CAS: 127045-41-4; Pazufloxacin

上下游产品

benzoxazine-6-carboxylic acid10-(1-benzyloxycarbonylamin°Cyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido1,2,3-de1,4benzoxazine-6-carboxylic acid 2,3,4,5-tetrafluorobenzoic acid ethyl 2,3,4,5-tetrafluorobenzenecarboxylate ethyl 4-carboxymethyl-2,3,5-trifluorobenzoateethyl (S)-9-fluoro-3,7-dihydro-3-methyl-10-(1-amin°Cyclopropyl)-7-oxo-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylate

(S)-9-(1-Benzyloxycarbonylamino-Cyclopropyl)-8-Fluoro-3-Methyl-6-Oxo-2,3-Dihydro-6H-1-Oxa-3A-Aza-Phenalene-5-Carboxylic Acid置于palladium On Activated Charcoal 氢气体系中,用 溶剂黄146 用作溶剂,化学反应 2.0H,反应生成帕珠沙星
参考文献:Pyridonecarboxylic Acids As Antibacterial Agents. Ix. Synthesis And Structure-Activity Relationship Of 3-Substituted 10-(1-Aminocyclopropyl)-9-Fluoro-7-Oxo-2,3-Dihydro-7H-Pyrido(1,2,3-De)-1,4-Benzoxazine-6-Carboxylic Acids And Their 1-Thio And 1-Aza Analogues.
标题:Pyridonecarboxylic Acids As Antibacterial Agents. Ix. Synthesis And Structure-Activity Relationship Of 3-Substituted 10-(1-Aminocyclopropyl)-9-Fluoro-7-Oxo-2,3-Dihydro-7H-Pyrido(1,2,3-De)-1,4-Benzoxazine-6-Carboxylic Acids And Their 1-Thio And 1-Aza Analogues.
摘要:为了研究 3-烷基取代基对 10-(1-氨基环丙基)-9-氟-7-氧代-2,3-二氢-7H-吡啶并[1,2,3-De]-1,4-苯并恶嗪-6-羧酸及其 1-硫代和 1-氮杂变体的抗菌效力和体内疗效的影响,我们合成了图 1 所列的一系列标题化合物.化合物(S)-1 在体外对五种具有代表性的革兰氏阳性和革兰氏阴性菌具有最强的活性,并使用金黄色葡萄球菌和绿脓杆菌小鼠感染模型对其进行了体内试验.(S)-氧氟沙星的体内疗效极佳,优于氧氟沙星和环丙沙星,随后对其进行了惊厥诱导活性,哺乳动物细胞毒性和拓扑异构酶 Ii 抑制试验.生物学结果表明,与氧氟沙星和环丙沙星相比,(S)-1 具有抗菌和毒性优势.小鼠口服和静脉注射(S)-1化合物及其甲磺酸盐后,血清浓度较高.
Doi:10.1248/cpb.42.2569

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-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

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.

专利号:WO-2009094569-A2
优先权日:2008-01-25
标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates