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Process for preparing sulbenicillin sodium by enzymatic method

A technology for preparing sulfobenicillin sodium and enzymatic method is applied in the field of preparing sulfobenicillin sodium by enzymatic method, which can solve the problems of high industrial control requirements, high toxicity to operators, cumbersome synthesis process, etc., and achieves alleviation of environmental pressure and safety. High and simplified process effect

Inactive Publication Date: 2019-04-30
慈溪市一众电器有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Although the technology of synthesizing sulbenicillin sodium by chemical method is relatively mature at present, there are some common shortcomings, namely, the synthesis process is cumbersome, the industrial control requirements are high, and the toxic organic compounds such as pivaloyl chloride, triethylamine and dichloromethane are used. There are many solvents, which are not only highly toxic to the operators, but also cause great environmental pressure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] A kind of technique that enzymatic method prepares sulbenicillin sodium comprises the following steps:

[0029] (1) 100L of 10% penicillin fermented liquid is added in the reactor that 2000KU penicillin acylase is housed, the pH of adjusting solution with 5% ammonia water is about 8.3, and temperature is set to 35 ℃, and stirring speed is 750 rpm, Detecting the content of penicillin during the reaction, when the conversion rate of penicillin is ≥ 95%, pass the resulting mixture through the screen at the bottom of the reactor to intercept penicillin acylase and other macromolecular substances;

[0030] (2) passing the mixed solution obtained in the step (1) successively through an ultrafilter with a molecular weight cut-off of 3000-5000 Daltons and a nanofilter with a molecular weight cut-off of 100-200 Daltons to obtain a concentrated solution;

[0031] (3) The concentrated solution obtained in step (2) is decolorized with activated carbon, and the amount of activated c...

Embodiment 2

[0035] A kind of technique that enzymatic method prepares sulbenicillin sodium comprises the following steps:

[0036] (1) 100L of 10% penicillin fermented liquid is added in the reactor that 2000KU penicillin acylase is housed, and the pH of adjusting solution with 5% ammonia water is about 7.8, and temperature is set to 25 ℃, and stirring speed is 600 rpm, Detecting the content of penicillin during the reaction, when the conversion rate of penicillin is ≥ 95%, pass the resulting mixture through the screen at the bottom of the reactor to intercept penicillin acylase and other macromolecular substances;

[0037] (2) passing the mixed solution obtained in the step (1) successively through an ultrafilter with a molecular weight cut-off of 3000-5000 Daltons and a nanofilter with a molecular weight cut-off of 100-200 Daltons to obtain a concentrated solution;

[0038] (3) The concentrated solution gained in step (2) is decolorized with gac, the gac add-on is 5‰, and the phenylacet...

Embodiment 3

[0042] A kind of technique that enzymatic method prepares sulbenicillin sodium comprises the following steps:

[0043] (1) 10% penicillin fermented liquid is joined in the reactor that 2000KU penicillin acylase is housed, and the pH of adjusting solution with 5% ammonia water is about 8.5, and temperature is set to 28 ℃, and stirring speed is 700 rev / mins, and reaction Detect the content of penicillin during the process, when the conversion rate of penicillin is ≥ 95%, pass the resulting mixture through the screen at the bottom of the reactor to intercept penicillin acylase and other macromolecular substances;

[0044] (2) passing the mixed solution obtained in the step (1) successively through an ultrafilter with a molecular weight cut-off of 3000-5000 Daltons and a nanofilter with a molecular weight cut-off of 100-200 Daltons to obtain a concentrated solution;

[0045] (3) The concentrated solution obtained in step (2) is decolorized with activated carbon, the amount of acti...

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Abstract

The invention discloses a process for preparing sulbenicillin sodium by an enzymatic method, and belongs to the technical field of pharmaceutical and chemical industry. In the method, a penicillin fermentation broth is used as a starting raw material, the steps of crystallization of 6-aminopenicillic acid, washing, drying and the like are omitted, and sulbenicillin sodium is obtained by direct reaction with sulfobenzylacetyl chloride under the action of penicillin acylase. Compared with a chemical synthesis method, the preparation process provided by the invention has the advantages of simpleoperation, low energy consumption, high safety and good stability. Therefore, the process is a low-cost and high-efficiency production process in promotion and application of industrial production.

Description

technical field [0001] The invention relates to a process for preparing sulfbenicillin sodium by enzymatic method, which belongs to the technical field of medicine and chemical industry. Background technique [0002] Sulbenicillin sodium, the Chinese chemical name is (2S, 5R, 6R)-3,3-dimethyl-6-(2-phenyl-2-sulfoacetamido)-7-oxo-4-thia -1-Azabicyclo[3.2.0]heptane-2-carboxylic acid disodium salt; generally white or light yellow powder; very soluble in water, easily soluble in methanol, slightly soluble in ethanol. [0003] Sulbenicillin sodium is a broad-spectrum semi-synthetic antipseudomonal penicillin with a similar antibacterial spectrum to carbenicillin. Its mechanism of action is to produce antibacterial effect by interfering with the synthesis of bacterial cell wall. It is mainly suitable for Gram-positive bacteria such as Pseudomonas aeruginosa, certain Proteus, Staphylococcus, and Streptococcus that are sensitive to this product, and has good antibacterial activity....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P37/04C12P37/02
CPCC12P37/04C12P37/02
Inventor 房庆红
Owner 慈溪市一众电器有限公司
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