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Amino butanetriol salt of cephalosporin compounds and preparing method

A technology of tromethamine and pine tromethamine is applied in the field of derivatives of cephalosporins and their preparation, and can solve the problems of vascular irritation, high risk, incompatibility and the like

Inactive Publication Date: 2007-08-08
GUANGDONG ZHONGKE DRUG R&D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many problems in the use process, such as: 1) there is vascular irritation, and long-term use can easily cause symptoms such as vasculitis; 2) most of them exist in the form of sodium salts, and sodium ions enter the human body in such a large amount Patients with diabetic bacterial infection, neurosurgery patients with severe neurosurgery, patients with heart and kidney insufficiency, or patients with high blood pressure are at high risk, which can easily cause hypernatremia and cause adverse reactions; 3) Some varieties have incompatibility and are inconvenient to use; 4) Muscle There is muscle irritation when injecting; etc.

Method used

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  • Amino butanetriol salt of cephalosporin compounds and preparing method
  • Amino butanetriol salt of cephalosporin compounds and preparing method
  • Amino butanetriol salt of cephalosporin compounds and preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1: the preparation of cefuroxime tromethamine

[0067] In a 250ml three-necked flask, add 12.1g (0.1mol) of tromethamine and 20ml of 60% ethanol, and drop into 20ml of 80% ethanol solution containing 42.4g (0.1mol) of cefuroxime acid under high temperature stirring, and stir until the mixture is Clarify, then stir at room temperature for 2 hours, drop the mixed reactants into 300ml (5-10°C) acetone solution to obtain white powder crystals, filter the solid powder with suction, wash the solid with a small amount of acetone, and pentoxide at high temperature Vacuum drying under the condition of diphosphorus for 24 hours yielded 48 g of powdery solid with a yield of 88%, mp: 121-123° C., content analysis: (HPLC method) containing cefuroxime acid 77.6-77.8%. The product was analyzed by elements (theoretical value: C44.0%H5.0%N12.8%032.3%S5.9%; measured value: C44.9%H5.2%N12.6%032.0%S5.3%), According to NMR, MS, UV, IR and HPLC analysis, the product is cefuroxime...

Embodiment 2

[0068] Embodiment 2: the preparation of ceftriaxone trometamol

[0069] In a 250ml three-neck flask, add 12.1g (0.1mol) of tromethamine, 4ml of methanol, and 2ml of water, stir at high temperature, add 57.7g (0.1mol) of ceftriaxone, stir to completely dissolve, then stir for 2 hours, and mix the mixture Dropped into 500ml of acetone at high temperature, a large amount of white crystalline powder was precipitated, the solid was filtered by suction, washed with a small amount of acetone, and dried at high temperature under phosphorus pentoxide for 24 hours to obtain 62.3g of white crystalline ceftriaxone tromethamine salt. Yield: 89.2%, mp: 93-95°C, content analysis (HPLC method): contains 82.1-84.1% of ceftriaxone acid. The product was analyzed by elements (theoretical value: C37.8%H4.0%N18.1%022.9%S13.8%Na3.4%; measured value: C38.0%H4.2%N17.9%022.7%S13. 7%Na3.5%), NMR, MS, UV, IR and HPLC analysis, the product is ceftriaxone tromethamine salt, and the purity of ceftriaxone tro...

Embodiment 3

[0070] Embodiment 3: the preparation of ceftezole trometamol

[0071] In a 250ml three-neck flask, add 12.1g (0.1mol) of tromethamine, 4ml of methanol, and 2ml of water, stir at high temperature, add 44g (0.1mol) of ceftezole, stir to make it completely dissolve, then stir for 1 hour, and put the mixture in Drop into 500ml of acetone at high temperature, a large amount of white crystalline powder is precipitated, the solid is suction filtered, washed with a small amount of acetone, and dried at high temperature under phosphorus pentoxide for 24 hours to obtain 49.8g of white crystalline ceftezole tromethamine salt. Yield: 88.8%, content analysis (HPLC method): it contains 77.8-79.0% of ceftezole acid. The product was analyzed by elements (theoretical value: C36.4%H4.1%N22.5%020.0%S17.0%; measured value: C36.2%H4.3%N 22.3%020.2%S17.0%), NMR , MS, UV, IR and HPLC analysis, the product is ceftezole tromethamine salt, and the purity of ceftizoxime tromethamine is 99.0%.

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Abstract

The invention discloses a pehanorm salt or hydrate with chemical formula as picture (1) and drug composition and application to treat bacterial infection, which comprises the following parts: cefuroxime oxtatromethane, cepham qusong tromethane, cepham thiotepa tromethane, cefoperazone tromethane, cephalothin tromethane, cefotaxime tromethane, cefolading tromethane, cefonixin tromethane, cefameizin tromethane, cefadizine tromethane, cefuroxime tromethane, cefazolin tromethane, cefapamine tromethane, cefazoline tromethane, cefaadid tromethane, cefaoxofluoride tromethane, cefaminol tromethane and their hydrate.

Description

Technical field: [0001] The invention belongs to the medical field of compounds, and relates to derivatives of cephalosporin compounds and a preparation method thereof. Background technique: [0002] Cephalosporins (Ce.pha) osporkr) are a family of β-lactam broad-spectrum semi-synthetic antibiotics. The antibacterial part is its mother nucleus 7-aminocephalosporanic acid (7ACA). activity, stability to β-lactamase, and certain pharmacokinetics. The first-generation cephalosporins have been widely used clinically in my country, and the second and third-generation cephalosporins have begun to be introduced, and some of them can also be produced. The fourth-generation cephalosporins are being vigorously researched and developed abroad, and will be introduced into my country and promoted for use soon. [0003] Resistance to most cephalosporins develops during use and has toxic side effects. There are many problems in the use process, such as: 1) there is vascular irritation, a...

Claims

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Application Information

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IPC IPC(8): C07D501/34C07D501/36C07D501/22A61K31/546A61K31/545A61P31/04
Inventor 陈文展王伟
Owner GUANGDONG ZHONGKE DRUG R&D
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