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1/2 water ceftizoxime sodium compound

A technology for hydroceftizoxime and ceftizoxime sodium, which is applied in the field of chemical engineering and pharmaceutical crystallization, can solve the problems of complicated operation, many side reactions, poor fluidity and the like, and achieves wide application prospect, stable product quality and good thermal stability. Effect

Inactive Publication Date: 2019-01-08
王秀香
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Regarding the synthesis of ceftizoxime sodium, three synthetic routes have been reported in the literature, (1) taking p-methoxybenzyl 7-phenylacetamido-3-cephalosporin-4-carboxylate as raw material, and removing the protecting group several times group, and then prepare ceftizoxime sodium with a salt-forming agent. This route has long reaction steps, increases operating procedures and production costs, and has many by-products
(2) Use 7-amino-3-desmethyl-3-cephalosporanic acid (7-ANCA) as the raw material to directly condense with aminothioxime acetic acid, and then form a salt. This route has more side reactions, and the resulting product needs to undergo Alumina chromatographic column purification requires a large amount of eluent, which is costly, complicated to operate and pollutes the environment, and is not suitable for industrial production
[0004] The ceftizoxime sodium compound prepared by the above method has serious problems such as poor storage stability, low thermal decomposition temperature, poor fluidity, and easy moisture absorption.
Thereby influence product quality, cause preparation product unclear, turbidity unqualified, and reduced the stability of preparation, in order to obtain a kind of performance more excellent ceftizoxime sodium compound, propose the present invention

Method used

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  • 1/2 water ceftizoxime sodium compound

Examples

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Embodiment 1

[0027]The preparation of embodiment 1 1 / 2 water ceftizoxime sodium compound

[0028] (1) Add 100g of 7-ANCA into 2L of chloroform, stir to form a suspension, slowly add 200ml of triethylamine, stir for 20min, then add 193g of AE-active ester and react at 30°C for 4h, after the reaction is complete, lower the temperature to 10°C , Add 4L of water for extraction, separate the water phase, add 20g of activated carbon, stir and absorb for 30min, filter, wash, combine the filtrate, adjust the pH value to 2.0 with 2mol / L hydrochloric acid solution, stir and crystallize at 10°C for 1h, filter, and wash with chloroform , dried under vacuum at 30°C for 20 minutes to obtain 169.3 g of ceftizoxime acid;

[0029] (2) Add ceftizoxime acid into 500ml of purified water, stir to form a suspension, lower the temperature to 5°C, slowly add 70ml of triethylamine, stir to dissolve, add 5g of activated carbon and stir for 20min to decolorize, filter, wash with purified water, slowly add Dissolve ...

Embodiment 2

[0033] The preparation of embodiment 2 1 / 2 water ceftizoxime sodium compound

[0034] (1) Add 120g of 7-ANCA into 2.5L of chloroform, stir to form a suspension, slowly add 240ml of triethylamine, stir for 20min, then add 232g of AE-active ester at 35°C for 5h, after the reaction is complete, lower the temperature to 15°C, add 5L of water for extraction, separate the water phase, add 20g of activated carbon, stir and adsorb for 30min, filter, wash, combine the filtrate, adjust the pH value to 2.5 with 2mol / L hydrochloric acid solution, stir and crystallize at 10°C for 1h, filter, trichloro Washed with methane, dried under vacuum at 30°C for 25 minutes to obtain 211.8 g of ceftizoxime acid;

[0035] (2) Add ceftizoxime acid into 500ml of purified water, stir to form a suspension, lower the temperature to 10°C, slowly add 100ml of triethylamine, stir to dissolve, add 5g of activated carbon and stir for 20min to decolorize, filter, wash with purified water, slowly add Dissolve 25...

Embodiment 3

[0039] Example 3 Preparation of 1 / 2 water ceftizoxime sodium compound

[0040] (1) Add 90g of 7-ANCA into 1.5L of chloroform, stir to form a suspension, slowly add 180ml of triethylamine, stir for 20min, then add 174g of AE-active ester and react at 35°C for 4.5h, after the reaction is complete, lower the temperature To 12°C, add 4L of water for extraction, separate the water phase, add 20g of activated carbon, stir and absorb for 20min, filter, wash, combine the filtrate, adjust the pH value to 2.2 with 2mol / L hydrochloric acid solution, stir and crystallize at 12°C for 1.5h, filter, Wash with chloroform, and dry under vacuum at 35°C for 20 minutes to obtain 152.4 g of ceftizoxamic acid;

[0041] (2) Add ceftizoxime acid into 400ml of purified water, stir to form a suspension, lower the temperature to 8°C, slowly add 90ml of triethylamine, stir to dissolve, add 5g of activated carbon and stir for 20min to decolorize, filter, wash with purified water, slowly add Dissolve 200m...

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Abstract

The invention discloses a 1 / 2 water ceftizoxime sodium compound and a preparation method of the 1 / 2 water ceftizoxime sodium compound, each molar of ceftizoxime sodium contains 1 / 2 molar of water, theceftizoxime sodium compound is white crystalline powder, and the ceftizoxime sodium compound has a characteristic diffraction peak when the angle 2theta of the corresponding main X-ray characteristicdiffraction peak is 11.43 plus or minus 0.2 degrees, 13.24 plus or minus 0.2 degrees, 16.54 plus or minus 0.2 degrees, 17.85 plus or minus 0.2 degrees, 19.46 plus or minus 0.2 degrees, 20.66 plus orminus 0.2 degrees, 22.33 plus or minus 0.2 degrees, 23.30 plus or minus 0.2 degrees, 23.65 plus or minus 0.2 degrees, 24.60 plus or minus 0.2 degrees. The 1 / 2 water ceftizoxime sodium compound prepared through the method is excellent stability and meets the requirement of the raw material of a preparation.

Description

technical field [0001] The invention belongs to the technical field of chemical engineering medicine crystallization, and in particular relates to a 1 / 2 water ceftizoxime sodium compound and a preparation method thereof. Background technique [0002] Ceftizoxime Sodium was first developed by Fujisawa Pharmaceutical Co., Ltd., Japan, and was first listed in Japan in 1982. Its trade name is epocelin. It is a third-generation cephalosporin antibiotic. It is biosynthesized to achieve bactericidal effect, and has the characteristics of broad spectrum, high efficiency, enzyme resistance, low toxicity and ability to penetrate the blood-brain barrier. Ceftizoxime sodium is stable to the spectrum β-lactamases produced by various Gram-positive and Gram-negative bacteria; Antibacterial effect, Pseudomonas such as Pseudomonas aeruginosa and Acinetobacter have poor sensitivity to this product; it has good antibacterial effect on Haemophilus influenzae and Neisseria gonorrhoeae; it has g...

Claims

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Application Information

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IPC IPC(8): C07D501/20C07D501/06C07D501/12A61K31/546A61P31/04
CPCC07B2200/13C07D501/06C07D501/12C07D501/20
Inventor 王秀香
Owner 王秀香
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