- Preparation method of moxifloxacin
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The invention provides a preparation method of moxifloxacin, which comprises the following steps: taking 1-cyclopropyl-6, 7-difluoro-8-methoxy-4-oxo-1, 4-dihydro-3-quinolinecarboxylic acid and (S, S)-2, 8-diazabicyclo[4.3. 0] nonane as raw materials, in an organic solvent, in the presence of an acid-binding agent, and carrying out condensation reaction by taking the tri-coordinated boride cation-chloroaluminate ionic liquid as a catalyst to prepare moxifloxacin. The structural formula of the tri-coordinated boride cation-chloroaluminate ionic liquid is BX2L, X is a halogen atom, and L is selected from 4-picoline (4-pic), imidazole (mim) and dimethylacetamide (DMA) ligands. The preparation method of moxifloxacin has the advantages of simple reaction steps, high yield, high product purity, mild conditions and easiness in industrial production.
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Paragraph 0039-0042
(2021/05/08)
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- Fluorescence quenching study of moxifloxacin interaction with calf thymus DNA
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Moxi oxacin (MOX) is a fourth-generation synthetic uoroquinolone antibacterial agent with many important therapeutic properties. Fluorescence quenching was used to study the interaction of MOX with calf thymus DNA (ct- DNA) in aqueous solution. The intercalative binding mode and a static quenching mechanism were conflrmed by the Stern-Volmer quenching rate constant (Kq) of 3.48 × 1011 M-1 s-1 at 298 K. The thermodynamic parameters (δH = -118.4 KJ mol-1 and δS = -299.4 J mol-1 K-1) were calculated at different temperatures, and they indicate that the main forces between MOX and ct-DNA are hydrogen bonding and Van der Waals force. We proved at the same time the presence of one single binding site on ct-DNA, and the binding constant is 1.28 × 105 M-1 at physiological pH. The results may provide a basis for further studies and clinical application of antibiotics drugs. Tubitak.
- Lv, Yun-Kai,Li, Pan,Jiao, Miao-Lun,Liu, Bao-Sheng,Yang, Chao
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p. 202 - 209
(2014/04/03)
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- IR, FT-ICR-MS studies on (1′S, 6′S)-1-cyclopropyl-7-(2,8- diazabicyclo[4.3.0] non-8-yl)-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3- carboxylic acid hydrochloride salt
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The infrared spectra of (1′S, 6′S)-1-cyclopropyl-7-(2,8- diazabicyclo[4.3.0] non-8-yl)-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3- carboxylic acid hydrochloride salt (CLF-HCl) were studied and compared with free base. Their fragmentation pathways were investigated using tandem mass spectrometric (MS/MS) techniques on Fourier-transform ion cyclotron resonance spectrum, and many characteristic fragment ions were found.
- Lin, Zhiwei
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p. 254 - 258
(2013/12/04)
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- Process for the preparation of moxifloxacin hydrochloride and intermediates thereof
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The present invention refers to a process for the preparation of Moxifloxacin hydrochloride through the synthesis of Moxifloxacin salts with sulfonic acids.
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Paragraph 0059; 0060
(2013/03/26)
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- MOXIFLOXACIN HYDROCHLORIDE COMPOUNDS AND INTERMEDIATES AND METHODS FOR MAKING SAME
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Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.
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Paragraph 0080; 0081
(2013/03/26)
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- Process for the Synthesis of Moxifloxacin Hydrochloride
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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):
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Page/Page column 5
(2010/06/22)
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- IMPROVED PROCESS FOR THE PREPARATION OF (S.S)-2.8-DIAZABICYCLO[4.3.0]NONANE
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The present invention is directed to an improved industrially viable, cost effective process for manufacturing (S,S)-2,8-Diazabicyclo[4.3.0]nonane in a substantially pure form and consequent conversion to Moxifloxacin hydrochloride monohydrate.
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Page/Page column 11
(2009/11/29)
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- CRYSTALLINE FORM OF MOXIFLOXACIN BASE
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The present invention relates to a crystalline form of moxifloxacin base, to a process for its preparation, to pharmaceutical compositions containing it, and to its use as an antibacterial agent.
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Page/Page column 9
(2008/12/08)
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- NOVEL PROCESS FOR THE PREPARATION OF MOXIFLOXACIN HYDROCHLORIDE AND A NOVEL POLYMORPH OF MOXIFLOXACIN
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The present invention relates to a novel process for the preparation of moxifloxacin hydrochloride compound of formula-1 through novel quinoline carboxamide intermediate compounds of general formula-2. The present invention provides the process for the preparation of novel quinoline carboxamide intermediate compounds of general formula-2. The present invention also relates to a novel process for the preparation of anhydrous form of moxifloxacin hydrochloride and a novel crystalline form of moxifloxacin.
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Page/Page column 22; 23-24
(2008/12/05)
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- PROCESS FOR THE SYNTHESIS OF MOXIFLOXACIN HYDROCHLORIDE
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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):
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Page/Page column 14-15
(2008/12/05)
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- Process for the preparation of moxifloxacin hydrochloride
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The present invention relates to a process for the preparation of Moxifloxacin hydrochloride monohydrate, of the formula
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Page/Page column 10
(2008/12/09)
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- Method for preparing moxifloxacin and moxifloxacin hydrochloride
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The present invention relates to a "one pot" method for preparing moxifloxacin and its chlorhydrate salt, without need to isolate the intermediate compounds. The new method allows the end product moxifloxacin to be obtained on a large scale with a good yield and in pure form by using a "one pot" method in which a smaller amount of bicyclic amine is used, this being an expensive reagent. Moreover, this method avoids and reduces the times and costs resulting from isolation of the intermediates, and substantially avoids obtaining the impurity produced by demethylation in 8-position of the ring.
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Page/Page column 5; 5-6; 6
(2008/06/13)
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- NOVEL CRYSTALLINE FORMS OF MOXIFLOXACIN HYDROCHLORIDE AND PROCESS FOR PREPARATION THEREOF
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Novel crystalline forms of moxifloxacin hydrochloride and process for preparation thereof.
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Page/Page column 12; 14
(2010/11/25)
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- Quinolonecarboxylic acids
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The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are linked to a β-lactam antibiotic, to their salts, to processes for their preparation and to antibacterial agents containing these derivatives.
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