CAS: 105956-97-6; 7-(3-Aminopyrrolidin-1-yl)-8-Chloro-1-Cyclopropyl-6-Fluoro-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

上下游产品

7-[(3-t-Butoxycarbonylamino)-1-pyrrolidinyl]-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid 8-chloro-1-cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid 1,4-diaza-bicyclo[2.2.2]°Ctane pyrrolidin-3-amine 28H26ClF3N6O4C28H26ClF3N6O4 8-chloro-1-cyclopropyl-7-(3-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propylamino)pyrrolidin-1-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 28H26Cl3FN6O4C28H26Cl3FN6O4

8-氯-1-环丙基-6,7-二氟-1,4-二氢-4-氧代-3-喹啉羧酸置于盐酸,溶剂黄146,三乙胺体系中,用 乙腈 用作溶剂,化学反应 25.0H,反应生成克林沙星
参考文献:喹诺酮类抗菌剂.8-取代的喹啉-3-羧酸和1,8-萘啶-3-羧酸的合成及构效关系.
标题:喹诺酮类抗菌剂.8-取代的喹啉-3-羧酸和1,8-萘啶-3-羧酸的合成及构效关系.
摘要:一系列7,8-二取代的1-环丙基-6-氟喹啉-3-羧酸,7-取代的1-环丙基-6-氟-1,8-萘啶-3-羧酸和10-取代的9-氟吡啶并苯并恶嗪已经制备了-6-羧酸并评估了其抗菌活性.在7-位(苯并恶嗪10-位)检测的侧链包括哌嗪基(g),3-氨基吡咯烷基(a),3-(氨基甲基)吡咯烷基(b)和烷基化的3-(氨基甲基)吡咯烷基(cf).喹诺酮环系统c-8的变异包括氢,硝基,氨基,氟和氯.8氢喹诺酮和1,8-萘啶上侧链对革兰氏阴性生物的体外活性的相对增强比cf更大,B更大,G更大.由8个取代基赋予取代的喹诺酮核的活性的顺序为:F大于cl大于萘啶大于h大于苯并恶嗪大于nh2大于no2.这些趋势在体内得以保留.
Doi:10.1021/jm00400A016

专利信息

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-4885386-A
优先权日:1988-10-28
标题 :Process for the synthesis of 3-chloro-2,4,5-trifluorobenzoic acid
发明人：WEMPLE JAMES N; KARRICK GREGORY L; SPENCE FLOYD G
权利人:WARNER LAMBERT CO
摘要:An improved process for the preparation of 3-chloro-2,4,5-trifluorobenzoic acid is described which involves reaction of a diester of 3,4,5,6-tetrafluoro-1,2-benzenedicarboxylic acid with a substituted amine to afford 3-amino-2,4,5-trifluorobenzoic acid followed by subsequent conversion of the amio intermediate into 3-chloro-2,4,5-trifluorobenzoic acid.

专利号:US-9693999-B2
优先权日:2011-01-26
标题:Small molecule RNase inhibitors and methods of use
发明人：DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

专利号:US-8399502-B2
优先权日:2008-09-17
标 题 :Analogs of indole-3-carbinol and their use as agents against infection
发明人：JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN
权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT
摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

专利号:US-2010203587-A1
优先权日:2009-01-13
标 题:Use of dna gyrase inhibitors for in vitro polypeptide synthesis reactions
发明人：VOLOSHIN ALEXEI M; ZAWADA JAMES F; GOLD DANIEL
权利人:SUTRO BIOPHARMA INC
摘要:The present invention provides methods and compositions useful for in vitro polypeptide synthesis reactions. The methods involve the use of DNA gyrase inhibitors to prevent bacterial contamination in lysates used for in vitro production of polypeptides. The compositions include contamination-free cell lysates for in vitro protein synthesis reactions.

专利号:US-7632944-B2
优先权日:2007-01-24
标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
发明人：HARMS ARTHUR E
权利人:BAUSCH & LOMB
摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.