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Refining method of imipenem

A refining method, imipenem technology, applied in the direction of organic chemistry, can solve the problems of unsatisfactory rapid dissolution and uneven crystal particle size, and achieve the effect of being suitable for large-scale production, loose process conditions, and avoiding the risk of introducing microorganisms

Active Publication Date: 2022-06-28
ZHUHAI UNITED LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The crystal particle size obtained by this method is not uniform, which cannot meet the clinical needs of rapid dissolution

Method used

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  • Refining method of imipenem
  • Refining method of imipenem
  • Refining method of imipenem

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Include the following steps:

[0042] S0: Add 216 mL of tetrahydrofuran to a 1L three-necked bottle, take an ice bath, and cool down to -10°C for later use;

[0043] S1: under a nitrogen atmosphere, heat 180 mL of water for injection to 40 °C, add 4 g of crude imipenem, stir to dissolve, and then cool down to 0 °C;

[0044] S2: After being treated with activated carbon, maintain the temperature at 0 °C, stir for 10 minutes and then filter; the filtration pore size is 0.22um.

[0045] S3: separate 72ml of the filtrate as solution A, and the rest as solution B;

[0046] S4: Pour 72ml of solution A into the tetrahydrofuran for cooling standby in SO, keep -10°C to generate seed crystals for 10min;

[0047] S5: Pour the remaining solution B into the mixed solution of S4, stir evenly and keep at -10°C for 30min;

[0048] S6: Add 500 ml of tetrahydrofuran dropwise to the solution of S5, and keep at -10 °C for 60 min.

[0049] S7: The precipitate is collected by filtration ...

Embodiment 2

[0051]Include the following steps:

[0052] S0: Add 100 mL of acetone to a 1L three-necked bottle, take an ice bath, and cool down to 10°C for later use;

[0053] S1: under a nitrogen atmosphere, heat 100 mL of water for injection to 70 °C, add 4 g of crude imipenem, stir to dissolve, and then cool down to 10 °C;

[0054] S2: After being treated with activated carbon, maintain the temperature at 30°C, and filter after standing for 10 minutes; the filtration pore size is 0.22um.

[0055] S3: separate 10ml of the filtrate as solution A, and the rest as solution B;

[0056] S4: Pour 10ml of solution A into the acetone for cooling standby in SO, and keep 10°C to generate seed crystals for 10min;

[0057] S5: Pour the rest of solution B into the mixed solution of S4, stir evenly and keep at 10°C for 30min;

[0058] S6: Add 500 ml of acetone dropwise to the solution of S5, and keep the crystal at 10°C for 30 min.

[0059] S7: The precipitate is collected by filtration, and dried...

Embodiment 3

[0061] Include the following steps:

[0062] S0: Add 140mL isopropanol to a 1L three-necked bottle, take an ice bath, and cool down to -5℃ for later use;

[0063] S1: under a nitrogen atmosphere, heat 140 mL of water for injection to 50 °C, add 4 g of crude imipenem, stir to dissolve, and then cool down to 20 °C;

[0064] S2: After being treated with activated carbon, maintain the temperature at 20°C, stir for 10min and filter; the filtration pore size is 0.22um.

[0065] S3: separate 28ml of the filtrate as solution A, and the rest as solution B;

[0066] S4: Pour 28ml of solution A into isopropanol for cooling standby in SO, keep -5°C to generate seed crystals for 10min;

[0067] S5: Pour the remaining solution B into the mixed solution of S4, stir well and keep at -5°C for 30min;

[0068] S6: Add 500 ml of isopropanol dropwise to the solution of S5, and keep the temperature at -5°C for 60 min.

[0069] S7: The precipitate is collected by filtration and dried to obtain 3...

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PUM

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Abstract

The invention relates to the technical field of preparation of heterocyclic compounds, in particular to a refining method of imipenem. The method comprises the following steps: dissolving, filtering, sub-packaging crystal growing seeds, growing crystals, and growing the crystals again. Natural seed crystals are formed in the production process in a segmented crystallization mode, and the risk of introducing microorganisms caused by external seed crystals can be avoided. According to the invention, an anti-crystallization mode is adopted for crystallization, and the prepared crystal product is small and uniform in particle size; the process is the same as the original grinding process. Meanwhile, the process conditions are loose, operation is easy, and the method is suitable for large-scale production.

Description

technical field [0001] The invention relates to the technical field of preparation of heterocyclic compounds, in particular to a method for purifying imipenem. Background technique [0002] Imipenem (imipenem) is a carbapenem extended-spectrum beta-lactam antibiotic developed by Merck Company, the chemical name is: (5R,6S)-6-[(1R)-1-hydroxyethyl base]-3-[[2-[(iminomethyl)amino]ethyl]thio]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid monohydrate. Usually used in combination with cilastatin sodium. The structural formula of imipenem monohydrate is as follows figure 1 shown. [0003] In the context of consistency evaluation, in most patents or literatures, to achieve the same crystal form as the original research, the premise is to induce crystallization by adding seed crystals before crystallization. This technology is used in the production process of sterile workshops. There is a risk of introducing microorganisms and is not suitable for industrial production. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D477/02C07D477/20
CPCC07D477/02C07D477/20Y02E60/10
Inventor 李琳崔振华方成乔刘宏宇何晨乔明福韩玉波
Owner ZHUHAI UNITED LAB
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