Antibacterial compound in broad spectrum and usage

A technology for compounds and antibacterial drugs, applied in the directions of antibacterial drugs, organic chemistry, drug delivery, etc., can solve problems such as affecting the use of drugs, and achieve the effects of simple production process design, new varieties, and low production costs.

Inactive Publication Date: 2007-07-25
GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazine[3,2-a]quinoline-3-carboxylic acid is insoluble in water, so it affects the use of its medicine

Method used

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  • Antibacterial compound in broad spectrum and usage
  • Antibacterial compound in broad spectrum and usage
  • Antibacterial compound in broad spectrum and usage

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] 15~20°C, add 50L water and 5L isopropanol into a 100L reaction tank, then add 10kg of compound II, add 13L of 50% gluconic acid aqueous solution dropwise under stirring, stir for 30 minutes, add 0.5g of activated carbon for needles, stir for 15 Minutes, filtered into the 500L crystallization tank; 10L water washing reaction tank, filtered into the 500L crystallization tank. Open the crystallization tank and stir, add 400 L of isopropanol dropwise, and finish adding isopropanol in 4 hours, and a solid precipitates out. Keep warm at 15-20°C and stir for 2 hours, filter, wash once with 20L of isopropanol, and vacuum-dry at 35-40°C. 8.9 kg of compound I were obtained.

[0056] The product elemental analysis results are as follows:

[0057] Analysis Project

C

H

N

S

measured value%

48.55

4.86

7.75

5.87

48.67

4.72

7.68

5.79

Calculated%

48.62

...

Embodiment 2

[0061] 10~15°C, add 50L water and 20L isopropanol to the reaction tank, then add 10kg compound II, add dropwise 13.4L of 50% gluconic acid aqueous solution under stirring, stir for 1 hour, add 0.5kg of activated carbon for needles, stir for 60 Minutes, filter and decarburize; the filtrate is pressed into a 1000L crystallization tank in a sterile room through a 0.22μm ultrafiltration membrane. 15L of water washes the reaction tank and pipelines, and is also pressed into the crystallization tank. Stirring was started, and 650 L of acetone was added dropwise, and the addition of acetone was completed in 5 hours, and a solid precipitated. Keep warm at 0-5°C and stir for 5 hours, filter, wash with acetone 30L×2 twice, and vacuum-dry at 35-40°C. Obtain 8.4kg of sterile powder of compound I.

Embodiment 3

[0063] 0~5°C, add 50ml of water to a 100ml three-neck flask, then add 10g of compound II, add 13.2L of 50% gluconic acid aqueous solution dropwise under stirring, stir for 30 minutes, add 0.5g of activated carbon for needles, stir for 15 minutes, filter Decarburization; wash the three-necked flask with 10ml of water, and filter. Combine the filtrates into a 500ml three-neck flask, add 300ml of ethanol dropwise under stirring, and add the mixed solution in 3 hours, and a solid precipitates out. Keep warm at 15-20°C and stir for 2 hours, filter, wash once with 20ml of absolute ethanol, and vacuum-dry at 35-40°C. 6.9 g of compound I are obtained.

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Abstract

This invention relates to an antibacterial compound, more specifically, 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1, 3] thiazine [3, 2-a] quinoline-3-carboxylic glyconate (compound I), its preparation method and its application. Compound I is prepared by reaction of 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1,3]thiazine[3,2-a]quinoline-3-carboxylic acid and gluconic acid. Compound I can be used as effective component and mixed with normal pharmaceutical carrier to manufacture antibacterial drug composition, which can be tablets, capsules, granules, injection, eye preparations, ear preparations, gynecological preparations, and external use preparations. Compound I has stable properties, and can be easily dissolved in water, thus can be easily manufactured into various preparations used in clinical treatment. The method has such advantages as simple and reasonable process.

Description

technical field [0001] The invention relates to a broad-spectrum antibacterial compound of quinolones, in particular to 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazine[ 3,2-a] Quinoline-3-carboxylic acid gluconate. Background technique [0002] Quinolones are antibacterial drugs that have developed rapidly in recent years. They have the advantages of broad antibacterial spectrum, strong antibacterial power, simple structure, convenient administration, no cross-resistance with other commonly used antibacterial drugs, and high curative effect and price ratio. It has been paid attention to by various countries and has become a hot drug that is competing for production and application. There are dozens of varieties of quinolone products on the market, which is one of the most active fields in the development of anti-infective drugs. [0003] 6-Fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazine[3,2-a]quinoline-3-carboxylic acid is a Qu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D513/04A61K31/496A61K9/20A61K9/48A61K9/14A61K9/08A61P31/04
Inventor 刘学斌刘丹青万平黄翔陈矛叶放梁少娟陈绍奎
Owner GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY
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