CAS: 61622-34-2; (6R,7R)-7-(2-(2-Aminothiazol-4-yl)Acetamido)-3-(((1-(2-(Dimethylamino)Ethyl)-1H-Tetrazol-5-yl)Thio)Methyl)-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid

该化合物是一种广泛频谱的甲状腺素抗生素,被归类为乙型乳腺抗生菌,主要用于治疗各种细菌感染,特别是由克型阳性细菌和克型阴性细菌引起的感染;Cefotiam展示了一种行动机制,它抑制了细菌细胞墙合成,导致细胞分解和死亡;该化合物的特点是稳定地防止某些乙型肺炎,这提高了其抗抗抗菌菌菌株的功效;通常通过注射进行,以相对较低的毒性特征为名;从药物学角度讲,乙型肝炎是一种很好的吸食剂,在人体组织中具有有利的分布,能够有效治疗不同地点的感染;常见副作用包括胃肠扰动,过敏反应,在罕见的情况下还有血液异常;与所有抗生能一样,必须明智地使用乙型脑膜来防止抗生炎的抗体抗体.总体而言,丙型硫磺是武器库中一种有价值的治疗剂,用于抗细菌感染.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

2-diazo-1H-phenalene-1,3(2H)-dione sulfuric acid ethyl (1-naphthoyl)acetate 2-Carboxy-3-hydroxyphenalenone

合成工艺路线路线简述

    2-氨基-4-噻唑乙酸盐酸盐置于三乙胺,三氯氧磷体系中,用 N,N-二甲基甲酰胺,乙腈 作为反应溶剂,化学反应生成 头孢替安
    参考文献:一种盐酸头孢替安的制备方法
    标题:一种盐酸头孢替安的制备方法
    摘要:本发明提供了一种盐酸头孢替安的制备方法,其特征在于:以碳酸二甲酯作为反应溶剂的条件下,采用三氟化硼络合物催化7‑氨基头孢烷酸与1‑(2‑二甲基氨基乙基)‑1H‑5‑巯基四氮唑的缩合反应后,不经结晶分离,再以纯水为反应溶剂与氨基噻唑乙酰氯盐酸盐缩合成头孢替安,头孢替安经盐酸酸化结晶后得到盐酸头孢替安.本明中所使用的溶媒均可以回收套用,大大减少了环保压力,环境污染小,在降低成本的同时提高了盐酸头孢替安的指标.

    海关参考信息

    专利信息


    专利号:US-8017776-B2
    优先权日:2003-07-15
    标题 :Methods for synthesis of acyloxyalkyl compounds
    发明人:BHAT LAXMINARAYAN; GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

    专利号:US-9693999-B2
    优先权日:2011-01-26
    标题:Small molecule RNase inhibitors and methods of use
    发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
    权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
    摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

    专利号:US-8143437-B2
    优先权日:2002-02-19
    标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
    发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
    权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
    摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

    专利号:US-2009111737-A1
    优先权日:1999-05-24
    标题:Novel antibacterial agents
    发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
    权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
    摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

    专利号:WO-2009056955-A1
    优先权日:2007-10-30
    标题 :Amine-bearing phospholipids (abps), their synthesis and use
    发明人:ZUMBUEHL ANDREAS
    权利人:UNIV BASEL; ZUMBUEHL ANDREAS
    摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

    专利号:US-9868747-B2
    优先权日:2014-02-18
    标题:Marinopyrrole derivatives and methods of making and using same
    发明人:LI RONGSHI; SEBTI SAID; LIU YAN; QIN YONG; SONG HAO; CHENG CHUNWEI
    权利人:H LEE MOFFITT CANCER CT & RES; CHONGQING ZEIN PHARMACEUTICAL CO LTD
    摘要:Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.
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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Tian Y, Wang YN, Han Y, Zhang X, Hu CQ. Isolation, identification and in silico toxicity predictions of two isomers from cefotiam hydrochloride. J Pharm Biomed Anal. 2018 Sep 5;158:425-430. doi: 10.1016/j.jpba.2018.06.020. Epub 2018 Jun 18. 42(5):733-736. doi: 10.1097/FTD.0000000000000759. 17(3):163-74. doi: 10.2165/00003088-198917030-00003. 192(2):174-6. doi: 10.1159/000246352. 44(3):481-4, 493. Chinese. 77(45-46):2163-82. Italian. case reports, RAST analysis, and a review of the literature. Clin Exp Allergy. 1994 Feb;24(2):127-33. doi: 10.1111/j.1365-2222.1994.tb00208.x. 53(2):126-32. doi: 10.1055/s-0031-1297083. 5(2):85-99. doi: 10.1016/0924-8579(94)00038-v. 68(1):14-8. doi: 10.1055/s-2007-968168.

    合成参考文献


    参考文献:10.1186/1476-0711-10-30
    摘要:Riordan JT, Dupre JM, Cantore-Matyi SA, Kumar-Singh A, Song Y, Zaman S, Horan S, Helal NS, Nagarajan V, Elasri MO, Wilkinson BJ, Gustafson JE. Alterations in the transcriptome and antibiotic susceptibility of Staphylococcus aureus grown in the presence of diclofenac. Annals of Clinical Microbiology and Antimicrobials. 2011 Jul 21;10(1):30. doi: 10.1186/1476-0711-10-30.
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