CAS: 110871-86-8; 5-Amino-1-Cyclopropyl-7-((3S,5R)-3,5-Dimethylpiperazin-1-yl)-6,8-Difluoro-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

该化合物是一种合成抗生素,属于氟丙酮类,主要用于治疗细菌感染;其化学结构具有双环核核心,含有氟原子,可增强抗菌活性; 肉毒杆菌表现出对乳腺阳性细菌和腺阴性细菌的广谱性活动,使其对呼吸道感染,皮肤感染和某些种类的尿道感染有效; 行动机制包括抑制细菌DNA甘蓝酶和对抗生素异构体酶IV,对DNA复制和修复至关重要的酶; 众所周知,肉毒杆菌具有有利的药用基因特性,包括口服生物利用率高和相对较长的半衰期,允许每天一次服用. 但是,与其他氟丙酮一样,它可能与副作用有关,如胃肠扰动,...

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号103772-14-1 5-Amino-l-Cyclo... | CAS号21655-48-1 顺式-2,6-二甲基哌嗪 | CAS号107564-02-3 1-cyclopropyl-5... | CAS号110872-04-3 ethyl 5-(benzyl... | CAS号103772-13-0 1-环丙基-5-酰胺-6,7,...

合成工艺路线路线简述

  • 合成目标产物 Sparfloxacin 主要起始原料 1-Cyclopropyl-5-Amido-6,7,8-Trifluoro-1,4-Dihydro-4-Oxo-3- Quinolinecarboxylic Acid Ethyl Ester
  • (文献来源)合成步骤主要原料 1-Cyclopropyl-5-Amido-6,7,8-Trifluoro-1,4-Dihydro-4-Oxo-3- Quinolinecarboxylic Acid Ethyl Ester

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-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-10308663-B2
优先权日:2015-06-16
标题:Inhibitors of PTP4A3 for the treatment of cancer
发明人:LAZO JOHN S; SHARLOW ELIZABETH R; MCQUEENEY KELLEY E; WIPF PETER; SALAMOUN JOSEPH M
权利人:LAZO JOHN S; SHARLOW ELIZABETH R; MCQUEENEY KELLEY E; WIPF PETER; SALAMOUN JOSEPH M; UNIV VIRGINIA PATENT FOUNDATION; UNIV OF PITTSBURGH —OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
摘要:The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesis of protein tyrosine phosphatase inhibitor and precursor compound thienopyridone (5).

专利号:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人:CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

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-10933051-B2
优先权日:2017-06-09
标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
权利人:FOB SYNTHESIS INC
摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
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主要参考文献


1: Schentag JJ. Sparfloxacin: a review. Clin Ther. 2000 Apr;22(4):372-87; discussion 371. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Japanese. Review. Review.

合成参考文献


参考文献:10.2147/copd.s21071
摘要:Wilson R, Anzueto A, Miravitlles M, Arvis P, Faragó G, Haverstock D, Trajanovic M, Sethi S. A novel study design for antibiotic trials in acute exacerbations of COPD: MAESTRAL methodology. Int J Chron Obstruct Pulmon Dis. 2011;6():373–83.
参考文献:10.4061/2011/712369
摘要:Dhama K, Mahendran M, Tiwari R, Dayal Singh S, Kumar D, Singh S, Sawant PM. Tuberculosis in Birds: Insights into theMycobacterium aviumInfections. Veterinary Medicine International. 2011;2011():1–14. doi: 10.4061/2011/712369.
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