Check patentability & draft patents in minutes with Patsnap Eureka AI!

Preparation method of cefdinir impurity F

A cefdinir and impurity technology, which is applied in the field of medicinal chemistry, can solve the problems of affecting drug safety, difficult to obtain monomer impurities, carcinogenic teratogenicity of impurities, etc. Effect

Inactive Publication Date: 2020-01-10
PI & PI BIOTECH
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Cefdinir impurities are a kind of ingredients that have no medicinal effect in medicines, and some impurities are carcinogenic and teratogenic. These impurities have adverse reactions, seriously affect the safety of medication, and bring immeasurable risks to drug users
[0004] The preparation process of cefdinir generic drug in China is various, resulting in different impurities, which are different from the original research drug, and the content and type of impurities will also be different. However, the domestic production mechanism, synthesis preparation, Separation, purification, and pharmacology have not been systematically and comprehensively studied. Some impurities have multiple tautomers. Due to the limitation of separation and purification technology, it is difficult to obtain monomeric impurities and cannot be systematically studied. As a result, the quality of generic drugs is significantly worse than that of original research. 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
  • Preparation method of cefdinir impurity F
  • Preparation method of cefdinir impurity F
  • Preparation method of cefdinir impurity F

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A preparation method of cefdinir impurity F, comprising the following steps:

[0030] (1) At room temperature, weigh 10 g of cefdinir, add 100 mL of acetonitrile, start stirring, add 10 mL of triethylamine dropwise, start the reaction, and react at 20°C for 6 hours;

[0031] (2) After the reaction is finished, adjust the pH to 5 with 0.1mol / L hydrochloric acid to obtain a mixed solution;

[0032] (3) Put the mixed solution obtained in step (2) on a 400mL C18 column for column chromatography separation, and successively use 1%, 3%, and 6% acetonitrile aqueous solutions to elute 2.5L, and the separated fractions are frozen After drying, the cefdinir impurity F with a purity of more than 90% was obtained, and the yield was 30.2%.

Embodiment 2

[0034] A preparation method of cefdinir impurity F, comprising the following steps:

[0035] (1) At room temperature, weigh 10 g of cefdinir, add 50 mL of acetonitrile, start stirring, add 1 mL of triethylamine dropwise, start the reaction, and react at 5°C for 6 h;

[0036] (2) After the reaction is finished, adjust the pH to 5 with 0.1mol / L hydrochloric acid to obtain a mixed solution;

[0037] (3) Put the mixed solution obtained in step (2) on a 400mL C18 column for column chromatography separation, and successively use 1%, 3%, and 6% acetonitrile aqueous solutions to elute 2.5L, and the separated fractions are frozen After drying, the cefdinir impurity F with a purity of more than 90% was obtained, and the yield was 32.7%.

Embodiment 3

[0039] A preparation method of cefdinir impurity F, comprising the following steps:

[0040] (1) At room temperature, weigh 10g of cefdinir, add 150mL of acetonitrile, start stirring, add 5mL of triethylamine dropwise, start the reaction, and react at 10°C for 7h;

[0041] (2) After the reaction is finished, adjust the pH to 5 with 0.1mol / L hydrochloric acid to obtain a mixed solution;

[0042] (3) Put the mixed solution obtained in step (2) on a 400mL C18 column for column chromatography separation, and successively use 1%, 3%, and 6% acetonitrile aqueous solutions to elute 2.5L, and the separated fractions are frozen After drying, the cefdinir impurity F with a purity of more than 90% was obtained, and the yield was 35.4%.

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 preparation method of cefdinir impurity F, belonging to the field of pharmaceutical chemistry. The preparation method of the cefdinir impurity F comprises the following steps: reacting cefdinir under triethylamine, and obtaining the cefdinir impurity F through separation and purification. The preparation method of cefdinir impurity F has mild reaction conditions, does not involve ultra-low temperature reaction, reduces process steps, and is suitable for laboratory pilot scale-up; the purity of cefdinir impurity F prepared can reach more than 90%, and the method can meet the quality research needs and provide a technical basis for improving the national quality standard of cefdinir.

Description

technical field [0001] The invention relates to a preparation method of cefdinir impurity F, which belongs to the field of medicinal chemistry. Background technique [0002] Cefdinir (Cefdinir) belongs to the third-generation cephalosporins, and is a cephalosporin antibiotic developed by Fujisawa Pharmaceutical Co., Ltd. in Japan. It was first listed in Japan in October 1991. The trade name is Cefzon. It was listed in the United States in December 1997. It was launched in South Korea in 2001, and domestic cefdinir was approved to be listed in China in 2001. In April 2009, Shanghai Anhante Biomedical Technology Co., Ltd. applied for the import of raw materials and was approved by SFDA. Cefdinir is stable against β-lactamase, has a broad antibacterial spectrum, strong antibacterial effect, high clinical efficacy, low toxicity, less allergic reactions, and is convenient to use. Compared with drugs such as cefixime, cefuroxime, cefaclor and cefprozil, cefdinir has the strongest...

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): C07D501/04C07D501/60
CPCC07D501/04C07D501/60
Inventor 袁晓林顺权
Owner PI & PI BIOTECH
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com