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A kind of method for preparing amoxicillin by deesterification liquid

A technology of amoxicillin and deesterification solution, which is applied in the field of preparing amoxicillin from deesterification solution and preparing amoxicillin and phenylacetic acid, which can solve the impact of amoxicillin product quality, unfavorable amoxicillin synthesis yield, 6 -The problem of low APA concentration, to achieve the effect of less colored impurities, good product quality and high yield

Active Publication Date: 2021-05-04
INNER MONGOLIA CHANGSHENG PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The problems in the synthesis of amoxicillin by the straight-through method are: (1) there is phenylacetic acid residue in the 6-APA solution obtained after the lysate is extracted, and phenylacetic acid has an inhibitory effect on amoxicillin synthase
(2) In the process of preparing 6-APA by an enzymatic method, the substrate concentration of the existing immobilized penicillin acylase is low, resulting in a low concentration of 6-APA in the lysate, and finally the 6-APA in the aqueous phase obtained by extraction is low. -The low concentration of APA is not conducive to the improvement of the yield of subsequent amoxicillin synthesis
(3) 6-APA is prepared by the filtrate through a straight-through process, and the extracted aqueous phase contains a certain amount of colored impurities, which will affect the quality of the subsequently synthesized amoxicillin

Method used

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  • A kind of method for preparing amoxicillin by deesterification liquid
  • A kind of method for preparing amoxicillin by deesterification liquid
  • A kind of method for preparing amoxicillin by deesterification liquid

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Embodiment 1

[0035] Embodiment 1 The method for preparing amoxicillin by deesterification solution according to the present invention

[0036] (1) Deesterification solution cracking

[0037] Take 200L deesterification solution, the penicillin titer is 178560u / mL, add 48L purified water, then add 25.34kg penicillin G acylase, the enzyme activity is 155u / g; start stirring, add 3.0mol / L ammonia water to the feed solution, Control the pH of the feed solution to 8.10, control the reaction temperature to 31°C; react for 50 minutes, stop the reaction, separate the enzyme from the feed solution to obtain 285L of lysate, sample and determine the concentration of 6-APA to be 45.21g / L, and the cleavage yield to be 99.30 %;

[0038] (2) Extraction

[0039] The lysate obtained in step (1) was cooled down. When the temperature dropped to 6° C., 285 L of dichloromethane was added to the lysate. The temperature of the methylene chloride was 5° C. Under stirring conditions, 30% hydrochloric acid was adde...

Embodiment 2

[0056] Embodiment 2 The method for preparing amoxicillin by deesterification solution according to the present invention

[0057] (1) Penicillin Potassium Cleavage

[0058] Take 200L of deesterification solution, the penicillin titer is 172980u / mL, add 40L of purified water, then add 24.55kg of penicillin G acylase, the enzyme activity is 155u / g, start stirring, add 3.0mol / L ammonia water into the reaction tank, Control the pH of the feed liquid to be 8.0-8.2, control the reaction temperature to be 28-31°C, react for 53 minutes, stop the reaction, separate the enzyme from the feed liquid to obtain 282L of lysate, take a sample to determine the concentration of 6-APA is 44.35g / L, crack The yield is 99.49%;

[0059] (2) Extraction

[0060] The lysate obtained in step (1) was cooled down. When the temperature dropped to 5° C., 141 L of dichloromethane was added to the lysate. The temperature of the methylene chloride was 5° C. Under stirring conditions, 30% hydrochloric acid wa...

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Abstract

The invention relates to a method for preparing amoxicillin from a deesterification solution, belonging to the technical field of pharmacy. In the method of the present invention, the deesterification liquid is subjected to the action of lyase to obtain a lysate containing 6-APA and phenylacetic acid. The lysate is extracted to obtain an aqueous phase containing 6-APA, the aqueous phase is basified, solvent removed and nanofiltration concentrated to obtain a solution with a higher concentration of 6-APA, which is mixed with D-hydroxyphenylglycine methyl ester The crude amoxicillin was synthesized under the action of penicillin G acylase. The crude amoxicillin is extracted by acidification, crystallized, washed and dried to obtain the finished amoxicillin. The process saves steps such as crystallization, washing and drying of 6-APA, saves the treatment of 6-APA mother liquor, simplifies the production process, improves the yield of amoxicillin, and reduces the production cost.

Description

technical field [0001] The invention relates to a method for preparing amoxicillin and phenylacetic acid, in particular to a method for preparing amoxicillin from a deesterified liquid, and belongs to the technical field of pharmacy. Background technique [0002] There are chemical and enzymatic methods for the synthesis of amoxicillin. Because the chemical method uses a large amount of toxic substances and the reaction conditions are relatively harsh, it has been replaced by the enzymatic method with mild reaction conditions and water phase reaction. The process of enzymatically synthesizing amoxicillin is as follows: 6-APA and D-hydroxyphenylglycine methyl ester synthesize amoxicillin under the action of penicillin G acylase, and the crude amoxicillin obtained is acidified, crystallized, washed and Dry to get amoxicillin. The lysate containing 6-APA and phenylacetic acid can be used to replace the 6-APA solid to carry out the synthesis of amoxicillin, and the crystalliza...

Claims

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Application Information

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IPC IPC(8): C12P37/00C07D499/68C07D499/18
CPCC07D499/18C07D499/68C12P37/00
Inventor 眭谦陈英新陈顺记王继明郭建明韩贺东
Owner INNER MONGOLIA CHANGSHENG PHARMA
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