Unlock instant, AI-driven research and patent intelligence for your innovation.

Florfenicol acetic ester and preparation method thereof

A technology of florfenicol acetate and florfenicol, which is applied in chemical instruments and methods, preparation of organic compounds, organic chemistry, etc. Expensive and other problems, to achieve the effect of long half-life, fast effect, and overcoming drug resistance

Inactive Publication Date: 2010-02-17
ZHENGZHOU HOUYI PHARMA
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solubility of water-soluble florfenicol obtained by the inclusion method can meet the requirements of soluble powder preparations, but hydroxypropyl-β-cyclodextrin is expensive and difficult to apply to veterinary drug preparations

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
  • Florfenicol acetic ester and preparation method thereof
  • Florfenicol acetic ester and preparation method thereof
  • Florfenicol acetic ester and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Example 1: Take 0.068mol of Florfenicol and place it in a three-neck flask, add 0.34mol of acetic anhydride and stir, then add 0.1ml of perchloric acid and stir to dissolve, heat to 50°C and continue stirring for 3h, then put in an ice-water bath Crystallize in the medium, filter with suction, then recrystallize in ethanol, filter with suction, wash the obtained crystals with 35ml of hexane, and then dry at 60°C to obtain florfenicol acetate.

Embodiment 2

[0014] Example 2: Take 0.137mol of Florfenicol and place it in a three-neck flask, add 0.6mol of acetic anhydride and stir, then add 0.137ml of perchloric acid and stir to dissolve, heat to 48°C and continue stirring for 4h, then put it into an ice-water bath Crystallization in the medium, suction filtration, and then recrystallization in ethanol, suction filtration, the resulting crystals were washed with 60ml of hexane, and then dried at 65°C to obtain florfenicol acetate.

Embodiment 3

[0015] Example 3: Take 0.15 mol of Florfenicol and place it in a three-neck flask, add 0.9 mol of acetic anhydride and stir, then add 0.18 ml of perchloric acid and stir to dissolve, heat to 45°C and continue stirring for 4 hours, then put it into an ice-water bath Crystallization in the medium, suction filtration, and then recrystallization in ethanol, suction filtration, the obtained crystals were washed with 80ml of hexane, and then dried at 70°C to obtain florfenicol acetate.

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

The invention discloses florfenicol acetic ester. A preparation method of the florfenicol acetic ester comprises the following steps: adding acetic anhydride to florfenicol acetic ester and mixing, and then adding perchloric acid and stirring for dissolving, heating to 45 DEG C-50 DEG C and stirring for fully reacting for 3-4 hours; putting reaction products in an icewater bath for crystallizationafter the reaction is ended; carrying out suction filtration; then carrying out recrystallization in ethanol; carrying out suction filtration; washing crystal by ethane, then drying at the temperature of 60-80 DEG C, and finally obtaining florfenicol acetic ester. The florfenicol acetic ester increases water solubility and has low loss during the physiological disposition after being taken orallyand injected; the florfenicol acetic ester releases ester and florfenicol after being metabolized by in vivo biological enzyme, wherein ester overcomes the drug resistance of bacteria, and meanwhile,florfenicol carries out targeting so as to display the extreme effort of drug to react on an organism. Florfenicol acetic ester has low use level, fast effect, long half decay period and high blood concentration and can maintain the blood concentration for a longer time.

Description

technical field [0001] The invention belongs to the technical field of medicines, relates to a florfenicol acetate and a preparation method of the florfenicol acetate. Background technique [0002] Florfenicol (Florfenicol), also known as florfenicol and florfenicol, is a 3-position fluorine derivative of thiamphenicol (Thiamphenicol) in chloramphenicol broad-spectrum antibacterial drugs, and its chemical name is: [ R-(R * , R * )]-2,2-dichloroN-[1-(fluoromethyl)-2-hydroxy-2-[4-(methylsulfonyl)phenyl]ethyl]acetamide. Florfenicol can be used to treat bovine respiratory diseases caused by Pasteurella and Haemophilus, has a good curative effect on cattle foot rot caused by Fusobacterium, and can also be used to treat pig and chicken infections caused by sensitive bacteria Diseases, such as pigs exposed to contagious pleuropneumonia. Florfenicol is a new type of antibiotic specially used in the animal health care market. Its biggest features are broad antibacterial spectrum,...

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
Patent Type & Authority Applications(China)
IPC IPC(8): C07C317/32C07C315/04A61P31/04
Inventor 吴红云李建正李亚娥刘应鹏
Owner ZHENGZHOU HOUYI PHARMA