CAS: 119914-60-2; 1-Cyclopropyl-6-Fluoro-5-Methyl-7-(3-Methylpiperazin-1-yl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

该化合物是一种合成的氟己酮抗生素,具有广泛的抗菌性,具有广泛的抗菌性,主要有效防治各种克己体和克己体细菌,有助于治疗呼吸道和尿道感染,抑制细菌DNA甘蓝和多孔异构体酶IV的复合功能,对DNA复制和转录至关重要的酶.格雷帕福罗克辛的特点是口服生物利用率较高,具有有利的药用植物特征,可以进行有效的系统分布.然而,与其他氟丙酮一样,它可能与副作用有关,包括胃肠紊乱,中...

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CAS号109-07-9 2-甲基哌嗪 | CAS号119915-47-8 1-环丙基-6,7-二氟-5-...

合成工艺路线路线简述

    📜2-甲基哌嗪,7-溴-1-环丙基-6-氟-5-甲基-4-氧代-1,4-二氢-3-喹啉羧酸置于乙醇,乙醇乙酸乙酯体系中,用 N-甲基吡咯烷酮 用作溶剂,化学反应 0.33H,以to Give 1-Cyclopropyl-6-Fluoro-7-(3-Methyl-1-Piperazinyl)-5-Methyl-1,4-Dihydro-4-Oxoquinoline-3-Carboxylic Acid (310 Mg)的收率获得格帕沙星
    参考文献:Benzoheterocyclic Compounds
    标题:Benzoheterocyclic Compounds
    摘要:化合物3-甲酰基-4-氧代喹啉的结构式如下:##str1## 其中r.Sup.1是氢原子或较低的脂肪酰基,R.Sup.2是氢原子或较低的烷基,R.Sup.3是较低的烷基,X是卤素,以及其药学上可接受的盐.该化合物具有优异的抗微生物活性,因此可用作抗微生物剂,以及含有该化合物作为活性成分的制药组合物.

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    专利信息


    专利号:US-2024197774-A1
    优先权日:2021-04-16
    标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
    发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
    权利人:UNIV TEXAS
    摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

    专利号:US-12252473-B2
    优先权日:2022-04-18
    标 题:Preparation methods of quinolone compounds and intermediates thereof
    发明人:LEI JIE; CHEN ZHONGZHU; XU ZHIGANG; TANG DIANYONG; XU JIAYU; ZHOU HAOYI; XIA DANDAN; LIU YAO; CAO YIHUA; LUO JIE
    权利人:UNIV CHONGQING ARTS & SCIENCES
    摘要:The present application relates to processes for the preparation of quinolone compounds and intermediates thereof, particularly to processes for the preparation of quinolones and pharmaceutical intermediates of the quinolones. In particular, the present application provides a process for the preparation of a compound of Formula I, and a process for the synthesis of quinolone compounds using the compound of Formula I as an intermediate. The process for the preparation of the compound of Formula I comprises the steps of:reacting a compound of Formula A with R5NH2 and R6Cl in the presence of a base to form the compound of Formula I,

    专利号:WO-2025128098-A1
    优先权日:2023-12-13
    标 题 :Solid oral dosage forms, kits, and methods of using the same
    发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
    权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
    摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

    专利号:US-8093381-B2
    优先权日:2007-05-24
    标题:Method of synthesis of fluoroquinolones
    发明人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS
    权利人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS; BIOCODEX
    摘要:The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and X are as defined in Claim 1.

    专利号:US-10443047-B2
    优先权日:2014-05-01
    标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase
    发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E
    权利人:NOVOGY INC
    摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.

    专利号:WO-2012149093-A1
    优先权日:2011-04-26
    标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof
    发明人:LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
    权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
    摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.

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    主要参考文献


    1: Watanabe M, Kobayashi M, Ogura J, Takahashi N, Yamaguchi H, Iseki K. Alteration of pharmacokinetics of grepafloxacin in type 2 diabetic rats. J Pharm Pharm Sci. 2014;17(1):25-33. doi: 10.1128/AAC.02818-14. Epub 2014 May 5.
    3: Atkins HS, Spencer S, Brew SD, Jenner DC, Sefton AM, MacMillan AP, Brooks TJ, Simpson AJ. Evaluation of azithromycin, trovafloxacin and grepafloxacin as prophylaxis against experimental murine Brucella melitensis infection. Int J Antimicrob Agents. 2010 Jul;36(1):66-8. doi: 10.1016/j.ijantimicag.2009.10.003. Epub 2009 Dec 21.

    合成参考文献


    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    参考文献:10.2165/00003495-199957060-00002
    摘要:Momméja-Marin H, Carbon C. What is the place of fluoroquinolones in the treatment of community-acquired respiratory tract infections Drugs. 1999 Jun;57(6):851–3. doi: 10.2165/00003495-199957060-00002.
    参考文献:10.1191/096032799678840237
    摘要:Takizawa T, Hashimoto K, Minami T, Yamashita S, Owen K. The comparative arthropathy of fluoroquinolones in dogs. Hum Exp Toxicol. 1999 Jun;18(6):392–9. doi: 10.1191/096032799678840237.
    参考文献:10.1016/s0924-8579(99)00057-6
    摘要:Roblin PM, Kutlin A, Reznik T, Hammerschlag MR. Activity of grepafloxacin and other fluoroquinones and newer macrolides against recent clinical isolates of Chlamydia pneumoniae. International Journal of Antimicrobial Agents. 1999 Jul;12(2):181–4. doi: 10.1016/s0924-8579(99)00057-6.
    参考文献:10.1007/s101560200000
    摘要:Niki Y. Pharmacokinetics and safety assessment of tosufloxacin tosilate. J Infect Chemother. 2002 Mar;8(1):1–18. doi: 10.1007/s101560200000.
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