- Preparation method of quinolone carboxylic acid derivative or phthalazinone carboxylic acid derivative
-
The invention belongs to the field of pharmaceutical chemicals, relates to a preparation method of a quinolone carboxylic acid derivative or a phthalazinone carboxylic acid derivative, and particularly relates to a preparation method of a 7-substituted-3-quinolone carboxylic acid derivative or a 7-substituted-1,5-phthalazinone carboxylic acid derivative. The preparation method comprises the following steps: (1) in an organic solvent, carrying out coupling reaction on a boron chelate II and organic amine III in the presence of an organosilicon compound to obtain a compound IV; and (2) mixing the compound IV with hydrochloric acid, and then filtering and separating the precipitated compound I. Compared with conventional methods, the preparation method provided by the invention has the advantages that the conditions are milder, the hydrolysis of the substrate quinoline carboxylic acid boric acid ester can be reduced, and meanwhile, the influence of a byproduct HF on the product purity is avoided. The method is high in yield and high in purity; compared with the traditional alkali, the organic silicon is more suitable for industrial preparation of the 7-substituted-3-quinolone carboxylic acid derivative or the 7-substituted-1,5-phthalazinone carboxylic acid derivative.
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- Preparation method of moxifloxacin hydrochloride (by machine translation)
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The reaction: the reaction, is added into the reaction kettle, to heat, and then the,dihydro - 8 8-oxo- 3 3-dihydro-8-methoxy - 4 4-dioxanone introduced into the reaction kettle, is added to the reaction still 1 - for heating and reacting the, by the reaction; first and then, refluxing under, heating. 1st. The method comprises, condensation reaction; adding a protecting gas, to a reaction kettle.] and reacting, to obtain moxifloxacin hydrochloride; second by heating and reacting with a heating reaction of, by a heating reaction of a heating reaction unit of a reaction scheme of, second in a reaction still further, heating a reaction, solution in, a reaction still further to react with a, reaction gas, second and refluxing, the reaction. (S,S) - 2,8 - The method comprises the following steps of heating and separating [4.3 .0] out of a reaction; and refluxing the reaction gas . The reaction mixture; is introduced, into the reaction kettle. (by machine translation)
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Paragraph 0048-0055; 0066-0080
(2020/05/01)
-
- Synthetic method of moxifloxacin hydrochloride
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The invention discloses a synthetic method of moxifloxacin hydrochloride. The synthetic method comprises the following steps: under the protection of argon, taking gatifloxacin carboxylate and (S,S)-2,8-diazabicyclo[4.3.0]nonane as raw materials; taking an organic alkali or an inorganic alkali as an acid-binding agent and a Lewis acid as a catalyst; reacting in a certain solvent at a proper temperature; concentrating, processing by alkali liquor, separating out moxifloxacin monomers at an isoelectric point, reacting moxifloxacin monomers with an acid to form salt, concentrating to obtain a moxifloxacin hydrochloride crude product, re-crystallizing, filtering, washing and drying to obtain a refined moxifloxacin hydrochloride finished product. The preparation method is mild in reaction conditions, simple to operate, less in pollution, and high in yield and industrial production can be realized easily.
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Paragraph 0037-0057
(2020/07/13)
-
- Preparation method of moxifloxacin hydrochloride
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The invention discloses a preparation method of moxifloxacin hydrochloride, and the preparation method comprises the following steps: (1) preparing 1-cyclopropyl-6,7-difluoro-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid-O3,O4-boron diacetate, and (2) carrying out a reaction on the 1-cyclopropyl-6,7-difluoro-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid-O3,O4-boron diacetate; (2)adding the 1-cyclopropyl-6,7-difluoro-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid-O3,O4-boron diacetate and (S,S)-2,8-diazabicyclo[4.3.0]nonane in a solvent in the presence of an acid-binding agent to obtain a borane condensate, removing the solvent, dissolving the borane condensate in water, and adding hydrochloric acid to form salt and crystallize to obtain moxifloxacin hydrochloride. According to the preparation method, the borane condensate is dissolved in water, and hydrochloric acid is added for salifying and crystallizing, so that genotoxic impurities such as chloromethaneand chloroethane are not generated, and an impurity C is not generated; therefore, moxifloxacin hydrochloride prepared by means of the preparation method is high in purity and low in risk.
