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Method for synthesizing penicillin sodium salt and potassium salt

A synthetic method and technology of penicillin sodium, applied in organic chemistry, antibacterial drugs, etc., can solve the problems of allergic reactions and high levels of related substances in the body, and achieve the effect of safe oral absorption, strong curative effect, and simple process

Inactive Publication Date: 2010-01-27
沈阳华威药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the high temperature in the spray-drying process leads to high levels of related substances, and the open-loop degradation products are likely to cause allergic reactions in the body. Therefore, the freeze-drying method and spray-drying method have been replaced by the solvent method.

Method used

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  • Method for synthesizing penicillin sodium salt and potassium salt
  • Method for synthesizing penicillin sodium salt and potassium salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] A kind of synthetic method of penicillin sodium salt, is to take the dried amoxicillin trihydrate 3.0g, join in the three-necked bottle, then add anhydrous methanol 20ml and anhydrous triethylamine 1.0ml in the three-necked bottle , after fully stirring to make it dissolve, place the three-necked flask in an ice bath, and when the temperature drops to 0°C, slowly add 3ml of methanol solution of sodium methoxide dropwise (concentration is 0.1mol / L) with a dropper to adjust The pH value is 9-10, the dropping time is 5 minutes, and the methanol solution of sodium methoxide is added dropwise and reacted for 20 minutes under stirring. Then the prepared above-mentioned reaction solution is added to a rotary evaporator, the temperature of the water-soluble pot is 40° C., and the pressure is 0.09 MPa. After the rotary evaporator drains the solvent, amoxicillin sodium crystallizes out, and the obtained wet amoxicillin The sodium is sent to a vacuum drying oven at 40° C. under a ...

Embodiment 2

[0062] A kind of synthetic method of penicillin sodium salt, is to get the dried amoxicillin trihydrate 8.0g, join in the three-necked bottle, then add anhydrous methanol 80ml and anhydrous triethylamine 5.0ml in the three-necked bottle , after fully stirring to make it dissolve, place the three-necked flask in an ice bath, and when the temperature drops to 15°C, slowly drop 5ml of methanol solution of sodium methoxide (concentration is 0.1mol / L) with a dropper to adjust The pH value is 10, the dropwise addition time is 60 minutes, and the methanol solution of sodium methoxide is added dropwise and reacted for 30 minutes under stirring. Then add the prepared above-mentioned reaction solution into a rotary evaporator, the temperature of the water-soluble pot is 60° C., and the pressure is 0.01 MPa. After the rotary evaporator drains the solvent, amoxicillin sodium crystallizes out, and the obtained wet amoxicillin The sodium is sent to a vacuum drying oven at 45° C. under a pre...

Embodiment 3

[0064] A kind of synthetic method of penicillin potassium salt, is to get the dried amoxicillin trihydrate 5.0g, join in the three-necked bottle, then add anhydrous methanol 60ml and anhydrous triethylamine 2.5ml in the three-necked bottle , after fully stirring to make it dissolve, place the three-necked flask in an ice bath, and when the temperature drops to 10°C, slowly drop 4ml of methanol solution of potassium methylate (concentration is 0.1mol / L) with a dropper to adjust The pH value is 9, the dropwise addition time is 28 minutes, and the methanol solution of potassium methoxide is added dropwise and reacted for 25 minutes under stirring. Then add the prepared above-mentioned reaction solution into a rotary evaporator, the temperature of the water-soluble pot is 50° C., and the pressure is 0.1 MPa. After the rotary evaporator drains the solvent, amoxicillin sodium crystallizes out, and the obtained wet amoxicillin The sodium is sent to a vacuum drying oven at 43°C under ...

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Abstract

A method for synthesizing penicillin sodium salt and potassium salt is disclosed, comprising the steps of: adding dried amoxicillin trihydrate 3-8 into a three-necked flask having the volume of 250 ml; then adding 30-60 ml of absolute methanol and 0.5-5 ml of anhydrous triethylamine into the three-necked flask for being dissolved by sufficient stirring; placing the three-necked flask filled with dissolving solution in ice bath and instilling slowly 3-5 ml of methanol solution of sodium methoxide or potassium methoxide with the concentration of 0.1 mol / L for 5-60 minutes by using a dropping pipette when the temperature drops to the range from 0 DEG C to 15 DEG C; reacting for 20 to 30 minutes under stirring after the pH value reaches 9 to 10, afterwards, placing reaction solution in a rotary evaporator with the temperature of a water-soluble pot being 40-60 DEG C and the pressure being 0.09-0.1 MPa, and obtaining wet penicillin sodium salt or potassium salt subsequent to emptying solvent in the rotary evaporator, in the end, conveying the obtained wet penicillin sodium salt or potassium salt to a vacuum drying oven for being dried for 5-6 hours at the temperature from 40 to 45 DEG C under the pressure from 0.09 to 0.1 MPa, thus resulting in the finished product. The invention has the advantages of simple process, rapidness, high conversion rate of salification and low cost.

Description

technical field [0001] The invention relates to a preparation method of medicine, in particular to a preparation method of penicillin sodium (potassium) salts. Background technique [0002] Penicillin is divided into first-generation penicillin and second-generation penicillin. The first-generation penicillin refers to natural penicillin, which is a total of 7 kinds of penicillins obtained from penicillium culture broth and cephalosporin fermentation broth, penicillin F (2-Pentenylpenicillin), dihydromycin F (Pentylpenicillin), penicillin G (Benzylpenicillin) ), penicillin K (Heptylpenicillifi), penicillin N (D-4-Amino-4carboxybutylpenicillin), penicillin V (Phenoxymethylpenicillin), penicillin X (p-Hydroxybenzylpenicillin). Among them, penicillin G has the strongest effect and the highest yield. It has clinical application value. Although penicillin G has been fully synthesized, its cost cannot be compared with that of biological fermentation. [0003] As a bactericidal ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/16C07D499/68A61P31/04
Inventor 王翔林曾昭钧
Owner 沈阳华威药业有限公司
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