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Anti infectious compound and usage

A compound and anti-infection technology, which is applied in the field of quinolone anti-infection drugs, can solve problems affecting the use of drugs, and achieve the effect of adding new varieties, definite structure, and stable properties

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 compound II is insoluble in water, it affects the use of its medicine

Method used

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  • Anti infectious compound and usage
  • Anti infectious compound and usage
  • Anti infectious compound and usage

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] Add 50L of water and 5L of ethanol into a 100L reaction tank, add 10Kg of compound II at 15-20°C, add 2.8Kg of methanesulfonic acid dropwise under stirring, stir for 30 minutes, add 0.5Kg of activated carbon for needles, stir for 15 minutes, and filter to 500L crystallization tank; wash the reaction tank with 10L water and filter into the 500L crystallization tank. Under stirring, about 350 L of isopropanol was added dropwise into the crystallization tank, and the addition of isopropanol was completed in 3 hours, and a solid was precipitated. Keep warm at 5-10°C and stir for 2 hours, filter, wash once with 20 L of isopropanol, and vacuum-dry at 35-40°C. 8.7 Kg of compound I were obtained.

[0087] The product elemental analysis results are as follows:

[0088] Analysis Project

C

H

N

S

measured value%

52.11

4.86

9.56

7.39

52.21

4.79

9.64

7.28

Calculated...

Embodiment 2

[0114] Add 50L of water and 15L of acetone into the reaction tank, add 10Kg of compound II at 10-15°C, add 2.8Kg of methanesulfonic acid dropwise under stirring, stir for 1 hour, add 0.5Kg of activated carbon for needles, stir for 20 minutes, filter and decarburize ; The filtrate is pressed into a 500L crystallization tank in a sterile room through a 0.22μm ultrafiltration membrane. 10L of water washes the reaction tank and pipeline, and is also pressed into the crystallization tank. Stirring was started, and 350 L of acetone was added dropwise. The addition of acetone was completed in 4 hours, and a solid precipitated. Keep warm at 0-5°C and stir for 5 hours, filter, wash twice with acetone 30L×2, and vacuum-dry at 35-40°C. Obtain 8.4Kg of sterile powder of Compound I.

Embodiment 3

[0116] Add 50ml of water into a 100ml three-neck flask, add 10g of compound II at 0-5°C, add 4.1g of methanesulfonic acid dropwise under stirring, stir for 30 minutes, add 0.5g of activated carbon for needles, stir for 15 minutes, filter and decarburize ; Wash the three-necked bottle with 10ml of water and filter. Combine the filtrates into a 500ml three-neck flask, add dropwise 350ml of ethanol under stirring, and finish adding the mixed solution in 2 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 anti-infective compound, more specifically, 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1, 3] thiazine [3, 2-a] quinoline-3-carboxylic mesylate (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 methyl sulfonic acid. Compound I can be used as effective component and mixed with normal pharmaceutical carrier to manufacture anti-infective 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 quinolone anti-infective drug, in particular to 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazine[3, 2-a] Quinoline-3-carboxylic acid methanesulfonate, preparation method and use thereof. 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 Quinol...

Claims

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Application Information

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IPC IPC(8): C07D513/04A61K31/496A61K9/20A61K9/48A61K9/08A61K9/14A61P31/00
CPCC07D513/04A61P31/00
Inventor 刘学斌刘丹青万平陈矛黄翔叶放梁少娟陈绍奎
Owner GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY
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