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Paragraph 0027; 0031-0035; 0040-0041
(2020/06/20)
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- Preparation method of moxifloxacin hydrochloride (by machine translation)
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The invention relates to a preparation method of moxifloxacin hydrochloride. , 1 - Cyclopropyl -7 - (S, S-2, diazabicyclo [4.3.0] nonane -8 - yl) -6 - fluoro -8 - methoxy -4 - oxo -1, 4 - dihydro -3 - quinoline carboxylic acid hydrochloride is prepared. The condensation reaction solvent acetonitrile is recovered after a certain technical means is recovered to form a condensation product borane chelating moxifloxacin, and the condensation reaction solvent acetonitrile can be reused for the condensation reaction step after the condensation reaction solvent acetonitrile is recovered by a certain technical means. The condensate is hydrolyzed with sodium hydroxide solution in acetone, and then pH is adjusted to acid by hydrochloric acid to form a moxifloxacin hydrochloride crude product, and the crude product is refined after refining in a mixture of ethanol and water to obtain refined moxifloxacin hydrochloride. To the method, the condensation reaction temperature is reduced, the product purity is improved, the emission of three wastes is reduced, the production cost is reduced, and the method is suitable for industrial production. (by machine translation)
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Paragraph 0032; 0035; 0038; 0041; 0044; 0047; 0048; 0051
(2020/12/14)
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- Preparation method of moxifloxacin hydrochloride and intermediate of moxifloxacin hydrochloride
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The invention provides a preparation method of moxifloxacin hydrochloride and an intermediate of moxifloxacin hydrochloride, and belongs to the technical field of heterocyclic compound. The preparation method comprises following steps: gatifloxacin intermediate, (S, S)-2, 8-diazabicyclo[4, 3, 0]nonane, a reaction solvent, an organic base, and a Lewis acid are mixed, are reacted fully at a preset temperature, and are subjected to cooling filtering, an obtained filtrate is heated, L-(+)-tartaric acid is added, thermal insulation crystallization is carried out, cooling is carried out, centrifugation filtration, washing, and drying are carried out so as to obtain moxifloxacin ethyl ester tartrate; moxifloxacin ethyl ester tartrate is added into a hydrogen chloride containing solution, heatingis carried out, thermal insulation full reaction is carried out, crystallization is carried out, after cooling, centrifugation filtration, beating, and baking are carried out so as to obtain finishedproducts. According to the preparation method, one-pot reaction is realized, the selectivity and conversion rate are higher than those of disclosed methods, energy is saved, post-treatment is convenient, the preparation method is suitable for industrialized production, and HPLC>99.9%.
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Paragraph 0050-0055
(2019/09/14)
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- Preparation process of moxifloxacin
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The invention relates to the technical field of pharmaceutical engineering, specifically to a preparation process of moxifloxacin. The preparation process comprises the following steps: carrying out ahydrolysis reaction on a moxifloxacin chelate which is chelated with borate so as to form a crude moxifloxacin product containing boric acid; subjecting polyol and the crude moxifloxacin product containing boric acid to a chelation reaction; and then adding a poor solvent for crystallization. The preparation process of the invention can effectively remove elemental boron in the crude moxifloxacinproduct, and the yield and the purity of prepared moxifloxacin are excellent.
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Paragraph 0083-0121
(2019/12/25)
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- Preparation method of moxifloxacin hydrochloride
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The invention discloses a preparation method of moxifloxacin hydrochloride. The method comprises the following steps: performing condensation by using 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-ethylquinolinecarboxylate as a central ring, and (S,S)-2,8-diazabicyclo[4,3,0]nonane as a side chain, after alkali hydrolysis is completed, adding a part of 6N hydrochloric acid, performing primary crystallization, adding the remaining 6N hydrochloric acid, performing secondary crystallization, and performing recrystallization on the crystallized product obtain by the secondary crystallization once by using ethanol to obtain the moxifloxacin hydrochloride with a high content and excellent quality. When the method provided by the invention is adopted to prepare the moxifloxacin hydrochloride, product loss caused by repeated crystallization is reduced, labor intensity is reduced, energy consumption is reduced, product stability is improved, product quality is greatly improved, and themethod is suitable for industrialized large-scale production; and the prepared moxifloxacin hydrochloride contains 99.6%-102.0% of C21H25ClFN3O4 calculated by an anhydrate, and has a low total impurity content.
