Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Sterilization compound in broad spectrum and usage

A compound and broad-spectrum technology, applied in the field of broad-spectrum bactericidal compounds, can solve problems such as affecting the use of drugs, and achieve the effects of simple production process design, addition of new varieties, and determination of structure.

Inactive Publication Date: 2007-07-25
GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY +1
View PDF0 Cites 5 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Sterilization compound in broad spectrum and usage
  • Sterilization compound in broad spectrum and usage
  • Sterilization compound in broad spectrum and usage

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] 10~15°C, add 45L water and 18L acetone to a 100L reaction tank, then add 10kg of compound II, add 3.9kg of aspartic acid under stirring, stir for 70 minutes, add 1.0kg of activated carbon for needles, stir for 15 minutes, and filter until 500L crystallization tank; 10L water washing reaction tank, also filtered into the 500L crystallization tank. Open the crystallization tank and stir, add dropwise 380L of acetone, and complete the addition of acetone within 2 hours, and a solid precipitates. Keep warm at 0-5°C and stir for 4 hours, filter, wash once with 30 L of acetone, and vacuum-dry at 35-40°C. 9.2 kg of compound I were obtained.

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

[0057] Analysis Project

C

H

N

S

measured value%

50.11

4.55

11.62

6.69

50.06

4.47

11.59

6.54

Calculated%

50.00

4.58

11.67

6.67

[00...

Embodiment 2

[0061] 10-15°C, add 65L of water and 10L of isopropanol into the reaction tank, then add 10kg of compound II, add 4.1kg of aspartic acid dropwise under stirring, stir for 1 hour, add 0.8kg of activated carbon for needles, stir for 60 minutes, Filtration and decarburization; the filtrate is pressed into a 1000L crystallization tank in a sterile room through an ultrafiltration membrane. 15L of water washes the reaction tank and pipelines, and is also pressed into the crystallization tank. Stirring was started, and 6500 L of acetone was added dropwise, and the addition of acetone was completed in 5 hours, and a solid was 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

[0063] 0~5°C, add 50ml of water to a 100ml three-neck flask, then add 10g of compound II, add 4.0g of aspartic 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 300ml of methanol / ethanol (2:7) 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. 7.4 g of compound I are obtained.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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 aspartate (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 polyaspartic 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, and low cost.

Description

technical field [0001] The invention relates to a broad-spectrum bactericidal compound of quinolones, in particular to 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazine[ 3,2-a] Aspartate of quinoline-3-carboxylic acid. 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 ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D513/04A61K31/496A61K9/16A61K9/20A61K9/48A61P31/04A61P15/00A61P17/00A61P27/02A61P27/16
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com