CAS: 91524-15-1; 1-Ethyl-6-Fluoro-4-Oxo-7-(1H-Pyrrol-1-yl)-1,4-Dihydroquinoline-3-Carboxylic Acid
该化合物是合成的氟己酮抗生素,具有广泛频谱抗菌活性,主要用于治疗各种细菌感染,特别是由克己体和某些克己体引起的感染;复合功能是抑制细菌DNA gylass和Topo异构体aseIV,这些酶对于DNA复制和转录至关重要,从而防止细菌细胞分解和生长;Irloxain的特点是水和有机溶剂溶解性相对较高,有利于生物系统的吸收和分布;该物质一般是白色到非白晶体化粉;其药用动力学特性包括良好的口服生物利用率,半衰期可以方便地服用剂量治疗;然而,与其他氟丙酮一样,Irloxain素可能与潜在的副作用有关,包括气态肠扰动,...
- 英文名称1-Ethyl-6-Fluoro-4-Oxo-7-(1H-Pyrrol-1-yl)-1,4-Dihydroquinoline-3-Carboxylic Acid
- 中文名称伊洛沙星
- IUPAC名称1-ethyl-6-fluoro-4-oxo-7-(1H-pyrrol-1-yl)-1,4-dihydroquinoline-3-carboxylic acid
- 其它别名Irloxacin; Pirfloxacin; 1-Ethyl-6-Fluoro-1,4-Dihydro-4-Oxo-7-(1H-Pyrrol-1-Yl)-3-Quinolinecarboxylic Acid; 1-Ethyl-6-Fluoro-1,4-Dihydro-4-Oxo-7-(1H-Pyrrol-1-Yl)Quinoline-3-Carboxylic Acid; Irloxacin Usp/ep/bp; Inhibitor,Acid Ph,Antibacterial Agent,Bacterial,Gram-Positive,Oral,Irloxacin,Pirfloxacin,Gram-Negative Bacteria,Inhibit; 3-Quinolinecarboxylic Acid, 1-Ethyl-6-Fluoro-1,4-Dihydro-4-Oxo-7-(1H-Pyrrol-1-Yl)-
- CAS编号91524-15-1
- MFCD编号:MFCD00868661
- FDA UNII编号:36SG77D21B
- 分子式:C16H13FN2O3分子量:300.29
- 产品CID: 1951966
- 同类组份化合物CAS122949-49-9 (sodium)91524-15-1 (free acid)
- 产品分类原料药 → 人工合成抗感染类药 → 喹诺酮类药
物理性质
- 熔点252-255 °C(溶剂: N,N-dimethylformamide (68-12-2))
- 沸点495.9 °C at 760mmHg
- 闪点253.7 °C
- 密度1.36g/cm3
- pKa:-0.07±0.20(预测)
- PSA:64.23
- LogP:2.6494
- 折射率1.634
- 蒸汽压1.18E-10 mmHg at 25 °C
- 溶解性DMSO:0.0(Max Conc. mg/mL);0.0(Max Conc. Mm)
- 外观形态白色至类白色固体
- 储存条件储存在 -20°C
- 产品应用该化合物是一种新的五氯酮衍生物,并显示使用酸PH的活性更大.它具有良好的活性抗体抗微生物光谱,对克阳性和克阴性细菌具有抗体细胞作用.将IRLOGUSININ的体外活性对抗甲状腺(20 M.肺结核,17 M. AVIUM,5 MYCOBACTERIUM BOVIS,5 MICOBCITRIUM CHELONAE,5 MECOBECTRIUM FORITUM和1 MICOBACTRIUM GADIUM)进行了比较(20 M. 肺结核, 17 M AV. AILLUM, 5 5,5 PELOXIN 和 2753 RP).所有在PH6.8和5.0 5 PH. 5的IRLOXIN CINAC 都对M. AVUM有更大的活动.