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Paragraph 0018-0028; 0031-0041; 0044-0054
(2019/08/30)
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- Preparation method of moxifloxacin hydrochloride and intermediate thereof
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The invention discloses a preparation method of moxifloxacin hydrochloride and an intermediate thereof. The preparation method of the intermediate III of the moxifloxacin hydrochloride includes the following steps: making an intermediate II of the moxifloxacin hydrochloride and (S,S)-2,8-diazabicyclo[4,3,0]nonane have condensation reaction in an organic solvent in the presence of alkali to obtainthe intermediate III of the moxifloxacin hydrochloride. The preparation method is simple and safe in operation, does not require special equipment and avoids use of highly toxic materials and mild inreaction conditions. The obtained the moxifloxacin hydrochloride I has high purity and low production cost, and is suitable for industrial production. (img file='DDA0001750656940000011.TIF' wi='700' he='192'/).
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Paragraph 0090-0093
(2019/01/16)
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- Preparation method for moxifloxacin hydrochloride
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The invention relates to a preparation method for moxifloxacin hydrochloride. The preparation method comprises the following steps: step 1, preparing an intermediate Im-1; step 2, preparing a crude product Im-2; step 3, preparing a moxifloxacin split crude product Im-3; and step 4, preparing a moxifloxacin finished product, wherein preparation for the moxifloxacin finished product comprises the following steps: (1) adding Im-3, octane and propylene glycol into a reaction kettle, heating until reflowing; (2) adding activated carbon, and reflowing and stirring; (3) filtering while hot, separating out solid and stirring for 2hour at the room temperature, cooling to 0-5 DEG C, stirring for 1-2 hours, and separating out crystals; and (4) cooling to 0-5 DEG C for water-leaching after filtering,and performing vacuum drying for 8-12 hours at a temperature being 50-55 DEG C, thereby obtaining a moxifloxacin hydrochloride competitive product.
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Paragraph 0075; 0083; 0084; 0085; 0086; 0087; 0088; 0089
(2018/07/30)
-
- Moxifloxacin hydrochloride new preparation method
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The invention provides a method for preparing a moxifloxacin intermediate and moxifloxacin hydrochloride, which comprises the following steps: carrying out condensation reaction on main ring chelate disclosed as Formula (I) and (S,S)-2,8-diazabicyclo-[4.3.0]nonane in the presence of an acid acceptor in a solvent, acidifying for salification, crystallizing, filtering, washing and drying to obtain the moxifloxacin hydrochloride. The method is characterized in that the solvent in the condensation reaction is alcohol. The condensation reaction is carried out in the alcohol solvent at the controlled temperature of 30-80 DEG C (preferably lower temperature), so the method has the advantage of mild reaction conditions, greatly reduces the generation of impurities, saves the energy; the alcohol solvent can be directly acidified after sufficient reaction, thereby saving the complex step of removing acetonitrile by evaporation and greatly simplifying the steps; and the method is suitable for industrial production.
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Paragraph 0063; 0064; 0069; 0071; 0073; 0075; 0077; 0079
(2018/05/24)
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- Method for preparing moxifloxacin hydrochloride
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The invention discloses a method for preparing moxifloxacin hydrochloride. The method includes the following steps: in the presence of shielding gas, adding CuCl2, glycol, iso-butylamine and 1-cyclopropyl-6, 7-difluoro-1, 4-dihydro-8-methoxyl-4-oxo-3-quinoline carboxylic ethyl ester into a reaction kettle containing methyl alcohol, performing contact reaction at the temperature of 45-55 DEG C for 3 hours, then heating up to the temperature of 65-80 DEG C, adding (S,S)-2, 8-diazabicyclo [4.3.0] nonane for continuous reaction for 4 hours, performing hot filtration to filter out insoluble matter, dropwise adding concentrated hydrochloric acid at room temperature, regulating the pH value to 2, stirring, cooling to minus 10-minus 5 DEG C prior to devitrification, and performing suction filtration, cold ethanol rinsing and vacuum drying to obtain the moxifloxacin hydrochloride. The method is particularly suitable for industrial scale production, simple in step and high in yield.
