CAS: 112398-08-0; 1-Cyclopropyl-6-Fluoro-7-((1S,4S)-5-Methyl-2,5-Diazabicyclo[2.2.1]Heptan-2-yl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

该化合物是合成的氟己酮抗生素,其有效杀菌活动针对广泛的克丁阴性病原体和某些克丁阳性病原体,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;Danofloxin展示了良好的组织渗透和长期消除半衰期,确保了持续的治疗浓度;它特别有效,能够防止兽医药物中的呼吸道和肠道感染,并表现出对抗巴斯德罗拉,Mycopslasma和Escherchicha coli的功效;该化合物的抗药性发展倾向性低,而且具有有利的药用动能特征,因此它成为有针对性的抗微生物疗法的可靠选择;其稳定性和溶解性进一步增强了各种管理途径的多功能.

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CAS号93107-30-3 1-环丙基-6,7-二氟-1,...

合成工艺路线路线简述

    📜1-环丙基-6,7-二氟-1,4-二氢-4-氧喹啉-3-羧酸,2-Methyl-2,5-Diazabicyclo[2.2.1]Heptane Dihydrochloride置于吡啶,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,化学反应 2.0H,以81%的收率获得达诺沙星
    参考文献:7-二氮杂双环烷基喹诺酮类化合物的合成与构效关系,包括一种新的兽药喹诺酮类抗菌药物达诺沙星.
    标题:7-二氮杂双环烷基喹诺酮类化合物的合成与构效关系,包括一种新的兽药喹诺酮类抗菌药物达诺沙星.
    摘要:一系列被各种c8(h,F,Cl,N)和n1(乙基,环丙基,乙烯基,2-氟乙基,4-氟苯基,2,4-二氟苯基)取代基取代的新颖的6-氟-7-二氮杂双环烷基喹诺酮羧酸,以及9-氟-10-二氮杂双环烷基吡啶并苯并恶嗪羧酸,并针对一系列重要的兽医病原菌进行了抗菌活性评估.在7位(苯并恶嗪10位)研究的二氮杂双环烷基侧链包括(1S,4S)-5-甲基-2,5-二氮杂双环[2.2.1]庚烷(2),(1S,4S)-2,5-二氮杂双环[2.2.1]庚烷(3),(1R,4R)-5-甲基-2,5-二氮杂双环[2.2.1]庚烷(4),8-甲基-3,8-二氮杂双环[3.2. 1]辛烷(5),9-甲基-3,9-二氮杂双环[4.2.1]壬烷(6),1,4-二氮杂双环[3.2.2]壬烷(7),1,4-二氮杂双环[3.3.1] ]壬烷(8)和9-甲基-3,9-二氮杂双环[3.3.1]壬烷(9).在这些侧链中,体外效能不是
    Doi:10.1021/jm00082A001

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    专利号:US-11274081-B2
    优先权日:2016-05-30
    标 题:Process for the synthesis of ivacaftor
    发明人:REDDY DUMBALA SRINIVASA; KULKARNI AMOL ARVIND; NATARAJAN VASUDEVAN; SHARMA MRITYUNJAY KESHAVPRASAD
    权利人:COUNCIL SCIENT IND RES
    摘要:The present disclosed an improved process for the synthesis of ivacaftor starting from indole acetic acid ester which can be performed in batch as well as continuous flow synthesis. The present invention further disclosed to a continuous process for the synthesis of compound of formula (II) or formula (III) from compound of formula (I) in continuous flow reactor.

    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:CN-102962041-B
    优先权日:2012-11-07
    标题 :Preparation method and application of microwave-assisted synthesis of chlorine-doped surface molecularly imprinted photocatalysts

    专利号:CN-102962041-A
    优先权日:2012-11-07
    标 题:Preparation method and application of microwave-assisted synthesis of chlorine-doped surface molecularly imprinted photocatalysts

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    主要参考文献


    1: Klein U, de Jong A, Moyaert H, El Garch F, Leon R, Richard-Mazet A, Rose M, Maes D, Pridmore A, Thomson JR, Ayling RD. Antimicrobial susceptibility monitoring of Mycoplasma hyopneumoniae and Mycoplasma bovis isolated in Europe. Vet Microbiol. 2017 May;204:188-193. doi: 10.1016/j.vetmic.2017.04.012. Epub 2017 Apr 14. doi: 10.1136/vr.103964. Epub 2017 Feb 17. doi: 10.1002/elps.201600475. Epub 2017 Mar 6. doi: 10.1016/j.rvsc.2016.11.005. Epub 2016 Nov 6. doi: 10.1007/s11356-017-8409-7. Epub 2017 Jan 20. doi: 10.1177/1040638716683212. Epub 2017 Jan 8. doi: 10.1371/journal.pone.0169134. eCollection 2017.
    8: Santoke H, Cooper WJ. Environmental photochemical fate of selected pharmaceutical compounds in natural and reconstituted Suwannee River water: Role of reactive species in indirect photolysis. Sci Total Environ. 2017 Feb 15;580:626-631. doi: 10.1016/j.scitotenv.2016.12.008. Epub 2016 Dec 20. doi: 10.1016/j.foodchem.2016.11.029. Epub 2016 Nov 8. doi: 10.1016/j.diagmicrobio.2016.07.020. Epub 2016 Jul 27. doi: 10.1111/jvp.12346. Epub 2016 Jul 31. doi: 10.1016/j.jpba.2016.06.001. Epub 2016 Jun 4. doi: 10.1080/19440049.2016.1184051. Epub 2016 Jun 9. doi: 10.3168/jds.2015-10593. Epub 2016 May 4. doi: 10.1016/j.placenta.2015.12.005. Epub 2015 Dec 12. German. doi: 10.1021/acs.jafc.5b02343. Epub 2015 Aug 4. Chinese. doi: 10.1016/j.ijantimicag.2015.04.008. Epub 2015 May 28. doi: 10.1016/j.chroma.2015.05.070. Epub 2015 Jun 5.

    合成参考文献


    摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
    摘要:https://www.sciencedirect.com/science/article/abs/pii/S0003267018311693
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