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Method for preparing cefprozil in pH responsive regenerative double aqueous phase system

A cefprozil and system technology, which is applied to the preparation of cefprozil and the synthesis field of cefprozil, can solve the problems of high production cost, low conversion rate, long production cycle, etc., and improve the problem of low product conversion rate and molar yield. Improve and avoid high cost effects

Pending Publication Date: 2017-07-11
EAST CHINA UNIV OF SCI & TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The traditional chemical synthesis of cefprozil has the disadvantages of complex process, long production cycle, environmental pollution, etc., which makes the production cost high
The aqueous phase enzymatic synthesis method is one of the ways to achieve mild reaction, fewer steps, and more environmentally friendly production methods of cephalosporins. The current enzymatic synthesis still has problems such as high reactant price, low conversion rate, low enzyme activity, and poor stability.

Method used

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  • Method for preparing cefprozil in pH responsive regenerative double aqueous phase system
  • Method for preparing cefprozil in pH responsive regenerative double aqueous phase system
  • Method for preparing cefprozil in pH responsive regenerative double aqueous phase system

Examples

Experimental program
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Effect test

Embodiment 1

[0051] P ADBA / P MDB Synthesis of cefprozil by enzyme reaction phase transfer in two aqueous phase system:

[0052] Configure P ADBA 3%(w / v) / P MDB 3% (w / v) two aqueous phase system 20mL, 0.2700g 7-amino-3-propenyl cephalosporanic acid (7-APRA) and 0.7320g D-p-hydroxyphenylglycine methyl ester hydrochloride (D-HPGME -HCl) into the two-phase system, add 0.0136g of potassium dihydrogen phosphate, adjust the pH of the solution to 5.50, control the reaction temperature to 20°C, add 1g of immobilized penicillin acylase (IPGA), and control the reaction speed to 200r / min, After reacting for 4 hours, the molar yield of cefprozil was 89.41% as detected by high performance liquid chromatography, and the distribution coefficient K of cefprozil remained at 1.30. The pH of the solution was adjusted to reclaim the two-phase polymer, and the recovery rate reached 94.33%. Add 5 times the volume DMF crystallization, centrifugation, washing and drying to obtain the crude product cefprozil. ...

Embodiment 2

[0056] P ADBA / P MDB Synthesis of cefprozil by enzyme reaction phase transfer in two aqueous phase system:

[0057] Configure P ADBA 3%(w / v) / P MDB 3% (w / v) two-phase aqueous system 20mL, add 0.2700g 7-APRA and 0.7320gD-HPGME-HCl to the two-phase aqueous system, add 0.0136g potassium dihydrogen phosphate and 0.0447g potassium chloride, adjust the pH of the solution To 5.50, control reaction temperature is 20 ℃, add 1g IPGA, control reaction speed 200r / min, react 4 hours, cefprozil partition coefficient K remains on 2.13, obtain cefprozil molar yield by liquid phase detection and be 93.02%, improved 16.48%. Adjust the pH of the solution to recover the two-phase polymer, and the recovery rate reaches 94.33%. Add 5 times the volume of DMF to crystallize, centrifuge, wash, and dry to obtain the crude product cefprozil.

[0058] The particle radius of cefprozil obtained through testing is identical to that of Example 1.

[0059] Such as figure 2 Shown is the P of Examples 1-...

Embodiment 3

[0061] P ADB / P MDB Synthesis of cefprozil by enzyme reaction phase transfer in two aqueous phase system:

[0062] Configure P ADB 4% (w / v) / P MDB 3% (w / v) two-phase aqueous system 20mL, add 0.2831g 7-APRA and 0.3835gD-HPGME-HCl to the two-phase aqueous system, add 0.0136g potassium dihydrogen phosphate, adjust the pH of the solution to 5.40, control the reaction temperature at 20°C, add 1 g of IPGA, control the reaction speed at 200 r / min, and react for 4 hours. The molar yield of cefprozil is 80.19% through liquid phase detection, and the partition coefficient K of cefprozil remains at 1.30. Adjust the pH of the solution to recover the two-phase polymer, and the recovery rate reaches 96.01%. Add 5 times the volume of DMF to crystallize, centrifuge, wash, and dry to obtain the crude product cefprozil.

[0063] The particle radius of cefprozil obtained through testing is identical to that of Example 1.

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Abstract

The invention relates to a method for preparing cefprozil in a pH responsive regenerative double aqueous phase system. The method comprises (1) preparing two double-aqueous phase systems, (2) orderly adding 7-APRA, D-p-hydroxyphenylglycine methyl ester hydrochloride into the systems, adjusting solution pH to 5.00-6.50 and controlling a solution temperature in a range of 10-30 DEG C, (3) adding immobilized penicillin acylase into the solution obtained by the step (2), and (4) standing the mixed solution, removing the immobilized penicillin acylase, adjusting the pH of the reaction solution, recovering P<ADBA> / <PMDB> and P<ADB> / P<MDB> polymers of the double-aqueous phase systems, feeding the supernatant to a crystallization section, carrying out crystallization, and carrying out centrifugation, washing and drying to obtain a product. The method reduces a chemical synthesis cost, improves a low product conversion rate of the monohydrolase catalytic reaction, effectively improves a yield, simplifies the operation, reduces a cost and realizes easy recovery of the double-aqueous phase systems.

Description

technical field [0001] The invention relates to the technical field of cefprozil, in particular to the technical field of a synthesis method of cefprozil, in particular to a method for preparing cefprozil in a pH-responsive regenerative two-water phase system. Background technique [0002] Cefprozil contains a β-lactam ring and belongs to the β-lactam antibiotics, which can inhibit the synthesis of bacterial cell walls. As a second-generation cephalosporin antibiotic, compared with the first-generation antibiotics, it has low toxicity, strong activity, and broad antibacterial spectrum (greatly expanded the antibacterial range of G-, mainly against Staphylococcus aureus and Streptococcus), etc. advantage. [0003] The traditional chemical synthesis of cefprozil has the disadvantages of complex process, long production cycle, environmental pollution, etc., which makes the production cost high. The aqueous enzymatic synthesis method is one of the production methods to achieve...

Claims

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Application Information

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IPC IPC(8): C12P35/04
CPCC12P35/04
Inventor 曹学君潘红霞杨婷
Owner EAST CHINA UNIV OF SCI & TECH
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