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Technology for preparing ampicillin by adopting enzymic method

A technology for ampicillin and enzymatic preparation, applied in the field of drug preparation, can solve the problems of cumbersome ampicillin process steps, high requirements for industrial control, and long reaction time, and achieve no solvent recovery, high product purity, and short reaction time Effect

Active Publication Date: 2014-05-21
NORTH CHINA PHARM GRP SEMISYNTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to provide a process for the preparation of ampicillin by enzymatic method, so as to solve the problems of cumbersome process steps, high industrial control requirements, low conversion rate and long reaction time in the preparation of ampicillin by existing enzymatic method

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Mix 0.058mol of 6-APA, 0.06mol of phenylglycine methyl ester hydrochloride, 2000IU of immobilized penicillin G acylase and 200mL of water, adjust the pH value of the reaction solution to 5.7 with sulfuric acid and sodium carbonate, and keep the temperature at 15 Reaction was carried out at -20°C; at the end of the reaction, the residual amount of 6-APA was at 5mM, and then the immobilized penicillin G acylase was separated from the reaction solution containing the ampicillin product; , adjusted to pH = 0.8-1.0 with hydrochloric acid, filtered, adjusted to crystallization with sodium bicarbonate, adjusted to pH = 5.0 at the end point; grown at 5°C for 3 hours, washed and dried to obtain ampicillin.

Embodiment 2

[0024] Mix 0.058mol of 6-APA, 0.073mol of phenylglycine methyl ester hydrochloride, 2000IU of immobilized penicillin G acylase and 200mL of water, adjust the pH value of the reaction solution to 5.9 with sulfuric acid and sodium carbonate, and keep the temperature at 15 Reaction was carried out at -20°C; at the end of the reaction, the residual amount of 6-APA was at 5mM, and then the immobilized penicillin G acylase was separated from the reaction solution containing the ampicillin product; , adjusted to pH = 0.8-1.0 with hydrochloric acid, filtered, adjusted to crystallization with sodium bicarbonate, adjusted to pH = 4.5 at the end point; grown at 8°C for 2 hours, washed and dried to obtain ampicillin.

Embodiment 3

[0026] Mix 0.058mol of 6-APA, 0.07mol of phenylglycine methyl ester nitrate, 1724IU of immobilized penicillin G acylase and 200mL of water, adjust the pH value of the reaction solution to 5.9 with sulfuric acid and sodium carbonate, and keep the temperature at 0- React at 10°C; when the residual amount of 6-APA is not higher than 10mM, the reaction ends, and then the penicillin G acylase is separated from the reaction solution containing the ampicillin product; the resulting solution containing the ampicillin product is heated at 35°C , use sulfuric acid to adjust the pH to 0.6, filter, adjust the crystallization with sodium carbonate, and adjust to the final pH=4.0; grow the crystal at 10°C for 3 hours, wash and dry to obtain ampicillin.

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Abstract

The invention discloses a technology for preparing ampicillin by adopting an enzymic method. The technology comprises the following steps of (a) mixing 6-aminopenicillanic acid, a phenylglycine derivative and penicillin G acylase into water to obtain mixed liquid; (b) adjusting and controlling the pH value of the mixed liquid to be 5.5-6.1 through acid or alkaline, and reacting under the temperature of 0-40 DEG C; (c) after the reaction is finished, performing separation, cleaning reaction liquid containing a coarse ampicillin product through the acid, crystallizing the reaction liquid through the alkaline, and performing grain cultivation, washing and drying to obtain an ampicillin product. The preparation technology provided by the invention is simple, convenient to operate, low in energy consumption, high in safety and high in stability; furthermore, the pH value required by a reaction system is easy to control, the reaction time is short, the conversion rate is up to over 99 percent, the product purity is high, and a solvent does not need to be recycled; and therefore, the low-cost and high-efficiency production technology can be popularized and applied in the industrial production.

Description

technical field [0001] The invention relates to a preparation method of medicine, in particular to a process for preparing ampicillin by enzymatic method. Background technique [0002] Ampicillin is a β-lactam antibiotic. In addition to its broad-spectrum antibacterial activity, strong bactericidal activity, low toxicity, wide indications and wide clinical application, it is also a raw material for the synthesis of many semi-synthetic penicillins, such as: ampicillin sodium , piperacillin, mezlocillin, azlocillin, etc. Therefore, the production demand of the drug is relatively large. [0003] At present, the synthesis methods of the drug are mainly chemical and enzymatic methods. The chemical synthesis process is cumbersome, the conditions are harsh, and the pollution to the environment is relatively large; while the enzymatic synthesis can significantly reduce the reaction steps, the conditions are mild, the energy consumption is reduced, and the environmental pollution i...

Claims

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Application Information

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IPC IPC(8): C12P37/04
Inventor 左丽华严正人刘慧勤朱军魏士倩
Owner NORTH CHINA PHARM GRP SEMISYNTECH CO LTD
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