Method for preparing ceftizoxime

A technology of ceftizoxime sodium and ceftizoxime acid, which is applied in the field of medicine, can solve the problems of harm to the human body and easy residual 2-mercaptobenzothiazole, and achieves the effect of reducing the generation of impurities and having high reactivity

Active Publication Date: 2012-12-05
SUZHOU ERYE PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, 2-mercaptobenzothiazole (accelerator M) is likely to remain in the product of this method, which is harmful to the human body

Method used

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  • Method for preparing ceftizoxime
  • Method for preparing ceftizoxime
  • Method for preparing ceftizoxime

Examples

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Embodiment Construction

[0021] Dissolve 2-(2-amino-4-thiazolyl)-2-methoxyiminoacetic acid (2.01g, 10mmol) in 20ml of ethanol, add DMAP (1.83g, 15mmol) and DCC (3g, 6.0mmol) at room temperature After stirring for half an hour, add N-hydroxysuccinimide (1.2g, 10mmol), stir at room temperature for half an hour, add saturated NH4Cl solution after stirring, extract with ethyl acetate, separate the ethyl acetate layer, and wash the organic phase with saturated salt Wash with water, dry over anhydrous sodium sulfate, evaporate the solvent, and elute with column chromatography (ethyl acetate / methanol=10:1) to obtain 2.8 g of active ester with a yield of 94%.

[0022] Dissolve the active ester (2.8g, 9.4mmol) in 20ml of dichloromethane, add 7-ANCA (1.9g, 9.4mmol) and 10ml of triethylamine and stir at room temperature for 8 hours, adjust the acidity with 1mol / l hydrochloric acid solution (PH=2.0), and react at -5°C for 2h. Extract with dichloromethane, decolorize with activated carbon, dry and concentrate to ...

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Abstract

The invention provides a method for preparing ceftizoxime. The method comprises the following steps of: (1) dissolving 2-(2-amino-4-thiazolyl)-2-methoxy-imine acetic acid in an organic solvent, and reacting with N-succinimide under the catalysis of dicyclohexyl carbodiimide / dimethylamino pyridine (DCC / DMAP) to obtain active ester; (2) dissolving the active ester in dichloromethane, and adding 7-amino-3-demethylation-3-cephalosporanic acid (7-ANCA) and alkali for reacting to obtain ceftizoxime acid; and (3) reacting the ceftizoxime acid with a salifying agent to obtain the ceftizoxime, wherein the salifying agent is sodium acetate, sodium ethoxide, sodium 2-ethylhexanoate, sodium isocaproate, sodium bicarbonate or sodium hydroxide.

Description

[0001] technical field [0002] The invention relates to a preparation method of ceftizoxime sodium, which belongs to the technical field of medicine. [0003] Background technique [0004] Ceftizoxime sodium was first developed by Japan Fujisawa Pharmaceutical Co., Ltd., and was first listed in Japan in 1982. Its English name is: Ceftizoxime, its molecular formula is: C13H13N5O5S2, and its chemical name is: (6r,7R)-7-[ (Z)-2-(2-Amino-4-thiazolyl)-2-methoxyiminoacetamido]-8-oxo-5-thia-1-aminobicyclo[4.2.0]octane -2-ene-2-carboxylic acid sodium salt, the structural formula is: [0005] [0006] Ceftizoxime sodium belongs to the third-generation cephalosporin, which has a broad-spectrum antibacterial effect and is effective against broad-spectrum β-lactamase (including penicillinase and cephalosporinase) produced by various Gram-positive and Gram-negative bacteria. )Stablize. Ceftizoxime sodium has a strong antibacterial effect on Escherichia coli, Klebsiella pneumoniae...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/20C07D501/06
Inventor 陈学文陆婷婷陆建忠华军杰顾利芬
Owner SUZHOU ERYE PHARMA CO LTD
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