MSDS等安全信息
上下游产品
CAS号696-59-3 2,5-二甲氧基四氢呋喃 | CAS号75001-63-7 7-amino-1-ethyl... | CAS号73510-05-1 dimethoxytetrah... | CAS号454-07-9 N-(2-氟-5-硝基苯基)乙酰胺 | CAS号369-36-8 2-氟-5-硝基苯胺 | CAS号96623-75-5 1-(2-氟-5-硝基苯基)-1H-吡咯 | CAS号75001-47-7 N-(5-氨基-2-氟苯基)乙酰胺合成工艺路线路线简述
- 合成目标产物 Irloxacin 主要起始原料 3-Quinolinecarboxylic Acid, 1-Ethyl-6-Fluoro-1,4-Dihydro-4-Oxo-7-(1H-Pyrrol-1-yl)-, Ethyl Ester
- 696-59-3 + 75001-63-7 = 91524-15-1 [标题:Reaction Conditions
标题:Studies On Antibacterial And Antifungal Agents. Note Vi. Pirfloxacin And Related Compounds: Synthetic And Microbiological Studies
作者:Artico,M.; Et Al
参考文献:Farmaco 日期:1986 卷标:41(5) 页码:366-80]
91188-89-5 + 696-59-3 = 91524-15-1
反应条件:1.1 Solvents: Acetic Acid
标题:New Structure-Activity Relationships Of The Quinolone Antibacterials Using The Target Enzyme. The Development And Application Of A Dna Gyrase Assay
作者:Domagala,John M.; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:1986 卷标:29(3) 页码:394-404]
91188-89-5 + 696-59-3 = 91524-15-1 [标题:Reaction Conditions
标题:Studies On Antibacterial And Antifungal Agents. Note Vi. Pirfloxacin And Related Compounds: Synthetic And Microbiological Studies
作者:Artico,M.; Et Al
参考文献:Farmaco 日期:1986 卷标:41(5) 页码:366-80]
96623-79-9 = 91524-15-1 [标题:Reaction Conditions
标题:1-Ethyl-6-Fluoro-1,4-Dihydro-4-Oxo-7-(1H-Pyrrol-1-Yl)Quinoline-3-Carboxylic Acid,A New Fluorinated Compound Of Oxacin Family With High Broad-Spectrum Antibacterial Activities
作者:Stefancich,G.; Et Al
参考文献:Farmaco 日期:1985 卷标:40(4) 页码:237-48]
96623-79-9 = 91524-15-1 [标题:Reaction Conditions
标题:Studies On Antibacterial And Antifungal Agents. Note Vi. Pirfloxacin And Related Compounds: Synthetic And Microbiological Studies
作者:Artico,M.; Et Al
参考文献:Farmaco 日期:1986 卷标:41(5) 页码:366-80]
696-59-3 + 75001-63-7 = 91524-15-1 [标题:Reaction Conditions
标题:Synthesis Of Antimicrobial Agents. 1. Syntheses And Antibacterial Activities Of 7-(Azole Substituted)Quinolones
作者:Uno,Toshio; Et Al
参考文献:Journal Of Medicinal Chemistry 日期:1987 卷标:30(12) 页码:2163-9]
= 91524-15-1 [标题:Reaction Conditions
标题:Process For The Preparation Of 1-Ethyl-6-Fluoro-7-(1-Pyrrolo)-1,4-Dihydro-4-Oxo-3-Quinolinecarboxylic Acid
参考文献:Spain]
96623-78-8 = 91524-15-1
反应条件:1.1 Solvents: Dimethylformamide2.1 -
标题:1-Ethyl-6-Fluoro-1,4-Dihydro-4-Oxo-7-(1H-Pyrrol-1-Yl)Quinoline-3-Carboxylic Acid,A New Fluorinated Compound Of Oxacin Family With High Broad-Spectrum Antibacterial Activities
作者:Stefancich,G.; Et Al
参考文献:Farmaco 日期:1985 卷标:40(4) 页码:237-48
📜1-(2-氟-5-硝基苯基)-1H-吡咯置于rh/al2O3 Sodium Hydroxide,氢气,Potassium Carbonate体系中,用 二苯醚,乙醇,水,N,N-二甲基甲酰胺 作为反应溶剂,90.0 °C,405.3 Kpa 条件下,反应 5.5H,反应生成 伊洛沙星
参考文献:Stefancich; Artico; Corelli,Farmaco,Edizione Scientifica,1985,Vol. 40,# 4,P. 237-248
标题:Stefancich; Artico; Corelli,Farmaco,Edizione Scientifica,1985,Vol. 40,# 4,P. 237-248
海关参考信息
- 2905110000-甲醇
2912110000-甲醛
2915110000-甲酸
2933310010-吡啶 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:CN-116348465-A
优先权日:2020-07-28
标 题:Chiral Synthesis of Fused Bicyclic RAF Inhibitors
专利号:CN-119638694-A
优先权日:2018-11-16
标 题 :Improved synthesis of key intermediates for KRAS G12C inhibitor compounds
专利号:CN-114728960-B
优先权日:2019-11-14
标 题:Improved synthesis of KRAS G12C inhibitor compounds
专利号:CN-113015724-B
优先权日:2018-11-16
标题 :Improved synthesis of key intermediates for KRAS G12C inhibitor compounds
专利号:CN-119638693-A
优先权日:2018-11-16
标 题 :Improved synthesis of key intermediates for KRAS G12C inhibitor compounds
专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人：FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.
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品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Yang M, Yang Y, Lei M, Ye C, Zhao C, Xu J, Wu K, Yu M. Experimental studies on soft contact lenses for controlled ocular delivery of pirfinedone: in vitro and in vivo. Drug Deliv. 2016 Nov;23(9):3538-3543. doi: 10.1080/10717544.2016.1204570. Epub 2016 Jul 17. 93(4):405-11. doi: 10.1016/j.tube.2013.02.017. Epub 2013 Mar 22. 53(2):121-5. doi: 10.1055/s-0031-1297082. 50(5):485-94. doi: 10.1055/s-0031-1300234. 49(5):448-56. doi: 10.1055/s-0031-1300441. 41(3):204-7. doi: 10.1159/000239345. 26(3):381-6. doi: 10.1093/jac/26.3.381. 34(6):1262-7. doi: 10.1128/AAC.34.6.1262.
9: Massa S, Corelli F, Mai A, Artico M, Panico S, Simonetti N. Research on antibacterial and antifungal agents. XI. New antibacterial quinolones related to pirfloxacin. Farmaco. 1989 Sep;44(9):779-93. 6(2 Suppl):152-3. 13(2):75-7. 41(5):366-80. Italian. 40(4):237-48.
合成参考文献
摘要:Arzneimittel-Forschung. Drug Research., 49(448), 1999 []
参考文献:10.1021/jm00153a015
摘要:Domagala JM, Hanna LD, Heifetz CL, Hutt MP, Mich TF, Sanchez JP, Solomon M. New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay. J Med Chem. 1986 Mar;29(3):394–404. doi: 10.1021/jm00153a015.
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