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Paragraph 0020; 0024; 0025; 0026
(2016/10/27)
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- A method for synthesizing moxifloxacin hydrochloride
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The invention discloses a novel synthesis method of moxifloxacin hydrochloride, belonging to the field of pharmaceutical chemistry. The synthesis method comprises the following steps: sequentially adding acetic anhydride and glacial acetic acid into a reaction kettle, adding anhydrous zinc chloride while stirring, dropwisely adding triethyl borate, stirring to react after finishing the dropwise addition, adding gatifloxacin intermediate, and carrying out after-treatment on the obtained solid to obtain a moxifloxacin hydrochloride intermediate; and in the presence of an organic solvent, reacting the moxifloxacin hydrochloride intermediate with (S,S)-2,8-diazabicyclo[4.3.0]nonane, dropwisely adding concentrated hydrochloric acid, reacting to obtain a moxifloxacin hydrochloride crude product, and recrystallizing with ethanol to obtain the high-purity moxifloxacin hydrochloride. The single impurity content of the moxifloxacin hydrochloride is lower than 0.05%, and the total impurity content is lower than 0.1%; and the method is simple to operate, has the advantages of mild conditions and high yield, and is suitable for industrial production.
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Paragraph 0028; 0029
(2017/02/24)
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- A hydrochloric acid moxifolxacin improved method for preparing
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The invention belongs to the medicine synthesis field, which concretely relates to a method for preparing moxifloxacin hydrochloride by one-pot method. The method comprises is characterized in that 1-cyclopropyl-6,7- difluoro-1,4-dihydro-8-methoxyl-4-oxo-3-quinoline carboxylic acid ethyl ester is taken as a raw material, then subjected to a chelating reaction by boron, is subjected to nucleophilic substitution reaction with (S,S)-2,8-diazabicyclo[4.3.0]nonane and an acidifying step to prepare moxifloxacin hydrochloride, and the reaction products can be directly used for reaction in next step without post-treatment or separation. The improvement of the invention has the advantages that the reaction steps can be simplified, the operation is simple and the yield is high, and is adapted to more suitable for industrial production.
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Paragraph 0038; 0039
(2017/01/23)
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- Method for preparing moxifloxacin hydrochloride
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The invention discloses a method for preparing moxifloxacin hydrochloride. The method comprises the following steps: in the existence of protective gas, enabling boric acid and propionic anhydride to have contact reaction for 1h at 95 to 105 DEG C, and cooling to 75 to 80 DEG C; adding a stable accelerant, adding 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxyl-4-oxo-3-quinolinecarboxylate, continuously stirring to react for 1.5h to 3h at 75 to 80 DEG C, monitoring and tracking until the reaction is completed, cooling to the room temperature, adding acetonitrile and organic amine, enabling the acetonitrile and organic amine to react with (S,S)-2,8-diazabicyclo[4.3.0] nonane for 1h to 2h at 65 to 75 DEG C, cooling to the room temperature, filtering insoluble articles, adding methanol, dropwise adding concentrated hydrochloric acid at the room temperature, adjusting the pH value to 1 to 3, stirring for 2h, then cooling to -10 to -5 DEG C, precipitating, suction filtering, washing by cold ethanol, and vacuum drying to obtain moxifloxacin hydrochloride, wherein the stable accelerator is selected from one or more of glycine, serine and threonine. The method is high in yield, high in product purity, simple and feasible in process and suitable for industrialized production.
