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Ceftizoxime sosium compound of new way

A kind of technology of ceftizoxime sodium and compound, applied in the field of drug synthesis, can solve the problems such as no literature and patent reports etc.

Inactive Publication Date: 2010-03-17
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, domestic manufacturers of ceftizoxime sodium preparations mainly rely on imported raw materials for sub-packaging, but there are no literature and patent reports on the production process of ceftizoxime sodium

Method used

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  • Ceftizoxime sosium compound of new way
  • Ceftizoxime sosium compound of new way
  • Ceftizoxime sosium compound of new way

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Example 1 Synthesis of 2-(2-formylaminothiazol-4-yl)-2-methoxyiminoacetic acid

[0027] Add 201 grams of aminothioxamic acid to 2 liters of formic acid, add 30 grams of 4A molecular sieves as a catalyst, heat up to 50 ° C for 4 hours, distill most of the formic acid under reduced pressure, add 1 liter of water, stir, and extract with 800 ml of ethyl acetate. Dry over sodium sulfate and concentrate under reduced pressure to obtain 217 g of the product 2-(2-formylaminothiazol-4-yl)-2-methoxyiminoacetic acid with a yield of 94.6%.

Embodiment 2

[0028] The synthesis of embodiment 2 ceftizoxime sodium

[0029] Dissolve 485 grams of triphenylphosphine in 1 liter of 1,2-ethylene dichloride, add dropwise to 1 liter of 2-ethylene dichloride containing 524 grams of triphosgene, and keep the reaction temperature at 5°C, after the dropwise addition, react at this temperature for 2 hours, then add the mixed solution dropwise to 200 grams of 2-(2-formylaminothiazol-4-yl)-2-methoxyimine acetic acid 800ml of 1,2-ethylene dichloride, reacted at 5°C for 1.5 hours, then this mixed solution was added dropwise to 2 In 1 liter of aqueous solution, the temperature was controlled at 0°C, and the pH of the reaction solution was controlled by sodium hydroxide solution to be 11. After the dropwise addition, the reaction was carried out for 1 hour, and then the pH was adjusted to 3 with hydrochloric acid, separated into layers, dried with anhydrous sodium sulfate, and reduced Concentrate under pressure, dissolve the concentrated product in ...

Embodiment 3

[0037] Example 3 Synthesis of 2-(2-formylaminothiazol-4-yl)-2-methoxyiminoacetic acid

[0038] Add 402 grams of aminothioxamic acid to 4 liters of formic acid, add 60 grams of 4A molecular sieves as a catalyst at the same time, heat up to 50 ° C for 4 hours, distill most of the formic acid under reduced pressure, add 2 liters of water, stir, and extract with 1500 ml of ethyl acetate. Dry over sodium sulfate and concentrate under reduced pressure to obtain 430.3 g of the product 2-(2-formylaminothiazol-4-yl)-2-methoxyiminoacetic acid with a yield of 93.8%.

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Abstract

The invention relates to a ceftizoxime sosium compound of a new way. Ceftizoxime sosium is prepared by firstly reacting a cefotaxime acid with a methanoic acid to generate 2-(2-formyl aminothiazole-4-radical)-2-methoxyl imine acetic acid, then adding 7-amino-3-nor-3-cephem-4-carboxylic acid, taking triphenylphosphine oxide and triphosgene as catalysts, stirring and reacting, and regulating an acid-base pH value.

Description

technical field [0001] The invention relates to a cephalosporin compound, in particular to a method for synthesizing a new route of ceftizoxime sodium compound, and belongs to the technical field of drug synthesis. Background technique [0002] Ceftizoxime sodium, its chemical name is: (6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-8-oxo Dai-5-thia-1-aminobicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt, molecular formula: C 13 h 12 N 5 NaO 5 S 2 , molecular weight: 405.38, structural formula: [0003] [0004] Ceftizoxime sodium was developed by Fujisawa Pharmaceutical Co., Ltd. of Japan, and was first listed in Japan in 1982. The trade name is ceftizox, which belongs to the third generation cephalosporin. The broad-spectrum β-lactamase (including penicillinase and cephalosporinase) produced by Gram-negative bacteria is stable, and has strong antibacterial effect on Enterobacteriaceae such as Escherichia coli, Klebsiella pneumoniae, Proteus mi...

Claims

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Application Information

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IPC IPC(8): C07D501/20C07D501/06B01J31/02B01J27/20A61P31/04
Inventor 邱民
Owner HAINAN LINGKANG PHARMA CO LTD
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