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A kind of meropenem compound and its preparation method

A technology of meropenem and compounds, which is applied in the field of meropenem compounds and their preparation methods, can solve the problems of low solubility and unfavorable industrial production, and achieve the effects of simple process, convenient operation and guaranteed product quality

Inactive Publication Date: 2011-12-07
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solubility of meropenem in water is very low. For example, a large amount of water is required to dissolve it at room temperature. In this way, a large amount of organic solvent is required when adding an organic solvent for crystallization in the next step, which is not conducive to industrial production.

Method used

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  • A kind of meropenem compound and its preparation method
  • A kind of meropenem compound and its preparation method
  • A kind of meropenem compound and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] (1) Disperse 200 g of crude meropenem with a purity of 95.68% in 1000 ml of water, and add sodium bicarbonate solution dropwise with sufficient stirring until the pH of the solution is 8.0 to obtain a meropenem salt solution; then add 4 g of activated carbon and keep warm at 45°C. Stir for 30min, filter, and collect the filtrate;

[0046] (2) Add hydrochloric acid to the above filtrate, stir at room temperature until the pH value of the solution is 5.0, cool to about 4°C, precipitate, and collect the precipitate by filtration;

[0047] (3) Dissolve the product in step (2) with a small amount of methanol, then add 100g of neutral alumina and stir evenly, add to the upper end of the prepared chromatographic column after waving off the solvent, and utilize the preparative chromatographic column to carry out separation and purification. The mobile phase is a mixed solvent of water and methanol with a volume ratio of 1:4, and the stationary phase is Baker column chromatograp...

Embodiment 2

[0051] (1) Disperse 200 g of crude meropenem with a purity of 95.68% in 1000 ml of water, and add it dropwise into potassium bicarbonate solution under full stirring until the pH value of the solution is 8.5 to obtain a meropenem salt solution; then add 2.5 g of activated carbon, 35 Keep warm at ℃, stir for 15 minutes, filter, and collect the filtrate;

[0052] (2) Add hydrochloric acid to the above-mentioned filtrate, stir at room temperature until the pH value of the solution is 5.5, cool to about 4°C, precipitate, and collect the precipitate by filtration;

[0053] (3) Dissolve the product in step (2) with a small amount of methanol, then add 100g of neutral alumina and stir evenly, add to the upper end of the prepared chromatographic column after waving off the solvent, and utilize the preparative chromatographic column to carry out separation and purification. The mobile phase is a mixed solvent of water and methanol with a volume ratio of 1:4, and the stationary phase is...

Embodiment 3

[0057] (1) Disperse 200g of crude meropenem with a purity of 95.68% in 1000ml of water, add dropwise into sodium bicarbonate solution under full stirring until the pH of the solution is 7.8, and obtain meropenem salt solution; then add 5g of activated carbon and keep warm at 40°C , stirred for 20min, filtered, and collected the filtrate;

[0058] (2) Add hydrochloric acid to the above filtrate, stir at room temperature until the pH value of the solution is 5.0, cool to about 4°C, precipitate, and collect the precipitate by filtration;

[0059] (3) Dissolve the product in step (2) with a small amount of methanol, then add 100g of neutral alumina and stir evenly, add to the upper end of the prepared chromatographic column after waving off the solvent, and utilize the preparative chromatographic column to carry out separation and purification. The mobile phase is a mixed solvent of water and methanol with a volume ratio of 1:4, the stationary phase is 18-32 μm ICN allumina N neut...

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Abstract

The invention relates to a meropenem compound and a preparation method thereof. In the method, crude meropenem prepared with the prior art is prepared into a relatively pure meropenem compound by adopting the following steps of: adding aqueous alkali into a crude meropenem raw material and fully reacting to clear to obtain a meropenem saline solution; adding active carbon for adsorbing, filteringand collecting filtrate, adding acid into a filtrating solution, and filtering and collecting precipitates; and separating and purifying by using a preparation type neutral aluminum oxide chromatographic column, collecting eluent, concentrating under reduced pressure, and drying in vacuum at the temperature 25-30 DEG C to obtain refined meropenem. The method has the advantages of simple process, convenience for operation and low cost, and is suitable for scale production. According to the invention, the purity is increased, the security of the meropenem compound in an anti-sensitive bacterialinfection medicament is ensured, the product quality of a preparation is improved, and toxic or side effect is reduced.

Description

technical field [0001] The invention relates to a meropenem compound and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Meropenem (Biapenem), belonging to penem antibiotics, is a white to slightly yellow crystalline powder, and its chemical name is: (-)6-[[(4R,5S,6S)-2-carboxy-6[(1R) -1-Hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-en-3-yl]thio]-6,7-dihydro-5H- Pyrazol[1,2-a][1,2,4]triazol-4-ium inner salt, the molecular formula is: C 17 h 25 N 3 o 5 S, molecular weight: 383.47, structural formula: [0003] [0004] Meropenem produces antibacterial effects by inhibiting the synthesis of bacterial cell walls. Meropenem easily penetrates the cell walls of most Gram-positive and negative bacteria and reaches its target penicillin-binding protein. [0005] Meropenem is sensitive to both Gram-positive and Gram-negative bacteria, and has strong antibacterial activity especially against Gram-negative bacte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D477/20C07D477/02A61P31/04
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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