Method for preparing ampicillin from benzylpenicillin potassium

A technology of penicillin potassium and ampicillin, which is applied in the field of preparing ampicillin and ampicillin from penicillin potassium, which can solve problems such as difficulty in application, low concentration, and impact on the quality of ampicillin products, and achieve the effect of less colored impurities and high concentration

Active Publication Date: 2017-03-22
INNER MONGOLIA CHANGSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Synthesis of ampicillin by the straight-through process exists: (1) the residual phenylacetic acid in the obtained 6-APA solution after extraction from the lysate has an inhibitory effect on the synthetase enzyme activity, (2) the 6-APA in the 6-APA solution The concentration is low, (3) 6-APA is prepared by the filtrate through a straight-through process, and the extracted aqueous phase of the gained contains a certain amount of colored impurities, which will affect the quality of ampicillin and other issues
It is difficult to obtain the application of the process of synthesizing ampicillin by the straight-through method

Method used

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  • Method for preparing ampicillin from benzylpenicillin potassium
  • Method for preparing ampicillin from benzylpenicillin potassium
  • Method for preparing ampicillin from benzylpenicillin potassium

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Embodiment 1

[0035] Embodiment 1 The method for preparing ampicillin by penicillin potassium according to the present invention

[0036] (1) Penicillin Potassium Cleavage

[0037] Weigh 10kg of penicillin potassium, add 100L of purified water, stir and dissolve, so that the penicillin potassium is completely dissolved, the mass concentration is 10%, then add 11.72kg of penicillin G acylase, the enzyme activity is 150u / g; Add 3.0 mol / L ammonia water to the solution, control the pH of the feed solution to 8.0, control the reaction temperature to 30°C, react for 48 minutes, stop the reaction, separate the feed solution from penicillin G acylase to obtain 125 L of penicillin potassium lysate, and take samples for determination The concentration of 6-APA was 45.82g / L, the concentration of phenylacetic acid was 28.73g / L, and the cleavage yield was 98.73%;

[0038] (2) Extraction

[0039] Lower the temperature of the penicillin potassium lysate obtained in step (1). When the temperature drops t...

Embodiment 2

[0056] Embodiment 2 The method for preparing ampicillin by penicillin potassium according to the present invention

[0057] (1) Penicillin Potassium Cleavage

[0058] Weigh 10kg of penicillin potassium, add 125L of purified water, stir and dissolve, so that the penicillin potassium is completely dissolved, the mass concentration is 8%, then add 11.72kg of penicillin G acylase, the enzyme activity is 150u / g; Add 3.0 mol / L ammonia water to the solution, control the pH of the feed solution to 8.2, control the reaction temperature to 28°C, react for 48 minutes, stop the reaction, separate the feed solution from penicillin G acylase to obtain 160 L of penicillin potassium lysate, and take samples for determination The concentration of 6-APA was 35.81g / L, the concentration of phenylacetic acid was 22.58g / L, and the cleavage yield was 98.68%;

[0059] (2) Extraction

[0060] The penicillin potassium lysate obtained in step (1) is cooled. When the temperature drops to 2° C., add 80 ...

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Abstract

The invention relates to a method for preparing ampicillin from benzylpenicillin potassium and belongs to the technical field of pharmacy. According to the method for preparing the ampicillin from the benzylpenicillin potassium, the benzylpenicillin potassium is split into 6-APA and phenylacetic acid under the action of penicillin acylase, a lysis solution is extracted through dichloromethane, and the 6-APA is separated from the phenylacetic acid. Ammonia water is added into an extracted water phase, the pH of a feed solution is adjusted to the neutral level, the dichloromethane is removed, the obtained feed solution is subjected to concentration by nanofiltration, and the ampicillin is synthesized by a concentrated solution and D-phenylglycine methyl ester hydrochloride under the action of amoxicillin synthetase. The inhibiting effect of the phenylacetic acid remaining in the 6-APA solution obtained after extracting the lysis solution on the enzyme activity of the synthetase is overcome, the concentration of the 6-APA in the 6-APA solution is high, few colored impurities exist in the extraction and do not influence the quality of ampicillin products, and the method for preparing the ampicillin from the benzylpenicillin potassium is easily applied to production.

Description

technical field [0001] The invention relates to a method for preparing ampicillin, in particular to a method for preparing ampicillin from penicillin potassium, and belongs to the technical field of pharmacy. Background technique [0002] Ampicillin can be synthesized by chemical and enzymatic methods. The chemical synthesis of ampicillin requires steps such as group protection and deprotection, and a large amount of organic reagents are used in the reaction process, and the reaction conditions are relatively harsh. Now it has been replaced by an enzymatic process with mild reaction conditions and environmental friendliness. In the process of enzymatic synthesis of ampicillin, it is necessary to dissolve the 6-APA solid with alkali to obtain a 6-APA solution, and the 6-APA solution and the solution of D-phenylglycine methyl ester hydrochloride are respectively put into the Carry out reaction synthetic ampicillin in the reaction tank of enzyme. The lysate is extracted, cry...

Claims

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Application Information

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IPC IPC(8): C12P37/04C12P37/02C07D499/68C07D499/18
CPCC07D499/18C07D499/68C12P37/04
Inventor 陈顺记陈英新眭谦郭建明王继明韩贺东
Owner INNER MONGOLIA CHANGSHENG PHARMA
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