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Method for enzymatic synthesis of penicillin V salt

A technology of penicillin V and enzymatic synthesis, which is applied in the field of medicine and chemical industry to achieve the effects of good product quality, low cost and short production cycle

Active Publication Date: 2019-04-16
HUNAN FLAG BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the fermentation method, the enzymatic synthesis method has the advantages of short production cycle, simple process, mild reaction conditions, high conversion rate, less by-products, less impurity content, and high product quality. Open literature report of penicillin V salt

Method used

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  • Method for enzymatic synthesis of penicillin V salt
  • Method for enzymatic synthesis of penicillin V salt
  • Method for enzymatic synthesis of penicillin V salt

Examples

Experimental program
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Effect test

Embodiment 1

[0032]Take 25.0g 6-APA, add 300mL pure water, drop 3mol / L ammonia solution to fully dissolve 6-APA, add 30.0g ethylene glycol phenoxyacetate, mix well, add 50.0g immobilized penicillin acylase , add dropwise 3mol / L ammonia solution to make the reaction pH 5.0, temperature 30°C, react for 90 minutes and take samples for HPLC detection. At this time, the concentration of 6-APA is 0.8mg / mL, and the concentration of penicillin V is 106.9mg / mL; Separate the immobilized enzyme and the reaction solution, adjust the pH value of the reaction solution to 3.0 with 6mol / L hydrochloric acid, grow the crystal for 20 minutes, and filter to obtain the penicillin V acid filter cake; the filter cake is transferred to 5 times the weight of pure water, and the Potassium carbonate solution of a certain concentration adjusts the pH value of the mixed solution to 6.0, then adds n-butanol to a certain concentration, evaporates and concentrates under reduced pressure until crystals are separated out, a...

Embodiment 2

[0034] Take 25.0g 6-APA, add 400mL pure water, add dropwise 3mol / L ammonia solution to fully dissolve 6-APA, add 30.0g phenoxyacetate glyceride, mix well, add 75.0g immobilized penicillin acylase, drop Add 3 mol / L ammonia solution to make the reaction pH 6.0, temperature 20°C, react for 80 minutes and take samples for HPLC detection. At this time, the concentration of 6-APA is 0.3 mg / mL, and the concentration of penicillin V is 87.5 mg / mL; catalyze and reaction solution, adjust the pH value of the reaction solution to 2.8 with 6mol / L hydrochloric acid, grow crystals for 20 minutes, and filter to obtain penicillin V acid filter cake; transfer the filter cake to 4 times the weight of pure water, potassium carbonate solution to adjust the pH value of the mixed solution to 6.3, then add n-butanol to a certain concentration, evaporate and concentrate under reduced pressure until crystals are precipitated, and the crystals are filtered, washed, and dried to obtain 39.1 g of penicilli...

Embodiment 3

[0036] Take 25.0g 6-APA, add 400mL pure water, add dropwise 3mol / L ammonia solution to fully dissolve 6-APA, add 35.0g phenoxyacetate butanetetrayl ester, mix well, add 50.0g immobilized penicillin acylase , add dropwise 3mol / L ammonia solution to make the reaction pH 5.0, temperature 30°C, react for 90 minutes and sample HPLC for detection. At this time, the concentration of 6-APA is 0.5mg / mL, and the concentration of penicillin V is 89.0mg / mL; Separate the immobilized enzyme and the reaction solution, adjust the pH value of the reaction solution to 2.8 with 6mol / L hydrochloric acid, grow the crystal for 20 minutes, filter to obtain the penicillin V acid filter cake; transfer the filter cake to 4 times the weight of pure water, and use Potassium carbonate solution of a certain concentration adjusts the pH value of the mixed solution to 6.5, then adds n-butanol to a certain concentration, evaporates and concentrates under reduced pressure until crystals are precipitated, and th...

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Abstract

The invention discloses a method for enzymatic synthesis of penicillin V salt. The method comprises the steps of enzymatically catalyzing the reaction of 6-APA and a phenoxyacetic acid derivative anda penicillin acylase catalyst to generate penicillin V; acidizing and dissolving out a penicillin V crystal after acylation enzyme in the solution is separated, and salting the penicillin V crystal toobtain the penicillin V salt. Compared with the prior art, the production period of the method is short, the method is simple in operation, friendly to the environment, free of pollution and low in production cost, the liquid phase purity of the prepared penicillin V salt can reach 99.7% or above, 4-hydroxyphenoxymethyl penicillin (impurity D) is not detected out, the polymer impurity is less than 0.02%, the product quality far exceeds the quality of the penicillin V salt produced by an existing fermentation method and is higher than the quality standards of similar foreign drug materials, and the method has a good industrial application value.

Description

technical field [0001] The invention relates to a method for synthesizing penicillin V salt, in particular to a method for generating penicillin V by reacting 6-APA and phenoxyacetic acid derivative raw materials in the next step under the catalysis of penicillin acylase, and belongs to the technical field of medicine and chemical industry. Background technique [0002] Penicillin V salts (penicillin V potassium, penicillin V sodium) are clinically commonly used antibiotics, and penicillin V potassium is more widely used. Penicillin V Potassium is a β-lactamase antibiotic. Its antibacterial spectrum is similar to that of penicillin G. It can destroy bacterial cell walls and has bactericidal effect. Abscess, purulent meningitis, pneumonia, gonorrhea embolism. Compared with penicillin G potassium / sodium, penicillin V potassium is stable to acid, not easy to be destroyed by gastric acid, and has good oral absorption, and its oral preparation is especially suitable for children...

Claims

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Application Information

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IPC IPC(8): C12P37/04
CPCC12P37/04
Inventor 许岗张娇黄斌苏程举曾红宇赵士敏
Owner HUNAN FLAG BIOTECHNOLOGY CO LTD
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