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Refining method of biapenem crude product

A refined method, the technology of biapenem, which is applied in the field of medicine, can solve the problems of difficult expansion and shortage, and achieve the effects of reduced usage, simple method, high yield and purity

Inactive Publication Date: 2015-11-25
NANJING SIMCERE DONGYUAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The current method of using anti-solvents such as ethanol and acetone to precipitate biapenem solids by dissolving in purified water uses a large amount of solvent. Usually, 1g of biapenem requires more than 25g of purified water to dissolve, and about 40-50g of anti-solvent is needed at the same time. Only the solvent can precipitate and crystallize the biapenem solid, so it is difficult to expand its scale. For example, a 1000L reaction crystallization kettle can only refine less than 10kg of biapenem product
[0005] At present, there is a lack of a method for refining crude biapenem with stable properties and high yield

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Dissolve 100g of crude biapenem in 500mL of 80% formic acid purified aqueous solution at room temperature, add 3.0g of activated carbon and stir for 15min to decolorize, filter, and filter the filtrate through a 0.22μm filter membrane, transfer the filtrate to a 2000mL reaction flask, add 1000mL of 95% ethanol dropwise . After the dropwise addition, the reaction was stirred for 2h and filtered. After drying, 84.6g of biapenem fine product was obtained. Yield 84.6%.

Embodiment 2

[0041] Dissolve 100g of crude biapenem in 500mL of 60% formic acid purified aqueous solution at room temperature, add 3.0g of activated carbon and stir for 15min to decolorize, filter, and filter the filtrate through a 0.22μm filter membrane, transfer the filtrate to a 2000mL reaction flask, add dropwise 1000mL of 95% ethanol . After the dropwise addition, the reaction was stirred for 2h and filtered. After drying, 86.2g of biapenem fine product was obtained. Yield 86.2%.

Embodiment 3

[0043] Dissolve 100g of crude biapenem in 500mL of 50% formic acid purified aqueous solution at room temperature, add 3.0g of activated carbon and stir for 15min to decolorize, filter, and filter the filtrate through a 0.22μm filter membrane, transfer the filtrate to a 2000mL reaction flask, add 1000mL of 95% ethanol dropwise . After the dropwise addition, the reaction was stirred for 2h and filtered. After drying, 87.2g of biapenem fine product was obtained. Yield 87.2%.

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Abstract

The invention discloses a refining method of a biapenem crude product. The method comprises the following steps: (1) under room temperature, dissolving the biapenem crude product into a methanoic acid water solution, wherein the percentage mass content of methanoic acid in the methanoic acid water solution is 30 to 80 percent; (2) adding activated carbon into the solution, stirring and destaining for 15 to 30 minutes; (3) filtering filter liquor through a filter membrane of 0.22 micrometers, then transferring the filter liquor into a reaction flask, dropwise adding 800 to 1000 mL of anti-solvent, and stirring for reacting for two hours for crystallization after finishing adding; (4) filtering solid matters in the solution, and drying to obtain a biapenem refined product. According to the method provided by the invention, the compound property is stable, the method is simple, biapenem is easy to produce and can be prepared effectively, the yield of the biapenem is improved, and the use amount of solvents are reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a method for refining crude biapenem. Background technique [0002] Biapenem is a synthetic carbapenem antibiotic; internal salt white or off-white powder. Soluble in water, insoluble in common organic solvents. It is more stable to renal dehydropeptidase than meropenem and does not require combined enzyme inhibitors. The activity against Gram-negative bacteria, especially against Pseudomonas aeruginosa is stronger than that of imipenem; the antibacterial activity against aerobic Gram-positive bacteria is slightly lower than that of imipenem; the activity against anaerobic bacteria is the same as that of imipenem . [0003] The solubility of biapenem determines its refining effect. The experiment found that its solubility in purified water at room temperature is poor. 1g of biapenem needs 35mL to 40mL of purified water to dissolve. If the dissolution temperature i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/06
CPCC07D519/06
Inventor 梁西周葛宗明王吉喜黄頲
Owner NANJING SIMCERE DONGYUAN PHARM CO LTD
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