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

Method for preparing fosfluconazole

A technology for forsefluconazole and crude forsefluconazole is applied in the field of preparation of pharmaceutical compounds, and can solve the problems of high content of special impurities, affecting product quality, and low purity of forsefluconazole.

Active Publication Date: 2016-07-13
ZHEJIANG CHENGYI PAHRMACEUTICAL
View PDF5 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The shortcoming of existing method is: the obtained fosfluconazole purity is not high, and the content of special impurity wherein is on the high side, and is difficult to remove, adopts above-mentioned prior art gained forsifluconazole content though can be greater than 98.5%, but two of them The content of a related impurity is greater than 0.3%, which affects the quality of the product. In order to meet higher standard requirements, the present invention improves the method

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
  • Method for preparing fosfluconazole
  • Method for preparing fosfluconazole
  • Method for preparing fosfluconazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] One, step one: the preparation of fosfluconazole intermediate (FSC-1)

[0053] 1) Ratio of materials

[0054]

[0055]

[0056] 2) Operation steps

[0057] Add 1.00kg of FSC-SM1 (fluconazole), 1.79kg of triethylamine, and 8L of dichloromethane into a 30L reaction kettle, stir and cool to -10~0°C;

[0058] Dissolve 538.33g of phosphorus trichloride into 2L of dichloromethane, add to the reaction kettle under stirring, control the rate of addition so that the temperature does not exceed 0°C;

[0059] After the dropwise addition, the temperature was raised to 10-20°C and stirred for 2 hours;

[0060] Drop 1.38kg of benzyl alcohol into the reaction bottle, control the rate of addition so that the temperature does not exceed 20°C; keep stirring at 10-20°C for 2 hours after dropping;

[0061] Cool the reaction solution to 0-10°C, drop 1.33kg of hydrogen peroxide into the reaction bottle, control the rate of addition so that the temperature does not exceed 20°C; keep ...

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 relates to a method for preparing fosfluconazole. The method comprises the following steps: 1, preparing a fosfluconazole midbody 1, namely, by taking fluconazole as a raw material, enabling fluconazole to react with phosphorus trichloride and benzyl alcohol so as to obtain the midbody 1; 2, preparing a crude product of fosfluconazole, namely, hydrogenating the fosfluconazole midbody 1 so as to obtain the crude product of fosfluconazole; 3, preparing a fine product of fosfluconazole, namely, recrystallizing the crude product of fosfluconazole by using a mixed solvent of acetone and dichloromethane in a ratio of 1:2 (v / v), thereby obtaining the fine product of fosfluconazole.

Description

technical field [0001] The invention relates to a preparation method of a pharmaceutical compound, in particular to a synthesis method of an antifungal drug fosfluconazole. Background technique [0002] Fosfluconazole (Fosfluconazole) was developed by Pfizer and launched in Japan in 2003 under the trade name Prodif, which is used to treat deep fungal infections of the respiratory tract, esophagus, and urinary tract. Its structural formula is as follows: [0003] [0004] After intravenous administration of fos fluconazole, it is rapidly hydrolyzed into the active body fluconazole in the plasma. Fluconazole can inhibit the synthesis of ergosterol in the fungal cell membrane, and shows strong activity in the yeast-type development phase and mycelium-type development phase of fungi. antibacterial power. [0005] Many Chinese patents describe the synthesis of fosfluconazole, such as the following Chinese patents [0006] [0007] The shortcoming of existing method is: t...

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): C07F9/6518
CPCC07F9/6518
Inventor 颜贻意茆利平陈丽琪
Owner ZHEJIANG CHENGYI PAHRMACEUTICAL
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