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Paragraph 0036-0038
(2017/01/12)
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- A preparation suitable for industrial production with high optical purity hydrochloric acid method moxifolxacin
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The invention provides a high optical purity moxifloxacin hydrochloride production method suitable for industrialized production; moxifloxacin hydrochloride containing 0.2 ~ 5% of optical isomers is used as a raw material for preparation of moxifloxacin hydrochloride with the optical isomer content less than 0.01% (compound shown as formula I). The new high optical purity moxifloxacin hydrochloride production method avoids the resolution of a conventional chiral reagent, by use of own different basic strength, the high optical purity moxifloxacin hydrochloride can be obtained by the acid-base neutralization method, the high optical purity moxifloxacin hydrochloride product is low in production cost, high in yield, simple in process and suitable for industrialized production.
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Paragraph 0051; 0053
(2016/10/10)
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- Preparation method of moxifloxacin impurity G compound
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The invention provides a preparation method of a moxifloxacin impurity G compound, comprising using 1-cyclopropyl-6,7-difluoro-8-methoxy-1,4-dihydro-4-oxoquinolyl-3-carboxylic acid ethyl ester as a starting material to react with triacetoxyboron, then removing ethyl ester to generate moxifloxacin boron diacetate, reacting with (S,S)-2,8-diazabicyclo[4.3.0]nonane, then removing a protective base and salifying to generate moxifloxacin hydrochloride, oxidizing via an oxidizing agent, and then acquiring moxifloxacin impurity G in the presence of a dewatering agent. The preparation method is simple to perform, a prepared target product has high purity, and an obtained substance is useful for studying moxifloxacin hydrochloride related substances.
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- A hydrochloric acid moxifolxacin method for the synthesis of
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The invention provides a synthetic method of moxifloxacin hydrochloride. The synthetic method comprises the following steps: by taking a primary ring chelate as shown in a formula (I) and (S, S)-2,8-diazabicyclo[4.3.0] nonane as raw materials and taking triethylamine as an acid absorber, carrying out condensation reaction in acetonitrile sufficiently; and concentrating, treating, then dissolving, carrying out acidolysis and salifying, crystallizing, filtering, washing and drying to obtain the moxifloxacin hydrochloride, wherein a weight ratio of the primary ring chelate to acetonitrile to triethylamine to (S, S)-2,8-diazabicyclo[4.3.0] nonane is 1 to (2-10) to (0.08-0.96) to (0.30-0.59). The synthetic method is characterized in that a condensation reaction temperature is larger than and equal to 30 DEG C and lower than 70 DEG C. The synthetic method has the following technical effects that nucleophilic substitution reaction is carried out in acetonitrile at a temperature not lower than 30 DEG C but lower than 70 DEG C, the reaction conditions are gentle, the production of impurities is greatly reduced and the energy resources are saved. After acetonitrile is evaporated, the treatment method is simple and rapid, acidification is carried out in alcohol to obtain moxifloxacin hydrochloride, and thus, the synthetic method is suitable for industrial production.
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- Preparation method of moxifloxacin hydrochloride
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The invention discloses a preparation method of moxifloxacin hydrochloride. The method includes the following steps of making boric acid and acetic anhydride make contact and react for 1 h at a temperature of 85-105 DEG C in protection gas, lowering the temperature to 75-80 DEG C, adding a stable promoter and 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid ethyl ester, continuing to conduct stirring for the reaction for 1.5-3 h at a temperature of 75-80 DEG C, conducting monitoring and tracking till the reaction ends, cooling to the room temperature, adding acetonitrile and organic amine to make the mixture react with (S,S)-2,8-diazabicyclo[4.3.0]nonane for 1-2 h at a temperature of 60-70 DEG C, cooling to the room temperature, adding methyl alcohol, dropwise adding concentrated hydrochloric acid at a temperature of 5-10 DEG C, adjusting the pH value to 1-3, conducting stirring for 2 h, cooling to a temperature of -10 DEG C to -5 DEG C, conducting crystallization and suction filtration, conducting washing through cold ethyl alcohol, conducting decompression drying, and obtaining moxifloxacin hydrochloride. The stable promoter is selected from one or more of glycine, serine and threonine. The method is high in yield, simple in operation and aftertreatment and suitable for industrial production.
