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Process for preparing azlocillin sodium

A technology of azlocillin sodium and azlocillin, applied in the directions of organic chemistry, antibacterial drugs, etc., can solve the problems of high residual ethyl acetate, high qualified products, complicated production, etc., and achieve obvious economic and social benefits, Low production cost and good quality

Inactive Publication Date: 2008-10-22
ZHEJIANG JINHUA CONBA BIO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0028] Said method adopts reaction in water / tetrahydrofuran mixed phase, crystallization in ethyl acetate, the residual amount of ethyl acetate in the prepared azlocillin product is high, can not directly add water and become salt freeze-drying and form qualified product (ethyl acetate High residual amount), but can only be obtained by crystallization according to the above method
And the production is complicated, the yield is low, and the cost is high

Method used

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  • Process for preparing azlocillin sodium
  • Process for preparing azlocillin sodium
  • Process for preparing azlocillin sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of Azlocillin:

[0042] Add a certain amount of 50Kg of purified water and 10Kg of ampicillin into the cleaned reaction pot, stir, cool down, and then slowly add 2N sodium hydroxide solution until all the ampicillin is dissolved. Slowly add 4.0Kg of imidazole chloride, control the pH value of the solution in the tank between 6.0-7.5, filter with suction, add 40Kg of acetone to the filtrate, and acidify it to 2.0-3.0 with hydrochloric acid. Centrifuge, wash twice with purified water first and then with acetone, separate and dry, wait for inspection, and pack. (Yield 92.25%)

[0043] Preparation of Azlocillin Sodium

[0044] Inhale 40Kg of water for injection into the batching tank, add 10Kg of azlocillin, stir for about 10 minutes, start to add 2N sodium hydroxide solution dropwise until the material liquid is completely clear and the pH value is between 6.8 and 8.5, which is the end point, add activated carbon, and continue stirring Decolorize for half an...

Embodiment 2

[0047] Preparation of azlocillin

[0048] Add a certain amount of 50Kg of purified water and 10Kg of ampicillin into the cleaned reaction pot, stir, then slowly add 2N sodium hydroxide solution until all the ampicillin is dissolved. Slowly add 4.0Kg of imidazole chloride, control the pH value of the solution in the tank between 6.0-7.5, filter with suction, add 60Kg of acetone to the filtrate, and acidify it to 2.0-3.0 with hydrochloric acid. Centrifuge, wash twice with purified water first and then with acetone, separate and dry, wait for inspection, and pack. (Yield 92.81%)

[0049] Preparation of Azlocillin Sodium

[0050] Inhale 60Kg of water for injection into the batching tank, add 10Kg of azlocillin, stir for about 10 minutes, start adding 2N sodium hydroxide solution dropwise until the material liquid is completely clear and the pH value is between 6.8 and 8.5, which is the end point, add activated carbon, and continue stirring Decolorize for half an hour, decarboni...

Embodiment 3

[0053] Preparation of azlocillin

[0054]Add a certain amount of 50Kg of purified water and 10Kg of ampicillin into the cleaned reaction pot, stir, cool down, and then slowly add 2N sodium hydroxide solution until all the ampicillin is dissolved. Slowly add 4.0Kg of imidazolyl chloride, control the pH value of the solution in the tank between 6.0-7.5, filter with suction, add 40Kg of ethanol to the filtrate, and acidify it to 2.0-3.0 with hydrochloric acid. Centrifuge, first wash twice with purified water and then with ethanol, separate and dry, wait for inspection, and pack. (Yield 94.76%)

[0055] Preparation of Azlocillin Sodium

[0056] Inhale 50Kg of water for injection into the batching tank, add 10Kg of azlocillin, stir for about 10 minutes, start to add 2N sodium hydroxide solution dropwise until the material liquid is completely clear and the pH value is between 6.8 and 8.5, which is the end point, add activated carbon, and continue stirring Decolorize for half an ...

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Abstract

The invention relates to a process for preparing azlocillin sodium, which comprises carrying out condensation reaction between ampicillin and imidazolidinoxyl chlorine in aqueous phase, the crystallizing in acetone / water, ethanol / water or acetone / ethanol / water system so as to obtain azlocillin, then directly obtaining salts with sodium hydroxide, finally freeze-drying.

Description

Technical field: [0001] The invention relates to the field of drug synthesis, in particular to a preparation method of azlocillin sodium. Background technique: [0002] Azlocillin sodium, its chemical name is (2S, 5R, 6R)-3,3-dimethyl-6-[(R)-2-(2-oxo-1-imidazolidinecarboxamido-2- Phenylacetylamino)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid sodium salt. Has the following formula I structure: [0003] [0004] Azlocillin is a semi-synthetic penicillin, which has good antibacterial effect on Gram-positive and negative bacteria and Pseudomonas aeruginosa. When combined with amikacin, gentamicin and netilmicin, it can produce synergistic effect. [0005] The existing method for preparing Azlocillin Sodium mainly contains following two kinds: [0006] 1. According to EUR.J.MED.CHEM.----CHIM.THER., 1982-17, N°1, PP.59-63, 6-[D-2-(2-oxo-imidazole- 1-Formylamino)-phenylacetamide]-penicillin acid (Azlocillin) is prepared as: [0007] (1) Ampicillin-trihydrate ...

Claims

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Application Information

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IPC IPC(8): C07D499/21A61P31/04
Inventor 余斌赖月琴张晟凯金鑫
Owner ZHEJIANG JINHUA CONBA BIO PHARM CO LTD
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