- A method for preparing [...] chelate compound
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The invention discloses a method for directly preparing a nemonoxacin chelate from nemonoxacin cyclization ester. According to the existing method, a reaction step is longer, and an amount of aftertreatment processes is larger, thus obviously prolonging the whole time of preparing nemonoxacin; and in addition, industrial production and environmental protection are not facilitated. The method comprises the following steps of: based on carboxylic acid anhydride or a mixed solvent of the carboxylic acid anhydride and carboxylic acid as a reaction solvent, adding boric acid or boric anhydride to carry out reaction; and adding the nemonoxacin cyclization ester into an obtained reaction solution to carry out chelation reaction, thus obtaining the nemonoxacin chelate. According to the preparation method, only one chelation reaction step exists, and a hydrolysis reaction process and complex aftertreatment operations thereof such as filtering and drying are saved, thus greatly shortening the whole time of preparing the nemonoxacin, and facilitating industrial production; and meanwhile, by avoiding the using of reagents such as concentrated hydrochloric acid and ethanol, the preparation method is economic and environment-friendly.
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Paragraph 0026; 0028
(2017/04/03)
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- ANTIBIOTIC DRUG
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This invention relates to a malic acid salt of (3S, 5R)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid. Also disclosed is a method of treating bacterial infection by an effective amount of this salt.
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Page/Page column 9
(2010/04/03)
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- Malate salts, and polymorphs of (3S,5S)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid
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The present invention is directed to malate salts of (3S,5S)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, and its polymorphs. The present invention is also directed to pharmaceutical compositions comprising the described salts and polymorphs.
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Page/Page column 9
(2008/06/13)
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- Hydride reduction process for preparing quinolone intermediates
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Hydride process for making acyclic diol intermediates from cyclic intermediates, useful in antibacterial quinolone synthesis.
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Page/Page column 7
(2008/06/13)
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- Coupling process for preparing quinolone intermediates
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Process for making 7-cycloamino-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids. Borate ester compounds suitable for use in such process.
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Page/Page column 8
(2008/06/13)
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