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A kind of preparation technology of cefotazone

A preparation process, the technology of ceftizonam, which is applied in the field of medicine, can solve the problems of no mature preparation process, etc., and achieve the effect of reducing process cost, cheap price and easy operation

Inactive Publication Date: 2018-04-24
上海博速医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no mature preparation process available for industrial production

Method used

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  • A kind of preparation technology of cefotazone
  • A kind of preparation technology of cefotazone
  • A kind of preparation technology of cefotazone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A kind of preparation technology of ceftizonam of the present invention comprises steps:

[0027] (1) Weigh 2.72g 7-aminocephalosporanic acid (7-ACA, compound I, MW272, 0.01mol), 3.5g AE-active ester (MAEM, compound VII, MW350, 0.01mol), mix and grind evenly, then Add 1.18g of compound III (MW118, 0.01mol) and 21.76g of triethylamine, stir to make the solid-liquid phase fully contact, add 27.2g of polyethylene glycol 400, and stir for 2 minutes;

[0028] (2) 450W microwave reaction for 2 minutes, 800W microwave reaction for 2 minutes, 1000W microwave reaction for 3 minutes;

[0029] (3) After the reaction, the reaction residue was washed with cold water at 0°C, and the remaining solid was dissolved in 48.96g of ethyl acetate, and 13.6g of petroleum ether at 0°C was added to precipitate a white solid, which was vacuum-dried at 40°C for 4 hours to obtain 5.02 gCompound IV (MW513), the yield is 97.9%, the purity is over 99.9%, the single impurity is less than 0.01%, and t...

Embodiment 2

[0032] A kind of preparation technology of ceftizonam of the present invention comprises steps:

[0033] (1) Weigh 2.72g 7-aminocephalosporanic acid (7-ACA, compound I, MW272, 0.01mol), 4.2g AE-active ester (MAEM, compound VII, MW350, 0.012mol), mix and grind evenly, then Add 1.416g of compound III (MW118, 0.012mol) and 27.2g of triethylamine, stir to make the solid-liquid phase fully contact, add 32.64g of polyethylene glycol 400, and stir for 5 minutes;

[0034] (2) 450W microwave reaction for 3 minutes, 800W microwave reaction for 3 minutes, 1000W microwave reaction for 5 minutes;

[0035] (3) After the reaction, the reaction residue was washed with cold water at 5°C, and the remaining solid was dissolved in 65.28g of ethyl acetate, and 21.76g of petroleum ether at 5°C was added to precipitate a white solid, which was vacuum-dried at 50°C for 6 hours to obtain 5.04 gCompound IV (MW513), the yield is 98.2%, the purity is over 99.9%, the single impurity is less than 0.01%, a...

Embodiment 3

[0038] A kind of preparation technology of ceftizonam of the present invention comprises steps:

[0039] (1) Weigh 2.72g 7-aminocephalosporanic acid (7-ACA, compound I, MW272, 0.01mol), 3.85g AE-active ester (MAEM, compound VII, MW350, 0.011mol), mix and grind evenly, then Add 1.298g of compound III (MW118, 0.011mol) and 24.48g of triethylamine, stir to fully contact the solid-liquid phase, add 29.92g of polyethylene glycol 400, and stir for 3 minutes;

[0040] (2) 450W microwave reaction for 2 minutes, 800W microwave reaction for 3 minutes, 1000W microwave reaction for 4 minutes;

[0041] (3) After the reaction, the reaction residue was washed with cold water at 0°C, and the remaining solid was dissolved in 54.4g of ethyl acetate, and 19.04g of petroleum ether at 0°C was added to precipitate a white solid, which was vacuum-dried at 40°C for 6 hours to obtain 5.09 gCompound IV (MW513), the yield is 99.2%, the purity is over 99.9%, the single impurity is less than 0.01%, and t...

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Abstract

The invention discloses a process for preparing cefuzonam. The process includes steps of (1), weighing 7-aminocephalosporanic acid (7-ACA, a chemical compound I) and AE-mica ester (AEMA, a chemical compound II), mixing the 7-aminocephalosporanic acid and the AE-mica ester with each other to obtain a mixture, then uniformly grinding the mixture, adding a chemical compound III and triethylamine into the mixture, stirring the chemical compound III, the triethylamine and the mixture so allow solid phases and liquid phases to be in sufficient contact with one another, adding polyethylene glycol 400 into the solid phases and the liquid phases and stirring the polyethylene glycol 400, the solid phases and the liquid phases for 2-5 minutes; (2), carrying out 450W microwave reaction for 2-3 minutes, carrying out 800W microwave reaction for 2-3 minutes and carrying out 1000W microwave reaction for 3-5 minutes; (2), washing reaction residues by the aid of cold water at the temperature of 0-5 DEG C after reaction is completed, dissolving remaining solid in ethyl acetate, adding petroleum ester at the temperature of 0-5 DEG C into the remaining solid, dissolving out white solid and drying the white solid to obtain a chemical compound IV. The process has the advantages that the microwave one-pot reaction is carried out, so that various reactants are in sufficient contact with one another by the aid of the polyethylene glycol 400 which is a surfactant under the alkaline actions of the triethylamine, the process is easy and convenient to implement and short in reaction time, and the high-purity cefuzonam can be obtained in a high-yield manner.

Description

technical field [0001] The invention relates to a preparation process, in particular to a preparation process of ceftriaxone sodium. It belongs to the field of medical technology. Background technique [0002] Ceftizolam is a fourth-generation semi-synthetic cephalosporin with broad-spectrum antibacterial activity, and its mechanism of action is similar to other cephalosporins. Ceftizonam is stable to β-lactamase and has high affinity to penicillin-binding protein (PBP) 1a, 1b, 3. It achieves bactericidal effect by inhibiting the formation of peptidoglycan crosslinks and inhibiting the synthesis of bacterial cell walls. For Staphylococcus aureus resistant to methicillin and cephem, it also shows antibacterial activity because of its affinity to the specific penicillin-binding protein (PBP) 2 that appears. [0003] This product is effective against Gram-positive bacteria such as Staphylococcus, Streptococcus, and Methicillin- and Cephem-resistant Staphylococcus aureus, and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/36C07D501/04
CPCC07D501/04C07D501/36
Inventor 张李锋
Owner 上海博速医药科技有限公司
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