Synthesis process of cefpirome sulfate as antibiotic

A cefpirome sulfate and synthetic method technology, applied in the direction of organic chemistry, etc., can solve the problems of high raw material cost, harsh reaction conditions, long reaction time, etc., and achieve the effects of stable product quality, simple process conditions, and short synthetic route

Active Publication Date: 2007-11-07
苏州盛达药业有限公司
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Problems solved by technology

[0005] In these known synthetic methods, the cost of raw materials is high, and the raw materials are not easy to obtain, the reaction process has various degrees of complexity, the reaction conditions are harsh, and the reaction time is long, which is not conducive to continuous and large-scale industrial production, and the obtained poor product quality

Method used

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  • Synthesis process of cefpirome sulfate as antibiotic

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Embodiment 1

[0021] Add 300 ml of deionized water and 150 ml of DMF into a 500 ml four-necked reaction flask, cool down to 0°C to -5°C, add 20 g of 7-ACP and 31.2 g of AEME, and dropwise add 13.5 ml of triethyl ether within 60 minutes The amine adjusts the pH value at 7.0 to 7.8, controls the temperature at 0°C to -5°C, stirs and reacts for 1 hour, then raises the temperature to 15°C to 18°C, reacts for 6 hours, and uses HPLC to detect that the reaction reaches the end point (residual 7 - After the ACP concentration is lower than 1 mg / ml), the reaction solution is extracted three times with 150 ml of dichloromethane each time. After the organic phase is separated, 5 g of activated carbon is added to the aqueous phase, stirred at room temperature for 30 minutes, filtered, and used 50 ml Deionized water washes gac, the solution that merges filtrate and washing gac obtains, after passing through 50 gram gamma-alumina columns (diameter is 2.5 centimeters, length is the glass chromatography colu...

Embodiment 2

[0025] The DMF in the first embodiment is replaced by DMAC, and the result is the same as that in the first embodiment.

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Abstract

The present invention relates to synthesis process of cefpirome sulfate as one kind of antibiotic. The present invention synthesizes cefpirome sulfate by using 7-amino-3-[(2, 3-cyclopentenyl pyridyl)-1-methyl] cefo phytanic hydrochloride and 2-methoxyimino-2-(2-amino-4-thiazolyl) -(z)-thioacetic benzothiazole ester as the initial material, and through acylation reaction and salt forming reaction. Compared with available technology, the present invention has the advantages of short synthesis path, simple technological condition, low cost, high product yield, high product quality, and being suitable for industrial production.

Description

technical field [0001] The invention relates to a method for synthesizing antibiotic cefpirome sulfate (cefpirome), which belongs to the field of drug synthesis. Background technique [0002] Cefpirome (cefpirome) belongs to the fourth-generation cephalosporin antibiotics. It was first successfully developed by the German company Hoechst and was launched in Sweden and Mexico in 1992. Among the cephalosporin varieties currently on the market, cefpirome is effective against Gram-positive bacteria (G + ) has the strongest antibacterial effect, so the clinical application of cefpirome has received extensive attention. [0003] As the fourth-generation cephalosporin, cefpirome has a wider antibacterial spectrum than the third-generation cephalosporins, and is effective against many antibiotic-resistant pathogens, such as staphylococci, penicillin-resistant pneumonia and enterococci, especially against green The antibacterial effect of Pseudomonas was sim...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/46
Inventor 方长明
Owner 苏州盛达药业有限公司
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