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Gatifloxacin hydrobride as quinolone compound and its prepn and application as antibacterial agent

A technology of gatifloxacin and quinolones, applied in antibacterial drugs, organic chemistry, pharmaceutical formulations, etc., can solve problems such as unstable light exposure, easy yellowing of aqueous solutions, and achieve good product stability, good water solubility, Low irritant effect on human body

Inactive Publication Date: 2004-11-24
海南康福中正发展有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the salt forms are methanesulfonate, hydrochloride, and lactate, but the above salt forms are unstable when exposed to light, and the aqueous solution easily turns yellow under light.

Method used

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  • Gatifloxacin hydrobride as quinolone compound and its prepn and application as antibacterial agent
  • Gatifloxacin hydrobride as quinolone compound and its prepn and application as antibacterial agent
  • Gatifloxacin hydrobride as quinolone compound and its prepn and application as antibacterial agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Get 30ml of ethanol, 10 grams (0.027mol) of gatifloxacin, in a 250ml there-necked flask, stir and react at 45°C for 0.5 hour, add 6.5g (40%) (0.032mol) of hydrobromic acid, react at 50°C for 2 hours, drop to room temperature, suction filtered, washed with 10 ml of absolute ethanol × 2, and vacuum-dried to obtain 11 g of gatifloxacin hydrobromide.

Embodiment 2

[0019] Take 20ml of water, 10g (0.027mol) of gatifloxacin, in a 250ml there-necked flask, stir and react at 50°C for 0.5 hours, add 5.5g (40%) (0.027mol) of hydrobromic acid, react at 50°C for 2 hours, add acetone 100ml, cooled to room temperature, suction filtered, washed with 10ml of 90% acetone aqueous solution × 2, and vacuum-dried to obtain 10 grams of gatifloxacin hydrobromide.

Embodiment 3

[0021] 8.2 g (40%) (0.0405 mol) of hydrobromic acid, 30 ml of ethanol, and 10 g (0.027 mol) of gatifloxacin.

[0022] Get ethanol 30ml, gatifloxacin 10 grams (0.027mol), in 250ml there-necked bottle, 45 ℃ of stirring reaction 0.5 hour, add hydrobromic acid 8.2 gram (40%) (0.0405mol), 50 ℃ of reaction 2 hours, drop to room temperature, suction filtered, washed with 10 ml of absolute ethanol × 2, and vacuum-dried to obtain 10.8 g of gatifloxacin hydrobromide.

[0023] Tests have shown that the aqueous solution of the above-mentioned quinolone gatifloxacin hydrobromide dissolved in water basically does not change color under light conditions for 7 days.

[0024] Embodiment 3: antibacterial agent preparation for injection

[0025] Take an appropriate amount of quinolone gatifloxacin hydrobromide, and operate according to the preparation process procedures of injection, powder injection, and freeze-dried powder injection. During the preparation process, an appropriate amount of ph...

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PUM

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Abstract

The present invention discloses Gatifloxacin hydrobromate as one kind of quinolone compound and its chemical structural expression, preparation and application. The preparation process adopts Gatifloxacin as main material, and includes reaction with hydrobromic acid in organic solvent or water at 40-50 deg.c for 1-5 hr to produce salt, and subsequent crystallization to obtain Gatifloxacin hydrobromate product. The compound has high water solubility, high stability and less irritation, and its Gatifloxacin component produces antibacterial effect in human body to treat various infectious diseases.

Description

technical field [0001] The invention relates to a quinolone compound, gatifloxacin hydrobromide, namely: hydrobromic acid, 1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methyl-1-piper Azinyl)-1,4-trihydro-4-oxidation-3-quinolinic acid, a preparation method of the compound, and an application of the compound as an antibacterial agent. Background technique [0002] Gatifloxacin (Gatifloxacin) is the fourth generation of fluoroquinolone antibacterial drugs, the drug has excellent broad-spectrum activity, not only maintains the strong activity of ciprofloxacin, ofloxacin, levofloxacin, etc. against Gram-negative bacteria Advantages, while overcoming their shortcomings of Gram-positive bacteria (especially Streptococcus pneumoniae), anaerobic bacteria, mycoplasma, chlamydia, mycobacteria, etc. are not active, and these pathogens also have better activity. In addition, gatifloxacin is rapidly absorbed orally, widely distributed in tissues, has a low serum protein binding rate, and has a ...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61P31/04C07D401/04
Inventor 汤小东汤旭东
Owner 海南康福中正发展有限公司
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