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Method for preparing cefditoren pivoxil

A technology of cefditoren axetil and ethyl acetate, applied in the direction of organic chemistry, antibacterial drugs, etc., can solve the problems of perishable yield, troublesome operation, etc.

Inactive Publication Date: 2011-06-15
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its shortcoming lies in the deficiencies in several aspects: troublesome operation, easy deterioration of the product in the purification process and low yield

Method used

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  • Method for preparing cefditoren pivoxil

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Effect test

Embodiment 1

[0021] Under the condition of avoiding light, 5 g of crude cefditoren axetil with a purity of 96.6% (as determined by HPLC) was dissolved in 100 mL of ethyl acetate at a temperature of 0° C. After washing three times with 40 mL of 1% dilute hydrochloric acid, the aqueous phases were combined, adjusted to pH = 2 with 0.1% wt sodium bicarbonate, and extracted three times with 50 mL of ethyl acetate. The organic phases were combined, washed twice with 100 mL of deionized water, dried with anhydrous sodium sulfate, and treated with activated carbon, the solvent was recovered under reduced pressure, and dried in a vacuum in the dark to obtain cefditoren axetil in a light yellow solid form, with a quality of 4.6 g, purity 98.8%, determined by HPLC.

Embodiment 2

[0023] Under the condition of avoiding light, 5 g of crude cefditoren axetil with a purity of 93.7% (as determined by HPLC) was dissolved in 30 mL of DMF at a temperature of 5° C. After it dissolves, transfer it into a pre-cooled mixed system of 100 mL ethyl acetate and 100 mL deionized water, keep stirring at 0°C for 10 min, and separate the liquids. The organic phases were combined and washed three times with 40 mL of 1% dilute hydrochloric acid, and the aqueous phases were combined, adjusted to pH = 2 with 5% wt sodium bicarbonate, and extracted three times with 50 mL of ethyl acetate. The organic phase was washed with water at a temperature of 5°C, dilute alkali, dilute acid and water, dried with anhydrous sodium sulfate, treated with activated carbon, recovered the solvent under reduced pressure, and dried under vacuum to obtain cefditoren in the form of light yellow solid The ester has a mass of 3.9 g and a purity of 98.1%, determined by HPLC.

Embodiment 3

[0025] Under the condition of avoiding light, 5 g of crude cefditoren axetil with a purity of 93.7% (as determined by HPLC) was dissolved in 30 mL of DMF at a temperature of 5° C. After it dissolves, transfer it into a pre-cooled mixed system of 100 mL ethyl acetate and 100 mL deionized water, keep stirring at 0°C for 10 min, and separate the liquids. The organic phases were combined and washed three times with 40 mL of 1% dilute hydrochloric acid, then the aqueous phases were combined, adjusted to pH=2 with 1% wt of sodium carbonate, and extracted three times with 50 mL of ethyl acetate. The organic phase was washed with water at a temperature of 5°C, dilute alkali, dilute acid and water, dried with anhydrous sodium sulfate, treated with activated carbon, recovered the solvent under reduced pressure, and dried under vacuum to obtain cefditoren in the form of light yellow solid The ester has a mass of 3.8 g and a purity of 98.2%, determined by HPLC.

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Abstract

The invention discloses a method for preparing cefditoren pivoxil in the technical field of medicine, which comprises: dissolving a cefditoren pivoxi crude product in a water-soluble solvent; preparing a cefditoren pivoxil organic phase; preparing a cefditoren pivoxil aqueous phase; and adjusting the pH value of the solution, performing acid extraction treatment and menstruum crystallization treatment, and obtaining the cefditoren pivoxil with the purity of 98.1 to 98.8 percent. The method ensures that the cefditoren pivoxil can obtain high-purity products according with pharmacopoeia throughpurification under stable condition by simple operation.

Description

technical field [0001] The invention relates to a preparation method in the technical field of medicines, in particular to a preparation method of cefditoren axetil. Background technique [0002] Cefditoren Pivoxil (Cefditoren Pivoxil) is a new type of cephalosporin antibiotic listed in Japan under the trade name of Meiact (Meiact) by the Japanese Meiji Fruit Company in 1994. After absorption, it is hydrolyzed into active cefditoren to exert antibacterial effect. Studies have shown that cefditoren axetil is effective in the treatment of community-acquired respiratory tract infections caused by five major pathogenic bacteria: Streptococcus pneumoniae, Haemophilus influenzae, Streptococcus pyogenes, Staphylococcus aureus, and Moraxella catarrhalis. Compared with third-generation cephalosporins, quinolones, macrolides, and β-lactam antibiotics containing enzyme inhibitors, cefditoren axetil is effective against these five major pathogens, especially against penicillin-resistan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/24C07D501/12A61P31/04
Inventor 张万斌刘德龙
Owner SHANGHAI JIAO TONG UNIV
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