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Method for preparing and purifying laevogyrate gatifloxacin

A technology of gatifloxacin and purification method, which is applied in the field of preparation and purification of levogatifloxacin, can solve the problems of low yield and the like, and achieve the effects of high yield, good product quality and easy operation.

Inactive Publication Date: 2005-08-31
NANJING SANHOME PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But the productive rate of this preparation method only has 40%, productive rate is lower

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] In a 250ml reaction flask, add 0.4g of anhydrous zinc chloride and 100ml (0.927mol) of acetic anhydride, heat to 80°C, then add 16.2g (0.245mol) of boric acid in batches, and control the temperature at 80-110°C. , stirred at 110° C. for 1 hour, then cooled to 80° C., added 60 g (0.185 mol) of quinolinecarboxylic acid cyclic ester and reacted at 80° C. for 2 hours. Reaction finishes, after decompression evaporates part acetic anhydride, add 350ml water while hot and fully stir, have solid to separate out, suction filtration, solid is washed to neutrality with a large amount of water, dry to obtain chelate weight 62g, yield 78.9%, appearance is Light orange-yellow powder. Mp: 114-117°C. In a 250ml reaction flask, add chelate 55g (0.13mol), acetonitrile 180ml, S-(+)-N-methylpiperazine 22g (0.216mol) and triethylamine 56ml, heat to 60°C for 3 hours, Recover the solvent by distillation under reduced pressure (the liquid temperature does not exceed 60°C), dilute the residua...

Embodiment 2

[0017] In a 250ml reaction flask, add 0.4g of anhydrous zinc chloride and 100ml (0.927mol) of acetic anhydride, heat to 80°C, then add 16.2g (0.245mol) of boric acid in batches, and control the temperature at 80-110°C. , stirred at 110° C. for 1 hour, then cooled to 80° C., added 60 g (0.185 mol) of quinolinecarboxylic acid cyclic ester and reacted at 80° C. for 2 hours. Reaction finishes, after decompression evaporates part acetic anhydride, add 350ml water while hot and fully stir, have solid to separate out, suction filtration, solid is washed to neutrality with a large amount of water, dry to obtain chelate weight 62g, yield 78.9%, appearance is Light orange-yellow powder. Mp: 114-117°C. In a 250ml reaction flask, add 55g (0.13mol) of chelate compound, 180ml of tetrahydrofuran, 22g (0.216mol) of S-(+)-N-methylpiperazine and 56ml of DMF, heat to 60°C for 4 hours, and distill under reduced pressure Recover the solvent (the liquid temperature does not exceed 60°C), dilute t...

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Abstract

A process for preparing and purifying levogatixacin includes such steps as reaction between cycloester quinolinecarboxylate and boric acid to generate a chelate, reacting on S-(+)-N-methylpiperazine in polar solvent, hydrolyzing and regulating pH value.

Description

technical field [0001] The present invention relates to levo-gatifloxacin, namely S-(-)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazine )-4-oxo-3-quinolinecarboxylic acid preparation and purification method. Background technique [0002] Levo-gatifloxacin, namely S-(-)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazine)- 4-oxo-3-quinoline carboxylic acid is a levorotatory form of gatifloxacin antibacterial agent, which has the characteristics of high spectral efficiency and low phototoxicity. There is not much difference between gatifloxacin optical enantiomers in terms of antibacterial activity and clinical efficacy (see Japanese Journal of Chemotherapy; 27-30, Volume 47, 1999; 112-123, Volume 47, 1999; and 124-130, Volume 47, 1999). Levo-gatifloxacin is significantly lower than dex-gatifloxacin in prolonging the APD effect, that is, reducing cardiotoxicity, and is more suitable for use as a drug. Its preparation method has been ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04
Inventor 张仓张文萍
Owner NANJING SANHOME PHARMACEUTICAL CO LTD
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