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A kind of synthetic method of cefadroxil

A cefadroxil and synthetic method technology, which is applied in the field of cefadroxil synthesis, can solve the problems of large solvent consumption, unfavorable industrial production, and increased production costs, and achieve the effects of reducing production costs, qualified quality indicators, and reducing consumption

Active Publication Date: 2015-08-19
苏州盛达药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This synthesis method consumes a large amount of solvent in the process of forming solvate, which greatly increases the production cost and is not conducive to industrial production.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] (1) In a dry reaction flask, add 50ml of dichloromethane and 25g of 7-ADCA, cool down to -20~-30°C, then add 15g of tetramethylguanidine, stir and dissolve until clear to obtain a 7-ADCA salt solution ;

[0020] (2) Add 50ml of dichloromethane and 50ml of DMF into another dry reaction bottle, then add 40g of hydroxydung salt and stir to dissolve, cool down to -50~-60℃, add 15g of pivaloyl chloride, and control the temperature at -40~- 50°C, react for 1.5 hours to obtain mixed anhydride liquid;

[0021] (3) Add the 7-ADCA salt solution obtained in step (1) under the condition that the temperature control does not exceed -70°C. After the addition is completed, the temperature is controlled at -20~-55°C for 3.0 hours, and 3mol / L hydrochloric acid is added at the end of the reaction 120ml, temperature controlled not to exceed 20°C, stirred and hydrolyzed, layered, dichloromethane was separated, and the aqueous phase was extracted twice with ethyl acetate, each time using 1...

Embodiment 2

[0024] (1) In a dry reaction flask, add 50ml of dichloromethane and 25g of 7-ADCA, cool down to -20~-30°C, then add 15g of tetramethylguanidine, stir and dissolve until clear to obtain a 7-ADCA salt solution ;

[0025] (2) Add 50ml of dichloromethane and 50ml of DMF into another dry reaction bottle, then add 40g of hydroxydane salt and stir to dissolve, cool down to -50~-60℃, add 15g of pivaloyl chloride, and control the temperature at -20~- 50°C, react for 1.5 hours to obtain mixed anhydride liquid;

[0026] (3) Add the 7-ADCA salt solution obtained in step (1) under the condition that the temperature control does not exceed -70°C. After the addition is completed, the temperature is controlled at -20~-55°C for 3.0 hours, and 3mol / L hydrochloric acid is added at the end of the reaction 120ml, temperature controlled not to exceed 20°C, stirred and hydrolyzed, layered, dichloromethane was separated, and the aqueous phase was extracted twice with dichloromethane, each time with ...

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Abstract

The invention discloses a synthetic method of cefadroxil. The synthetic method of cefadroxil comprises the following steps of: dissolving 7-aminodesacetoxycephalosporanic acid by adopting organic base at the temperature ranging from minus 10 DEG C to minus 50 DEG C to obtain 7-aminodesacetoxycephalosporanate; carrying out reaction on HPCDane salt and pivaloyl chloride at the temperature ranging from minus 20 DEG C to minus 70 DEG C to generate mixed anhydride and carrying out condensation reaction on the mixed anhydride and 7-aminodesacetoxycephalosporanate, extracting and regulating pH value of a water layer, then separating salt and regulating pH value, and crystallizing to obtain cefadroxil. By adopting the manner, the synthetic method of cefadroxil has the advantages that a process is simple, solvate does not need to be formed in a synthetic process, crystallization can be directly carried out in water, consumption of an organic solvent is reduced, production cost is reduced, yield of cefadroxil is high, various quality indexes are qualified, pharmacopeia standards are met, and implementation of industrial production can be facilitated.

Description

technical field [0001] The invention relates to the technical field of medicine and chemical industry, in particular to a method for synthesizing cefadroxil. Background technique [0002] Cefadroxil is a semi-synthetic first-generation oral cephalosporin, which is a broad-spectrum oral cephalosporin antibiotic. It has a broad antibacterial spectrum, and its antibacterial activity is similar to that of cefazolin. It is also effective against penicillin-resistant staphylococci. Oral absorption is good, mainly used for urinary tract, biliary tract, and respiratory tract infections, especially suitable for children. [0003] Now the commonly used synthesis process of cefadroxil is to use 7-ADCA as the starting raw material, through condensation with the mixed anhydride generated by hydroxydangium salt and pivaloyl chloride, hydrochloric acid hydrolysis, and the cefadroxil generated and solvent such as DMF or DMAC to form The solvate was separated and dried, and then the solvat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/22C07D501/06
Inventor 陈雷孙悦铭周自金刘要武王璨杨虎星王金龙
Owner 苏州盛达药业有限公司
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