CAS: 100490-36-6; 7-(3-Aminopyrrolidin-1-yl)-1-(2,4-Difluorophenyl)-6-Fluoro-4-Oxo-1,4-Dihydro-1,8-Naphthyridine-3-Carboxylic Acid

该化合物是一种氟己酮抗生素,其抗药性广泛,对克伦阳性细菌和克伦正阴性细菌具有抗药性,其行动机制包括抑制细菌DNA gyrase 和topo异构体4,有效地干扰了DNA复制和转录;Tosufloxain表现出对呼吸道,尿道和软组织感染,包括抗药性菌株感染的功效;该化合物表现出有利的药效,口服生物利用率和组织渗透率良好;它加强了对克伦阳性生物体(如肺炎链球菌)的防治活动,将其与以前的氟丙酮区分开来;Tusufloxainci素也因其稳定性,与常见的抗菌抗药机制相抗,因此值得注意;临床研究支持在其他抗生素可能不那么有效的地方使用该物质治疗感染;适当使用需要考虑到细菌和病人特有的因素.

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7-(3-Aminopyrrolidin-1-yl)-1-(2,4-Difluorophenyl)-6-Fluoro-4-Oxo-1,4-Dihydro-[1,8]Naphthyridine 3-Carboxylic Acid Ethyl Ester

合成工艺路线路线简述

    📜7-(3-Aminopyrrolidin-1-yl)-1-(2,4-Difluorophenyl)-6-Fluoro-4-Oxo-1,4-Dihydro-[1,8]Naphthyridine 3-Carboxylic Acid Ethyl Ester 反应生成甲苯磺酸妥舒沙星
    参考文献:Todo,Jodzo;Yamafudzi,Tehtsuo;Minamikumo,Katsuyuki;Kitayama,Isio;Nagak+
    标题:Todo,Jodzo;Yamafudzi,Tehtsuo;Minamikumo,Katsuyuki;Kitayama,Isio;Nagak+

    海关参考信息

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:US-11332444-B2
    优先权日:2018-04-25
    标题:Method for the hydrolysis of quinolonecarboxylic esters
    发明人:FEY PETER; BERWE MATHIAS; WIRTHS Joerg; WISCHNAT RALF; LONGERICH MARKUS; DIETZEL ANTJE
    权利人:BAYER ANIMAL HEALTH GMBH
    摘要:Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I):The method comprises the step A):A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and waterIn step A), ≥30 to ≤40 mol of acetic acid, ≥0.3 to ≤1 mol of sulfuric acid and ≥0.9 to ≤2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.

    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-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    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-2010203587-A1
    优先权日:2009-01-13
    标 题:Use of dna gyrase inhibitors for in vitro polypeptide synthesis reactions
    发明人:VOLOSHIN ALEXEI M; ZAWADA JAMES F; GOLD DANIEL
    权利人:SUTRO BIOPHARMA INC
    摘要:The present invention provides methods and compositions useful for in vitro polypeptide synthesis reactions. The methods involve the use of DNA gyrase inhibitors to prevent bacterial contamination in lysates used for in vitro production of polypeptides. The compositions include contamination-free cell lysates for in vitro protein synthesis reactions.

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    主要参考文献


    1: Kim YD, Kim MK, Wee WR, Choi HJ. Tosufloxacin deposits in compromised corneas. Optom Vis Sci. 2014 Sep;91(9):e241-4. doi: 10.1097/OPX.0000000000000348. doi: 10.1128/AAC.00048-13. Epub 2013 Mar 4.
    3: Niu H, Cui P, Yee R, Shi W, Zhang S, Feng J, Sullivan D, Zhang W, Zhu B, Zhang Y. A Clinical Drug Library Screen Identifies Tosufloxacin as Being Highly Active against Staphylococcus aureus Persisters. Antibiotics (Basel). 2015 Jul 31;4(3):329-36. doi: 10.3390/antibiotics4030329.
    4: Matsubara R, Kibe T, Nomura T. Crystalline nephropathy caused by tosufloxacin. Pediatr Int. 2016 Nov;58(11):1219-1221. doi: 10.1111/ped.13116. Therapeutic efficacy of azithromycin, clarithromycin, minocycline and tosufloxacin against macrolide-resistant and macrolide-sensitive Mycoplasma pneumoniae pneumonia in pediatric patients. PLoS One. 2017 Mar 13;12(3):e0173635. doi: 10.1371/journal.pone.0173635. eCollection 2017.

    合成参考文献


    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.
    参考文献:10.1007/s101560200001
    摘要:Kohno S. Clinical assessment of tosufloxacin tosilate. J Infect Chemother. 2002 Mar;8(1):19–27. doi: 10.1007/s101560200001.
    参考文献:10.1007/s101560200003
    摘要:Niki Y, Watanabe S, Yoshida K, Miyashita N, Nakajima M, Matsushima T. Effect of pazufloxacin mesilate on the serum concentration of theophylline. J Infect Chemother. 2002 Mar;8(1):33–6. doi: 10.1007/s101560200003.
    参考文献:10.1007/s101560200019
    摘要:Miyashita N, Fukano H, Yoshida K, Niki Y, Matsushima T. In-vitro activity of moxifloxacin and other fluoroquinolones against Chlamydia species. J Infect Chemother. 2002 Mar;8(1):115–7. doi: 10.1007/s101560200019.
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