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Method for synthetizing amoxicillin through enzymatic method

A technology for amoxicillin and enzymatic synthesis, which is applied in the field of enzymatic synthesis of amoxicillin, can solve the problems of amoxicillin stability, which are few, and does not involve the stability of amoxicillin, and achieves good clarity. , shorten the reaction time, good effect of purity

Active Publication Date: 2019-02-22
GUANGZHOU LIXIN PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But this application does not relate to the stability of the prepared amoxicillin
[0008] The current research on amoxicillin is mainly based on the yield, purity and production cost of amoxicillin, and there are very few studies on the stability of the obtained amoxicillin

Method used

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  • Method for synthetizing amoxicillin through enzymatic method
  • Method for synthetizing amoxicillin through enzymatic method
  • Method for synthetizing amoxicillin through enzymatic method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1 A kind of method of enzymatic synthesis of amoxicillin

[0044] Specifically include the following steps:

[0045] (1) First take immobilized penicillin G acylase, control its dosage to be 2KU / L, and after cleaning it with distilled water, add a concentration of 3mol / L hydrochloric acid solution, soak for 5min, then drop into the enzyme reactor, Drain water;

[0046] (2) Weigh p-hydroxyphenylglycine methyl ester and 6-APA, control the molar ratio of the two to 1:1, mix the two evenly, add a hydrochloric acid solution with a concentration of 3mol / L, soak for 20min, then add pure water and mass Ratio is 3:1 sucrose and histidine, drop into the enzyme reactor that adds penicillin G acylase described in step (1);

[0047] (3) Turn on stirring and control the stirring speed to 300r / min, use 3mol / L ammonia water to control the pH value to 6.5, and use a circulating refrigerator to control the temperature to 10°C, until the conversion rate of 6-APA no longer inc...

Embodiment 2

[0049] Embodiment 2 A kind of method of enzymatically synthesizing amoxicillin

[0050] Specifically include the following steps:

[0051] (1) First take the immobilized penicillin G acylase, control its dosage to 2.1KU / L, and wash it with distilled water, then add a hydrochloric acid solution with a concentration of 3.5mol / L, soak for 6min, and then put it into the enzyme reactor medium, drained;

[0052] (2) Weigh p-hydroxyphenylglycine methyl ester and 6-APA, control the molar ratio of the two to 1.1:1, mix the two evenly, add a hydrochloric acid solution with a concentration of 3.5mol / L, soak for 25min, then add pure water and Mass ratio is 3: 1 sucrose and histidine, drop into the enzyme reactor that adds penicillin G acylase described in step (1);

[0053] (3) Turn on stirring and control the stirring speed to be 350r / min, use 3.5mol / L ammonia water to control the pH value to 6.6, and use a circulating freezer to control the temperature to 12°C until the conversion rat...

Embodiment 3

[0055] Embodiment 3 A kind of method of enzymatic synthesis amoxicillin

[0056] Specifically include the following steps:

[0057] (1) First take the immobilized penicillin G acylase, control its dosage to 2.4KU / L, and wash it with distilled water, then add a hydrochloric acid solution with a concentration of 4mol / L, soak for 8min, and then put it into the enzyme reactor , drain the water;

[0058] (2) Weigh p-hydroxyphenylglycine methyl ester and 6-APA, control the molar ratio of the two to 1.2:1, mix the two evenly, add a hydrochloric acid solution with a concentration of 4mol / L, soak for 20min, then add pure water and quality Ratio is 3:1 sucrose and histidine, drop into the enzyme reactor that adds penicillin G acylase described in step (1);

[0059] (3) Turn on the stirring and control the stirring speed to 400r / min, control the pH value to 6.8 with 4mol / L ammonia water, and control the temperature to 15°C with a circulating freezer until the conversion rate of 6-APA n...

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Abstract

The invention discloses a method for synthetizing amoxicillin through an enzymatic method. The method comprises the following steps: (1) immobilized penicillin G acylase is washed through distilled water and then soaked through hydrochloric acid; (2) Methyl p-hydroxyphenylglycinate and 6-APA are evenly mixed and then soaked through hydrochloric acid, and then purified water is added; (3) the immobilized penicillin G acylase, the Methyl p-hydroxyphenylglycinate and the 6-APA are mixed and then react to obtain an amoxicillin suspension; and (4) the amoxicillin suspension is cooled, hydrochloricacid is dripped till the solution is clear, gain growing is conducted after suction filtration, washing and drying are conducted, and then the amoxicillin product is obtained. In the reaction process,the immobilized penicillin G acylase is soaked by the hydrochloric acid for a short time, thus the reaction speed is increased, the reaction time is shortened, the yield of the product is increased,and the purity of the product is improved; and sucrose and histidine with the mass ratio being 3 to 1 are added in a reaction system, and thus the stability of the product is improved.

Description

technical field [0001] The invention relates to a method for synthesizing medicine, in particular to a method for enzymatically synthesizing amoxicillin. Background technique [0002] Amoxicillin, also known as amoxicillin, its chemical name is (2S,5R,6R)-3,3-dimethyl-6-[(R)-(-)-2-amino-2-( 4-(p-hydroxyphenyl)acetamido]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid trihydrate, molecular formula C 16 h 19 N 3 o 5 S. 3H 2 O, the molecular weight is 419.46, the structural formula is as follows: [0003] [0004] Amoxicillin is a white or off-white crystalline powder with a slightly specific smell and bitter taste, hardly soluble in water and methanol, extremely difficult to ethanol, almost insoluble in acetone, chloroform and benzene. [0005] Amoxicillin, as the main species of the second-generation penicillin, is a broad-spectrum semi-synthetic penicillin, which can inhibit the synthesis of bacterial cell walls, make it rapidly become spherical and break...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P37/04
CPCC12P37/04
Inventor 高悦译刘恩桂陈新颖
Owner GUANGZHOU LIXIN PHARM CO LTD
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