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Organic amine salt of cilin analog compound and its preparation method

A technology of organic amine salts and compounds, applied in the field of derivatives of penicillin antibiotic compounds and their preparation, can solve problems such as muscle irritation, vasculitis, hypernatremia, etc.

Inactive Publication Date: 2007-08-01
陈文展
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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;) Most of them exist in the form of sodium salts, and sodium ions enter the human body in such a large amount that diabetes Bacterial infection patients, neurosurgery patients, patients with heart and kidney insufficiency, or high blood pressure patients are at high risk, which can easily cause hypernatremia and cause adverse reactions; 3) Some varieties have incompatibility and are inconvenient to use; 4) Intramuscular injection Sometimes there is muscle irritation; etc.

Method used

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  • Organic amine salt of cilin analog compound and its preparation method
  • Organic amine salt of cilin analog compound and its preparation method
  • Organic amine salt of cilin analog compound and its preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0047] Embodiment 1: the preparation of azlocillin arginine

[0048] In a 250ml three-necked flask, add 17.4g (0.1mol) of arginine and 20ml of 60% ethanol, drop into 20ml of 80% ethanol solution containing 46.2g (0.1mol) of azlocillinic 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 56.2 g of powdery solid with a yield of 88.3%. Content analysis: (HPLC method) contained 72.2-73.1% of azlocillinic acid. According to NMR, MS, UV, IR and HPLC analysis, the product is azlocillin arginine salt with a purity of 95.2%.

Embodiment 2

[0049] Embodiment 2: the preparation of amoxicillin arginine

[0050] In a 250ml three-neck flask, add 17.4g (0.1mol) of arginine, 4ml of methanol, and 2ml of water, stir at high temperature, add 33.3g (0.1mol) of amoxicillin, stir until it is completely dissolved, and then stir for 2 hours. Dropped into 500ml of acetone at high temperature, a large amount of white crystalline powder was precipitated, the solid was filtered with suction, washed with a small amount of acetone, and dried at high temperature under phosphorus pentoxide for 24 hours to obtain 45.4g of white crystalline amoxicillin arginine salt. Yield: 89.5%, content analysis (HPLC method): containing 65.1-66.2% of amoxicillin acid. NMR, MS, UV, IR and HPLC analysis showed that the product was amoxicillin arginine salt with a purity of 94.3%.

Embodiment 3

[0051] Embodiment 3: the preparation of ampicillin arginine

[0052] In a 250ml three-necked flask, add 17.4g (0.1mol) of tromethamine, 4ml of methanol, and 2ml of water, stir at high temperature, add 34.9g (0.1mol) of ampicillin, stir to completely dissolve and then stir for 1 hour, and put the mixture in Drop it into 500ml of acetone at high temperature, a large amount of white crystalline powder precipitates out, 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 46.4g of white crystalline ampicillin tromethamine salt. Yield: 88.7%, content analysis (HPLC method): containing 66.3-67.1% of ampicillin acid. NMR, MS, UV, IR and HPLC analysis showed that the product was ampicillin arginine salt with a purity of 96.2%.

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Abstract

The invention relates to the organic amine salt or hydrate for Nishibayashi compound used for treating bacteria infection, and the chemical formula is demonstrated in (I). It comprises azlocillin organic amine salt, amoxicillin organic amine salt, ampicillin organic amine salt, oxacillin organic amine salt, furbenicillin organic amine salt, cloxacillin organic amine salt, mezlocillin organic amine salt, mecillin organic amine salt, piperacillin organic amine salt, ticarcillin organic amine salt, flucloxacillin organic amine salt, hetacillin organic amine salt, ortho-chlorocillin organic amine salt, penicillin organic amine salt and their hydrate. The invention provides the medical compound taking compound in formula (I) as active element and its application to preparation of medicine for treating bacteria infection.

Description

Technical field: [0001] The invention belongs to the medical field of compounds, and relates to derivatives of cillin antibiotic compounds and a preparation method thereof. Background technique: [0002] Penicillin drugs belong to the penicillin class of antibiotics, including aminopenicillins (including ampicillin, amoxicillin, bamicillin, pampicillin, etc.), and are mainly used for penicillin-sensitive Gram-positive bacteria and some Gram-negative bacteria such as large intestine Bacillus, Proteus mirabilis, Salmonella, Shigella and influenza bacilli, etc.; anti-staphylococcal penicillins (including cloxacillin, dicloxacillin, oxacillin, flucloxacillin, methicillin, nafcillin, etc.) , also has a good effect on β-lactamase-producing Staphylococcus; anti-pseudomonal penicillins (including carbenicillin, mezlocillin, piperacillin, ticarcillin, etc.), have a more natural effect on grass-positive bacteria Penicillin or aminopenicillin is poor, but has antibacterial activity ag...

Claims

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Application Information

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IPC IPC(8): C07D499/44C07D499/74C07D499/76A61K31/43A61K31/431A61P31/04
Inventor 陈文展
Owner 陈文展
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