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Paragraph 0025; 0033; 0034; 0035
(2016/11/28)
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- A high-purity hydrochloric acid moxifolxacin method for the synthesis of (by machine translation)
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The present invention provides a high-purity hydrochloric acid method for synthesizing moxifolxacin, comprising the following steps: the benzol the 1-cyclopropyl -6,7-difluoro-8-methoxy -1,4-dihydro-4-oxo-quinolyl-3-carboxylic acid ethyl ester carbonyl of protection, then the (S, S) - 2,8-diazabicyclo [4.3.0] nonane after to conduct the condensation reaction, to adopt the hydrochloric acid is deprotected, star thick mozambican Xisha hydrochloric acid obtained; the resulting star thick mozambican Xisha of the hydrochloric acid aqueous solution of alkali is dissolved, then extracting with an organic solvent, removal of the organic phase, the aqueous phase by adding hydrochloric acid to adjust pH in value to acidity, then crystallization, filtering to obtain the filter cake, then the aqueous organic solvent to the obtained filter cake of performing recrystallization, final filtering, drying to obtain high-purity hydrochloric acid Moxifloxacin. The method of the invention high purity of the prepared product, high yield, good reproducibility, has extremely strong the feasibility of industrial operation. (by machine translation)
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Paragraph 0037
(2017/04/03)
-
- 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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- AN IMPROVED PROCESS FOR THE PREPARATION OF MOXIFLOXACIN HYDROCHLORIDE
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The present invention relates to an improved and industriously advantageous process by means of providing coupling/condensing of wet mass of (l-cyclopropyl-6,7-difluoro-8- methoxy-4-oxo- 1,4~dihydro-3-qumoline carboxylic acid-O3, O4)bis(acyloxy-0)borate with (S,S)-2,8-diazabicyclo[4.3.0]nonane to give l-cyclopropyl-7-[S,S]-2,8-diazabicyclo- [43.0]non-8-yl)-6-fluoro-l,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride (Moxifloxacin hydrochloride) of Formula-I with high purity.
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Page/Page column 12-19
(2014/06/24)
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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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- 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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- PROCESS FOR PREPARING MOXIFLOXACIN AND SALTS THEREOF
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The present invention relates to a process for the synthesis of Moxifloxacin of Formula (I) and salts thereof by means of a process providing the coupling reaction of 1-cyclopropril-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinic acid or ester thereof with (4aS, 7aS)-octahydro-1H-pyrrole[3,4-b]pyridine using a magnesium salt.
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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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- NOVEL POLYMORPH OF MOXIFLOXACIN HYDROCHLORIDE
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The present invention relates to novel polymorph of moxifloxacin hydrochloride, processes for its preparation and to pharmaceutical compositions containing it. Thus, for example moxifloxacin hydrochloride is suspended in methanol and water and the pH is adjusted to 1.0 - 2.0 with concentrated hydrochloric acid at 25 °C and the separated solid is collected and dried to obtain moxifloxacin hydrochloride monohydrate polymorph IV.
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Page/Page column 5; 6
(2010/06/11)
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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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- 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 13-14
(2008/12/05)
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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 24
(2008/12/05)
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- CRYSTALLINE FORM OF MOXIFLOXACIN HYDROCHLORIDE
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The present invention refers to a new stable crystalline form of moxifloxacin hydrochloride, to a process of its preparation and to its use in the preparation of pharmaceutical compositions. It is provided a process comprising to dissolve crude moxifloxacin hydrochloride in a mixture of methanol/water by heating at the reflux temperature; to add acetone and to heat the dissolution at a temperature comprised between 40 and 45°C; to cool until a temperature comprised between 15 and 25°C; to separate the crystals formed by filtration; to wash and dry the obtained product until a constant weight is obtained.
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Page/Page column 8
(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 15
(2010/11/25)
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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 6
(2008/06/13)
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- NEW CRYSTALLINE FORM OF MOXIFLOXACIN HYDROCHLORIDE AND PROCESS FOR ITS PREPARATION
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The present invention relates to a new crystalline form of 1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methoxy-7-[(4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid hydrochloride of the Formula I with a moisture content below 2 % w/w (Form A). The present invention also relates to a process of preparing the new crystalline form.
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Page/Page column 14-15
(2008/06/13)
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