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
View PDF1 Cites 8 Cited by
  • 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 materi...

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Ceftizoxime sosium compound of new way
  • Ceftizoxime sosium compound of new way
  • Ceftizoxime sosium compound of new way

Examples

Experimental program
Comparison scheme
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%.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Melting pointaaaaaaaaaa
Melting pointaaaaaaaaaa
Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07D501/20C07D501/06B01J31/02B01J27/20A61P31/04
Inventor 邱民
Owner HAINAN LINGKANG PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap