CAS: 112811-72-0; 1-Cyclopropyl-6,7-Difluoro-8-Methoxy-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

上下游产品

ethyl 8-methoxy-1-cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate 1-cyclopropyl-6,7-difluoro-8-hydroxy-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid dimethyl sulfate 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid methyl ester gatifloxacin 7-[3-(S)-amino-4-(S)-fluoromethyl-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxoquinoline-3-carboxylic acid 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-7-(3-methylaminopiperidin-1-yl)-3-quinolinecarboxylic acid 1-cyclopropyl-6-fluoro-8-methoxy-7-(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl-1,4-dihydro-4-oxo-3-quinoline carboxylic acid

专利信息

专利号:US-8680276-B2
优先权日:2009-03-06
标题 :Synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine
发明人：MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO
权利人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO
摘要:The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.

专利号:US-6017911-A
优先权日:1996-02-27
标 题 :Pyridonecarboxylic acid derivatives and intermediates for the synthesis thereof
发明人：HORIUCHI NOBUHIKO; YONEZAWA TAKENORI; CHIBA KATSUMI; YOSHIDA HIROAKI
权利人:DAINIPPON PHARMACEUTICAL CO
摘要:This invention relates to pyridonecarboxylic acid derivatives of the following general formula, esters thereof and salts thereof, as well as pharmaceutical preparations containing them. ##STR1## wherein: R is cycloalkyl which may be substituted by halogen, or the like; n X is hydrogen, lower alkyl, amino or the like; n Y is hydrogen or halogen; n A is nitrogen or a group of the formula C--Z in which Z is lower alkoxy that may be substituted by halogen, or the like; n R 1 and R 2 may be the same or different and are each hydrogen or the like; n R 3 is hydrogen or lower alkyl; n R 4 , R 5 , R 6 , R 7 , R 8 and R 9 may be the same or different and are each hydrogen, halogen or lower alkyl; n m is 0 or 1; and n n and p may be the same or different and are each 0 or 1. n This invention also relates to bicyclic amine compounds useful as direct intermediates for the synthesis of the above-described pyridonecarboxylic acid derivatives.

专利号:WO-2006004561-A1
优先权日:2004-06-30
标 题:Process for the preparation of gatifloxacin and regeneration of degradation products
发明人：RUZIC MILOS; RELIC MILENKA; TOMSIC ZDENKA; MIRTEK MIRJANA
权利人:KRKA TOVARNA ZDRAVIL D D NOVO; RUZIC MILOS; RELIC MILENKA; TOMSIC ZDENKA; MIRTEK MIRJANA
摘要:The subject of the present invention are an improved synthesis process comprising a process for regeneration of a side product of gatifloxacin and an analysis method for process control in the synthesis of gatifloxacin (Formula I).

专利号:US-8198451-B2
优先权日:2006-11-13
标题 :Process for the synthesis of moxifloxacin hydrochloride
发明人：RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; PATHI SRINIVAS LAXMINARAYAN; PUPPALA RAVIKUMAR; GANGRADE MANISH; KANATHALA SHASHIREKHA
权利人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; PATHI SRINIVAS LAXMINARAYAN; PUPPALA RAVIKUMAR; GANGRADE MANISH; KANATHALA SHASHIREKHA; CIPLA LTD
摘要:A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph. In addition, new intermediates in the formation of moxifloxacin hydrochloride are described, having formulas (1) and (II):

专利号:WO-2012131629-A1
优先权日:2011-03-31
标题 :A process for preparation of intermediate of moxifloxacin
发明人：WANKHEDE KARUNA; JAGTAP ASHUTOSH; ROY MITA; HARIHARAN SIVARAMAKRISHNAN; KUMBHAR AJAY
权利人:PIRAMAL HEALTHCARE LTD; WANKHEDE KARUNA; JAGTAP ASHUTOSH; ROY MITA; HARIHARAN SIVARAMAKRISHNAN; KUMBHAR AJAY
摘要:The present invention provides a process for the preparation of racemic or chiral octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine of formula I, a key intermediate in the synthesis of moxifloxacin or its pharmaceutically acceptable salts. The process comprises reaction of racemic or chiral tetrahydro-6-(phenylmethyl)-1H- pyrrolo[3,4-b]pyridine-5,7(6H)-dione of formula II with a reducing agent, which is a mixture of two agents, that is mixture of dimethyl sulphate and sodium borohydride or aluminum chloride and sodium borohydride used in a molar ratio ranging from 1:1 to 1: 4, in the presence of a polar solvent at a temperature ranging from 15°C to 45°C 10 to obtain racemic or chiral octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine of formula I having purity ≥ 96%.

专利号:US-2008188658-A1
优先权日:2002-08-14
标题 :Novel synthesis of gatifloxacin