CAS: 74011-58-8; 1-Ethyl-6-Fluoro-4-Oxo-7-(Piperazin-1-yl)-1,4-Dihydro-1,8-Naphthyridine-3-Carboxylic Acid

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CAS号110-85-0 哌嗪 | CAS号114171-68-5 1-ethyl-6-fluor... | CAS号23651-62-9 ethyl N-ethyl-b... | CAS号82671-02-1 3-氰基-2,6-二氯-5-氟吡啶 | CAS号96568-25-1 2,5-difluoro-6-... | CAS号108108-37-8 2,5-difluoro-6-... | CAS号114190-30-6 1-ethyl-6-fluor... | CAS号87939-13-7 1-ETHYL-6-FLUOR... | CAS号74274-68-3 1-ethyl-6-fluor...

7-(4-Ethoxycarbonyl-1-Piperazinyl)-1-Ethyl-6-Fluoro-1,4-Dihydro-4-Oxo-1,8-Naphthyridine-3-Carboxylic Acid置于sodium Hydroxide体系中,用 乙醇 作为反应溶剂,化学反应 4.0H,以87%的收率获得产物依诺沙星
参考文献:通过balz-Schiemann反应合成氟化吡啶.新型抗菌性吡啶酮羧酸依诺沙星的替代途径†
标题:通过balz-Schiemann反应合成氟化吡啶.新型抗菌性吡啶酮羧酸依诺沙星的替代途径†
摘要:描述了通过balz-Schiemann反应对2,6-二取代的3-氨基吡啶5和12的氟化.2,6-二氯-3-Pyridinediazonium四氟硼酸盐(6)和2-取代的6-乙酰氨基-3-Pyridinediazonium四氟硼酸盐13用或不用溶剂加热,得到相应的氟化吡啶7和14分别,以非常好产率.通过已知方法将2-取代的6-乙酰氨基-3-氟吡啶(14)转化为一系列的7-取代的1-乙基-6-氟-1,4-二氢-4-氧代-1,8-萘啶-3-羧酸21包括新的潜在抗菌剂依诺沙星[1-乙基-6-氟-1,4-二氢-4-氧代-7-(1-哌嗪基)-1,8-萘啶-3-羧酸[(2)] .
DOI:10.1002/jhet.5570210309

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-2024035023-A1
优先权日:2022-06-24
标题 :Computer implemented method for engineering fluorinase enzymes for synthesis of fluorophenyl compounds
发明人：R PRAVIN KUMAR; G GLADSTONE SIGAMANI; L ROOPA; B K NAVEEN; SHETTY ANUJ J; M LIKITH
权利人:KCAT ENZYMATIC PRIVATE LTD
摘要:The present invention discloses a computer-implemented method for engineering fluorinase enzymes towards the synthesis of fluorophenyl compounds. Limited or no mechanistic details of fluorinase enzymes have hindered progress in understanding their catalytic mechanisms for synthesizing synthetic organofluorine compounds. Through a comprehensive computational screening process, specific methionine-sulfonium phenyl substrates, including [(3S)-3-amino-3-carboxypropyl][2,5-difluoro-4-(4-methoxy-2,4-dioxobutyl)phenyl]methylsulfonium, were designed and optimized using quantum chemical optimization techniques. This methodology uncovers crucial information on F— ion attack conformation and the catalytic mechanism of the substrate, leading to the formation of Methyl 3-oxo-4-(2,4,5-trifluorophenyl)butanoate. Furthermore, a protein sequence and 3D modeling-based enzyme screening process was employed to identify the most suitable enzyme for this substrate. The identified enzyme was then engineered using the mechanistic insights gained from the studies, resulting in improved substrate scope, stability and catalytic efficiency. This computer-based approach offers an efficient and precise alternative to traditional trial-and-error methods, advancing the field towards the successful synthesis fluorophenyl compounds.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

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:WO-9611194-A1
优先权日:1994-10-06
标题:Pyridonecarboxylic acid derivative and intermediate for the synthesis of the same
发明人：OKADA HIDETSUGU; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA
权利人:DAINIPPON PHARMACEUTICAL CO; OKADA HIDETSUGU; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA
摘要:A pyridonecarboxylic acid derivative represented by general formula (I), an ester and a salt thereof, an antibacterial agent containing the same, and a bicyclic amine compound serving as a direct intermediate for the synthesis of the pyridonecarboxylic acid derivative, wherein R represents cycloalkyl, optionally substituted phenyl, etc.; G represents carbon, etc.; A represents C-Z (Z being hydrogen, halogeno, lower alkoxy, etc.) or nitrogen; X represents hydrogen, amino, etc.; Y represents hydrogen or halogeno; m is an integer of 1 to 3; and W represents -(CH2)nN(R1)R2 (R1 and R2 being the same or different and each representing hydrogen, lower alkyl, etc., and n being an integer of 0 or 1).

专利号:US-7211590-B2
优先权日:2002-08-01
标 题:Nitrosated proton pump inhibitors, compositions and methods of use
发明人：FANG XINQIN; GARVEY DAVID S; LETTS L GORDON
权利人:NITROMED INC
摘要:The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated proton pump inhibitor compound, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.