195532-12-8Relevant articles and documents
Synthesis method of pradofloxacin
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Paragraph 0055; 0056; 0059-0064, (2018/05/16)
The invention relates to a synthesis method of pradofloxacin. According to the method, a cheap and easy-to-obtain compound is taken as a raw material and subjected to chlorination, acylation, nucleophilic substitution, cyclization, hydrolysis and alkylation reactions, and the target product, namely, pradofloxacin, is obtained. The nucleophilic substitution target product beta-substituted amino-alpha-substituted benzoyl acrylate compound has good quality and has the purity of 98% or above and the yield of 80%-90%, and the yield is increased by 10% or above as compared with that in the prior art; the provided ester hydrolysis method and product quality are good, and the reaction yield reaches 93%-98%; organic base is used for replacing conventional inorganic base to serve as a cyclization reaction catalyst, the operation is simple, no pollution is caused, and the cost is substantially reduced; halogenated hydrocarbon is taken as an alkylation solvent, the reaction temperature is the roomtemperature, the reaction is mild and easy to operate, fewer impurities are produced in the alkylation reaction at the temperature of 20-40 DEG C as compared with those produced in the alkylation reaction at the high temperature in the prior art, the yield is high, halogenated hydrocarbon solvents are easy to recycle and reuse, pollution is greatly reduced, and the synthesis method is environmentally friendly.
PROCESS FOR PREPARING PRADOFLOXACIN
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Page/Page column 2, (2009/12/28)
The invention relates to an improved process for preparing pradofloxacin, in which the substituent in the 7 position is introduced by nucleophilic substitution in an N-methylpyrrolidone-ethanol solvent mixture.
Crystal modification B of 8-cyano-1-cyclopropyl-7-(1S,6S-2, 8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
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Page column 4, (2008/06/13)
The present invention relates to a defined crystal modification of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I), to processes for its preparation and to its use in pharmaceutical preparations. The crystal modification can be distinguished from other crystal modifications of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I) by its characteristic X-ray powder diffractogram and its differential thermodiagram (see description).
Crystal modification C of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo-[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihyro-4-oxo-3-quinoline carboxylic
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Page/Page column 3, (2008/06/13)
The present invention relates to a defined crystal modification of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (1), to processes for its preparation and to its use in pharmaceutical preparations. The crystal modification can be distinguished from other crystal modifications of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (1) by its characteristic X-ray powder diffractogram and its differential thermodiagram (see description).
Optionally substituted 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids and their derivatives
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, (2008/06/13)
Intermediates useful in the preparation of 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl-6-fluorol,4-dihydro-4-oxo-3-quinolinecarboxylic acids of the following structures are claimed.