; UNIV BRANDEIS
    摘要:The present invention relates in general to methods and products for initiating an immune response against an antigen, and in particular relates to transepithelial delivery of antigens to provoke tolerance and immunity. The present invention further relates to methods and products for the transepithelial delivery of therapeutics. In particular, the invention relates to methods and compositions for the delivery of therapeutics conjugated to a FcRn binding partner to intestinal epithelium, mucosal epithelium and epithelium of the lung. The present invention further relates to the synthesis, preparation and use of the FcRn binding partner conjugates as, or in, pharmaceutical compositions for oral systemic delivery of drugs and vaccines.

    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

    专利号:AU-2007308022-A1
    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-2008107598-A1
    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: Nishikawa H, Goto M, Fukunishi S, Asai A, Nishiguchi S, Higuchi K. Cancer Cachexia: Its Mechanism and Clinical Significance. Int J Mol Sci. 2021 Aug 6;22(16):8491. doi: 10.3390/ijms22168491.
    2: Bedi H, Hammond C, Sanders D, Yang HM, Yoshida EM. Drug-Induced Liver Injury From Enobosarm (Ostarine), a Selective Androgen Receptor Modulator. ACG Case Rep J. 2021 Jan 7;8(1):e00518. doi: 10.14309/crj.0000000000000518.
    3: Yuan Y, Lee JS, Yost SE, Frankel PH, Ruel C, Egelston CA, Guo W, Gillece JD, Folkerts M, Reining L, Highlander SK, Robinson K, Padam S, Martinez N, Tang A, Schmolze D, Waisman J, Sedrak M, Lee PP, Mortimer J. A Phase II Clinical Trial of Pembrolizumab and Enobosarm in Patients with Androgen Receptor-Positive Metastatic Triple-Negative Breast Cancer. Oncologist. 2021 Feb;26(2):99-e217. doi: 10.1002/onco.13583. Epub 2020 Nov 24.

    合成参考文献


    参考文献:10.1186/cc10307
    摘要:Hasslacher J, Bijuklic K, Bertocchi C, Kountchev J, Bellmann R, Dunzendorfer S, Joannidis M. Levosimendan inhibits release of reactive oxygen species in polymorphonuclear leukocytes in vitro and in patients with acute heart failure and septic shock: a prospective observational study. Crit Care. 2011 Jul 12;15(4):R166.
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