Preparation method of cefadroxil

A technology for cefadroxil and fadroxil, which is applied in the field of medicine and can solve the problems of the decrease in the catalytic activity of penicillin acylase, the harm to the ecological environment caused by the volatile organic solvent, and the low yield of the target product.
CN109852660AActive Publication Date: 2019-06-07NINGXIA UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
NINGXIA UNIVERSITY
Publication Date
2019-06-07

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Abstract

The invention relates to a preparation method of cefadroxil. The preparation method comprises the following steps of adding preset volume of a cosolvent consisting of ionic liquid and a thiophosphatesalt buffer solution to a reactor with constant-temperature water bath; adding preset molar ratio of D-HPGM and 7-ADCA to the cosolvent, wherein the molar ratio of the D-HPGM to the 7-ADCA is (1 to 1)to (1 to 2.0), and the concentration of the 7-ADCA is 0.1-1.0mol / L; adding magnetic fossilized penicillin G acylase to the cosolvent of the D-HPGM and the 7-ADCA,and continuing performing stirring toenable the magnetic fossilized penicillin G acylase to be in sufficient contact with the D-HPGM and the 7-ADCA until the reaction is finished; performing layered standing on the reaction system liquid after the reaction is finished, so that an upper-layer thiophosphate salt buffer solution and lower-layer ionic liquid in which the cefadroxil dissolves to be subjected to layering; and regulating the pH of the separated thiophosphate salt buffer solution to 4.0-5.5, so that the cefadroxil is separated out and dried.
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Description

Technical field

[0001] The invention relates to the technical field of medicine, in particular to a preparation method of sporadroxil. Background technique

[0002] Cefadroxil (cefadroxil) is an important semi-synthetic β-lactam antibiotic widely used clinically. It has the advantages of strong activity, good oral absorption, low 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°C, 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 uses 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 The ester (D-HPGM) reaction to synthesize cefadroxil, ...

Claims

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