CAS: 101363-10-4; Rufloxacin

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CAS号101337-89-7 rufloxacin-1-oxide | CAS号367-21-5 3-氯-4-氟苯胺 | CAS号109-01-3 N-甲基哌嗪 | CAS号101337-95-5 8-chloro-7-fluo... | CAS号101337-87-5 N-Desmethylrufl...

📜Ethyl 10-Chloro-9-Fluoro-7-Oxo-2,3-Dihydro-7H-Pyrido<1,2,3-De><1,4>Benzothiazine-6-Carboxylate置于lead(Iv) Acetate,Sodium Hydroxide,Potassium Bromide,三氯化磷体系中,用 水,溶剂黄146,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 5.75H,反应生成如氟沙星
参考文献:喹诺酮羧酸.2.7-氧代-2,3-二氢-7H-吡啶并[1,2,3-De] [1,4]苯并噻嗪-6-羧酸的合成及抗菌性能评价.
标题:喹诺酮羧酸.2.7-氧代-2,3-二氢-7H-吡啶并[1,2,3-De] [1,4]苯并噻嗪-6-羧酸的合成及抗菌性能评价.
摘要:合成了一系列的吡啶并苯并噻嗪酸衍生物,并对其体外抗菌活性进行了评估.1,4-苯并噻嗪中间体是通过gould-Jacobs喹啉合成而生成吡啶基苯并噻嗪酸的,其制备方法是将取代的2-氨基苯并噻唑进行水解碱性裂解,然后用1-溴-2-氯乙烷或一氯乙酸进行连续环缩合反应,然后通过lialh4.吡啶并苯并噻嗪酸10C,30和31对革兰氏阳性和革兰氏阴性病原体显示出强大的抗菌活性.讨论了构效关系.化合物9-氟-10-(4-甲基-1-哌嗪基)-7-氧代-2,3-二氢-7H-吡啶基[1,2,3-De] [1,4]苯并噻嗪-6-羧酸已发现酸(31)(mf-934)具有抗菌活性,
Doi:10.1021/jm00386A005

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-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:US-8227597-B2
优先权日:2006-10-06
标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
发明人：HARMS ARTHUR E
权利人:HARMS ARTHUR E; 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:US-2009054643-A1
优先权日:2007-05-24
标 题:Novel method of synthesis of fluoroquinolones

专利号:US-8252783-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; ARUL RAMAKRISHNAN; SONI ANIL K
权利人:HARMS ARTHUR E; ARUL RAMAKRISHNAN; SONI ANIL K; BAUSCH & LOMB
摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, Ib, 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.