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Synthesis process of ceftezole sodium

A technology of ceftizole sodium and synthesis process, applied in the field of medicine, can solve the problems of complicated steps, low yield and high processing cost, and achieve the effects of simple steps, high yield and low processing cost

Inactive Publication Date: 2011-04-13
JIANGSU HI STONE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The current prior art for the processing technology of ceftezole sodium, its steps are loaded down with trivial details, yield is lower and processing cost is higher, is not suitable for mass production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1. Synthesis of Ceftezole

[0033] Add 5.12 kg of 1H-tetrazolium acetic acid and 48 L of tetrahydrofuran into reaction kettle A, stir to dissolve, slowly add 7.16 kg of thionyl chloride dropwise under stirring at 45°C-50°C, the solution gradually changes from turbid to clear, and use ammonia water Absorbs acid gases. During the dropping process, the temperature was maintained at 45°C-50°C, and the dropwise addition was completed in about 50 minutes. Stir at this temperature for 1.5 hours. The mixed liquid of thionyl chloride and tetrahydrofuran was evaporated at room temperature to obtain a viscous liquid, which was cooled, dried and sealed for future use.

[0034] Add 9.36kg of 7-amino-3-[2-(1,3,4)-thiadiazolyl]thiomethyl-3-cephem-4-carboxylic acid, 40L of ethyl acetate in B reactor, and stir Cool to 0°C, under the protection of nitrogen, add 4.34 kg of trimethylchlorosilane dropwise with stirring, the solution turns into a yellow solution, and continue to stir at a...

Embodiment 2

[0042] 1. Synthesis of Ceftezole

[0043] Add 5.12 kg of 1H-tetrazolium acetic acid and 48 L of tetrahydrofuran into reaction kettle A, stir to dissolve, slowly add 7.16 kg of thionyl chloride dropwise under stirring at 45°C-50°C, the solution gradually changes from turbid to clear, and use ammonia water Absorbs acid gases. During the dropping process, the temperature was maintained at 45°C-50°C, and the dropwise addition was completed in about 50 minutes. Stir at this temperature for 1.5 hours. The mixed liquid of thionyl chloride and tetrahydrofuran was evaporated at room temperature to obtain a viscous liquid, which was cooled, dried and sealed for future use.

[0044] Add 9.36kg of 7-amino-3-[2-(1,3,4)-thiadiazolyl]thiomethyl-3-cephem-4-carboxylic acid, 40L of ethyl acetate in B reactor, and stir Cool to 0°C, under the protection of nitrogen, add 4.34 kg of trimethylchlorosilane dropwise with stirring, the solution turns into a yellow solution, and continue to stir at a...

Embodiment 3

[0052] 1. Synthesis of Ceftezole

[0053] Add 5.12 kg of 1H-tetrazolium acetic acid and 48 L of tetrahydrofuran into reaction kettle A, stir to dissolve, slowly add 7.16 kg of thionyl chloride dropwise under stirring at 45°C-50°C, the solution gradually changes from turbid to clear, and use ammonia water Absorbs acid gases. During the dropping process, the temperature was maintained at 45°C-50°C, and the dropwise addition was completed in about 50 minutes. Stir at this temperature for 1.5 hours. The mixed liquid of thionyl chloride and tetrahydrofuran was evaporated at room temperature to obtain a viscous liquid, which was cooled, dried and sealed for future use.

[0054] Add 9.36kg of 7-amino-3-[2-(1,3,4)-thiadiazolyl]thiomethyl-3-cephem-4-carboxylic acid, 40L of ethyl acetate in B reactor, and stir Cool to 0°C, under the protection of nitrogen, add 4.34 kg of trimethylchlorosilane dropwise with stirring, the solution turns into a yellow solution, and continue to stir at a...

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PUM

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Abstract

The invention relates to a synthesis process of ceftezole sodium, comprising the following process steps of: firstly, synthetizing ceftezole; then, synthetizing the crude product of ceftezole sodium; and finally, refining the crude product of the ceftezole sodium. The synthesis process of the ceftezole sodium has the advantages of simple steps, higher yield and lower processing cost and is suitable for mass production.

Description

technical field [0001] The invention relates to a synthesis process of ceftezole sodium, which belongs to the technical field of medicine. Background technique [0002] Ceftezole sodium, the English name is Ceftezole Sodium for Injection, its chemical name is (6R,7R)-3-[(1,3,4-thiadiazol-2-yl)thiomethyl]-8-oxo Sodium 7-[2-(1H-tetrazol-1-yl)acetamido]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2carboxylate. Properties: This product is white to light yellow crystalline powder, odorless and hygroscopic. Ceftezole sodium is a semi-synthetic cephalosporin derivative, and its mechanism of action is to exert antibacterial activity by inhibiting the synthesis of bacterial cell walls. Ceftezole sodium can be widely distributed in the body, among which the kidney is the highest, followed by serum, liver, lung, heart and spleen. There is also a small amount of distribution in the cerebrospinal fluid, but the distribution increases significantly when the meninges are inflamed. In the distr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/04
Inventor 王多平
Owner JIANGSU HI STONE PHARMA
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