CAS: 98105-99-8; 6-Fluoro-1-(4-Fluorophenyl)-4-Oxo-7-(Piperazin-1-yl)-1,4-Dihydroquinoline-3-Carboxylic Acid

该化合物是一种合成的氟己酮抗生素,其抗菌活性很强,能够防止广泛的克格朗阴性病原体和一些克格伦阳性病原体,其行动机制包括抑制细菌DNAgyras和TOpo异构体4,干扰DNA复制和转录.萨拉福克斯辛表现出高度的生物利用率和有效组织渗透,使其在兽医医学中特别有用,用于治疗家禽和牲畜的呼吸道,胃肠道和尿道感染.该化合物在不同的环境条件下表现出稳定性,在适当使用时抗药性低.其药性特征支持每日服用一次,加强临床应用的合规性.萨拉福克斯辛通常通过饮用水或注射进行,确保农业环境中的实用性.

结构式图片

上下游产品

7-(4-Ethoxycarbonyl-piperazin-1-yl)-6-fluoro-1-(4-fluoro-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid piperazine 6,7-difluoro-1-(4-fluorophenyl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid ethyl 2,4,5-trifluorobenzoylacetate1-(p-fluorophenyl)-6-fluoro-7-(4-butyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid naringenin-ethylidene-sarafloxacin apigenin-ethylidene-sarafloxacin genistin-ethylidene-sarafloxacin

合成工艺路线路线简述

    2-(2,4-二氯-5-氟苯甲酰基)-3-乙氧基丙烯酸乙酯置于sodium Hydroxide,Sodium Hydride体系中,用 四氢呋喃,乙二醇二甲醚,乙醇,二氯甲烷 作为反应溶剂,化学反应 33.0H,反应生成 沙拉沙星
    参考文献:Synthesis And Structure-Activity Relationships Of Novel Arylfluoroquinolone Antibacterial Agents
    标题:Synthesis And Structure-Activity Relationships Of Novel Arylfluoroquinolone Antibacterial Agents
    摘要:A Series Of Novel Arylfluoroquinolones Has Been Prepared. These Derivatives Are Characterized By Having A Fluorine Atom At The 6-Position,Substituted Amino Groups At The 7-Position,And Substituted Phenyl Groups At The 1-Position. Structure-Activity Relationship (Sar) Studies Indicate That The In Vitro Antibacterial Potency Is Greatest When The 1-Substituent Is Either P-Fluorophenyl Or P-Hydroxyphenyl And The 7-Substituent Is Either 1-Piperazinyl,4-Methyl-1-Piperazinyl,Or 3-Amino-1-Pyrrolidinyl. The Electronic And Spatial Properties Of The 1-Substituent,As Well As The Steric Bulk,Play Important Roles In The Antimicrobial Potency In This Class Of Antibacterials. As A Result Of This Study,Compounds 45 And 41 Were Found To Possess Excellent In Vitro Potency And In Vivo Efficacy.
    DOI:10.1021/jm00149A003

    海关参考信息

    专利信息


    专利号:US-2025179012-A1
    优先权日:2022-03-04
    标 题:Synthesis of sulfur(vi) compounds and reagents for same
    发明人:LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY
    权利人:H LEE MOFFITT CANCER CT & RES
    摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.

    专利号:WO-2025101716-A1
    优先权日:2023-11-07
    标题:Processes for synthesis of trifunctionalized sulfur(vi) compounds
    发明人:LOPCHUK JUSTIN; SHULTZ ZACHARY; ATHAWALE PARESH
    权利人:H LEE MOFFITT CANCER CT & RES
    摘要:This disclosure describes processes for the asymmetric synthesis of trifunctionalized sulfur(VI) containing organic compounds of Formula I and Formula VI, as well as compounds of Formula I and Formula VI prepared by the processes 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-2009054643-A1
    优先权日:2007-05-24
    标 题:Novel method of synthesis of fluoroquinolones

    专利号:WO-2023168108-A2
    优先权日:2022-03-04
    标 题 :Synthesis of sulfur(vi) compounds and reagents for same
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    主要参考文献


    1: Evaluation of certain veterinary drug residues in food. Fiftieth report of the joint FAO/WHO Expert Committee on Food Additives. World Health Organ Tech Rep Ser. 1999;888:i-vii, 1-95. Review. Review.

    合成参考文献


    参考文献:10.1080/19440049.2011.587028
    摘要:Takeda N, Gotoh M, Matsuoka T. Rapid screening method for quinolone residues in livestock and fishery products using immobilised metal chelate affinity chromatographic clean-up and liquid chromatography-fluorescence detection. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2011 Sep;28(9):1168–74. doi: 10.1080/19440049.2011.587028.
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