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Prepn of amoxcillion sodium

A technology of amoxicillin sodium and amoxicillin, which is applied in the field of western medicine synthesis, can solve the problems of strong toxic and side effects of dibutylamine solvent, low product content, and product allergy easily.

Inactive Publication Date: 2002-08-07
HEBEI XINZHANG PHARMA
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  • Abstract
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Problems solved by technology

[0003] There are two production methods of amoxicillin sodium salt, one is to suspend amoxicillin trihydrate in water or a mixture of water and isopropanol, add sodium hydroxide solution to dissolve it, and freeze-dry or The sodium salt is separated by spray drying. This method has the disadvantages of low product content, high content of degraded substances, and the product is prone to allergies. In the amine organic solvent of Amoxicillin such as dibutylamine, this method has the disadvantages that the dibutylamine solvent used has strong toxic and side effects, and is not conducive to labor protection of workers.

Method used

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Embodiment Construction

[0030] A preparation method of amoxicillin sodium, which comprises first reacting amoxicillin trihydrate with triethylamine and then purifying, then reacting with purified sodium isooctanoate, crystallizing, filtering, washing and drying to obtain the finished product .

[0031] Wherein, the reaction between the amoxicillin trihydrate and triethylamine is carried out in the presence of anhydrous methanol, methyl acetate, and isopropanol, and the amoxicillin trihydrate is completely dissolved and then cooled to 0-5°C; Wherein the proportioning of parts by weight of each raw material is:

[0032] Amoxicillin trihydrate 35 parts

[0033] 25 parts of triethylamine

[0034] 40 parts of anhydrous methanol

[0035] 38 parts of isopropanol

[0036] 25 parts methyl acetate

[0037] The purification of the sodium isooctanoate includes dissolving sodium isooctanoate in a mixed solution of methyl acetate and anhydrous methanol, and obtaining the filtrate through filtration to obtain ...

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Abstract

The preparation method of amoxicillin sodium includes the following steps: firstly, making amoxicillin trihydric acid react with triethylamine, and making purification, then making obtained product react with purified sodium isocaprylate, crystallizing, filtering, washing and drying to obtain the invented product with high quality.

Description

field of invention [0001] The invention relates to a synthesis method of western medicine, in particular to a preparation method of amoxicillin sodium. technical background [0002] Amoxicillin is a semi-synthetic penicillin created by the British BEECHAM company. So far, there have been many patents on the synthesis method of Amoxicillin and its improved method, but the most commonly used method for large-scale production is the same as the principle in the monograph published in 1978. Similarly, the amino group of D-(-)-P-hydroxyphenylglycine reacts with ethyl methylacetate to form an internal amine that is protected to generate Dane salt. Remove the solvent, separate the solid Dane salt, suspend in acetone or dichloromethane, and react with ethyl chloroformate or trimethylacetyl chloride under the action of a basic catalyst such as N-methylmorpholine at -10-50°C , to form a mixed acid anhydride, add 6-chloropenicillanic acid (6-APA) in the dichloromethane solvent of trie...

Claims

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Application Information

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IPC IPC(8): C07D499/68
Inventor 冯兰春金志勇
Owner HEBEI XINZHANG PHARMA
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