Method for enzymatic synthesis of cefprozil in recyclable aqueous two-phase system by using immobilized penicillin acylase

A technology of penicillin acylase catalysis and penicillin acylase, which is applied in the direction of fermentation, can solve the problems of restricting large-scale production, inability to recycle, difficult to recycle, etc., and achieve increased yield, reduced by-products, and synthesis/hydrolysis ratio Improved effect
CN103451259AInactive Publication Date: 2013-12-18南通康鑫药业有限公司 +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
南通康鑫药业有限公司
Publication Date
2013-12-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for the enzymatic synthesis of cefprozil in a recyclable aqueous two-phase system by using immobilized penicillin acylase. The method comprises the following steps: dissolving a cefprozil parent nucleus and an acylation reagent in an aqueous two-phase polymer solution, wherein the molar ratio of the parent nucleus to the acylation reagent is 1: (1-4); and adding immobilized penicillin G acylase, then adding a two-phase distribution conditioning agent, adjusting the pH value to 4.5-7, and reacting for 1 to 80 hours at the temperature of 5-30 DEG C, wherein the concentration of enzyme in a reaction system is 50-150U / ml. By adopting the method, the hydrolytic activity of the penicillin acylase can be effectively inhibited, thus the hydrolysis degrees of the acylation reagent and the cefprozil product can be reduced. Compared with a method using water as a medium, the method disclosed by the invention has the advantages that the product and the enzyme are distributed in two different water phases, a reactant is fully in contact with the enzyme, so that a synthesis / hydrolysis specific value is greatly increased, the yield of the cefprozil can be increased by 20%, and the highest yield can reach 78%; the adopted novel recyclable aqueous two-phase system can be recycled, so that the production cost is reduced.
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Description

technical field

[0001] The invention relates to a preparation method of cefprozil, in particular to a method for catalyzing the synthesis of cefprozil by using immobilized penicillin acylase in a reusable two-water phase system. Background technique

[0002] Cefprozil (Cefprozil), is a broad-spectrum cephalosporin antibacterial drug. It has strong antibacterial activity against G+, G-bacteria and anaerobic bacteria, especially against G+ bacteria, and is stable against β-lactamase. It is mainly used for the treatment of otitis media, respiratory tract infections, skin and skin soft tissue infections, etc. Cefprozil has high bioavailability, complete gastrointestinal absorption, broad antibacterial spectrum and good stability. It is a semi-synthetic cephalosporin drug with good development prospects.

[0003] The chemical synthesis of cefprozil mainly contains two kinds of methods, and one is to use the cephalosporin mother nucleus as starting material, introduce propenyl at...

Claims

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