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Preparation method of cefadroxil

A cefadroxil and magnetic technology, applied in the field of medicine, can solve the problems of decreased catalytic activity of penicillin acylase, harm to ecological environment due to volatile organic solvent, low yield of target product and the like

Active Publication Date: 2022-05-24
NINGXIA UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Although the use of organic reagent solvents can inhibit the hydrolysis reaction to a certain extent, the catalytic activity of penicillin acylase in organic solvents capable of dissolving substrates has declined significantly, resulting in low yields of target products; and the volatility of organic solvents Harmful to the ecological environment

Method used

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  • Preparation method of cefadroxil
  • Preparation method of cefadroxil
  • Preparation method of cefadroxil

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preparation example Construction

[0028] A method for preparing cefadroxil provided by the invention comprises the following steps: adding a predetermined volume of ionic liquid and a phosphate buffer solution to a reactor with a constant temperature in a water bath to form a co-solvent; adding a predetermined molar ratio of D to the co-solvent -HPGM and 7-ADCA and stirring them, the molar ratio of D-HPGM and 7-ADCA is 1:1~1:2.0; the concentration of 7-ADCA is 0.1~1.0mol / L; The magnetically immobilized penicillin G acylase was added to the co-solvent of ADCA, and the mass ratio of the magnetically immobilized penicillin G acylase to 7-ADCA was 1:10 to 1:50, and the magnetically immobilized penicillin G acylase was continuously stirred. Fully contact with D-HPGM and 7-ADCA until the end of the reaction, wherein the stirring speed is controlled to be 150 to 250r / min; the reaction system liquid after the reaction ends is layered and left to stand, so that the upper layer of phosphate buffered with cefadroxil is di...

Embodiment 1

[0036] Embodiment 1, add 60mL ionic liquid 1-butyl-3-methylimidazole bis-trifluoromethanesulfonimide salt and 40mL sodium phosphate buffer solution (0.10mol / L, pH 7.0) in the reactor, after mixing evenly 0.1 mol of 7-ADCA and 0.15 mol of D-HPGM were added, and the concentration of 7-ADCA at this time was 214 g / L. Then add 0.42g magnetic immobilized penicillin G acylase, at this time the mass ratio of the immobilized enzyme to 7-ADCA is 1:50, the temperature of the water bath is controlled at 30°C, the stirring speed is controlled to be 150r / min, and the reaction is performed for 10 hours. The immobilized enzyme was isolated under the action. The pH value of the upper layer solution of the separated reaction system was adjusted to 5.2, and crystals of cefadroxil were obtained by crystallization. The reactor can be a batch reactor commonly used in the industry.

Embodiment 2

[0037] Embodiment 2, add 60mL ionic liquid 1-butyl-3-methylimidazolium hexafluorophosphate and 40mL sodium phosphate buffer solution (0.10mol / L, pH 7.0) in the reactor, add 0.1mol 7- ADCA and 0.15mol D-HPGM, the concentration of 7-ADCA at this time was 214g / L. Then 0.42g of magnetically immobilized penicillin G acylase was added, the mass ratio of the immobilized enzyme and 7-ADCA was 1:50, the temperature of the water bath was controlled at 30°C, the stirring speed was controlled to be 150r / min, and the reaction was performed for 10 hours. The immobilized enzyme was isolated. The pH value of the upper layer solution of the separated reaction system was adjusted to 5.0, and crystals of cefadroxil were obtained by crystallization.

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Abstract

A method for preparing cefadroxil, comprising the steps of: adding a predetermined volume of ionic liquid and a phosphate buffer solution to form a co-solvent in a water-bath constant temperature reactor; adding D-HPGM and 7-ADCA of a predetermined molar ratio to the co-solvent and stirring it, the molar ratio of D-HPGM and 7-ADCA is 1:1~1:2.0; the concentration of 7-ADCA is 0.1~1.0mol / L; Magnetically immobilize penicillin G acylase, and keep stirring to make the magnetically immobilized penicillin G acylase fully contact with D-HPGM and 7-ADCA until the end of the reaction; The upper phosphate buffer solution of cefadroxil is layered with the lower ionic liquid, and the pH of the separated phosphate buffer solution is adjusted to 4.0-5.5, so that cefadroxil crystals are precipitated and dried.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of fadroxil. Background technique [0002] Cefadroxil is an important semi-synthetic β-lactam antibiotic widely used in clinic. It has the advantages of strong activity, good oral absorption, low toxicity and side effects and broad antibacterial spectrum. At present, the domestic production of cefadroxil generally adopts the mixed acid anhydride method (such as CN201310227621.9), the steps are cumbersome, the group protection process in the process needs to be carried out at a low temperature of -30 ℃, and a large amount of toxic reagents are used, resulting in a large amount of waste, serious harm to the ecological environment. The enzymatic method is to use penicillin G acylase (penicillin G acylase, EC 3.5.1.11, referred to as PGA) to catalyze 7-amino-3-deacetoxycephalosporanic acid (7-ADCA) and D-p-hydroxyphenylglycine methyl ester. The ester (D-HPGM) ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12P35/04C12N11/14C12N11/082C12N9/84
CPCY02P20/54
Inventor 薛屏张玮玮史可人李鹏郑庆忠杨金会胡春苗
Owner NINGXIA UNIVERSITY
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