Method of synthesizing antibiotics cefamandole nafate

A technology of cefamandide sodium and a synthesis method, which is applied in directions such as organic chemistry, can solve problems such as affecting acylation reaction, increase manufacturing cost, increase operation steps, etc., and achieves simple process operation, good product quality and product yield high effect

Active Publication Date: 2008-01-23
苏州盛达药业有限公司
View PDF2 Cites 23 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In this method, the by-product ammonia gas produced in the silylation reaction needs to be removed from the silylation reaction system as much as possible, otherwise it will affect the acylation reaction. Additional fulvic acid agent is used to neutralize the hydrogen chlori

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 of synthesizing antibiotics cefamandole nafate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0025] In a 500ml four-necked reaction flask, add 300ml ethyl acetate, 30g 7-ATCA (0.092mol), control the temperature at 20~25℃, add 13.5ml HMDS (0.064mol), add 8.2ml dropwise while stirring Trimethylchlorosilane (0.064mol). After the dropwise addition is completed, the temperature is raised to 35-40°C for reaction, and after 3 to 4 hours of reaction, the temperature is lowered to 25-30°C to obtain a silicon ester solution of 7-ATCA.

[0026] Add 15.6ml D-(-)-2-formyloxy-2-phenylacetyl chloride (0.092mol) dropwise to the above-mentioned 7-ATCA silicon ester solution. After 30 minutes of dropping, keep the temperature at 25 At -30°C, the reaction was carried out with stirring for 1.5 to 2 hours, and the end of the reaction was detected by HPLC (the concentration of remaining 7-ATCA in the reaction solution was less than 1 mg / ml).

[0027] 200ml of deionized water was added to carry out the hydrolysis reaction, stirred for 20 minutes, the water layer was removed, the organic layer c...

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 synthetic method of the antibiotic cefamandole nafate, which adopts the 7-amino-3-(1-methyl-1H-tetrazoline-5-base)-sulfomethyl-3-cef-4-carboxylic acid as raw material and gains the solid of the cefamandole nafate through such five steps as the silylation reaction, acylation reaction, hydrolysis reaction, decolorization and salifying. The silanizing agent used in the silylation reaction adopts the mixture of the silicon amine alkane and the alkylogen silane. Compared with the prior art, the invention is characterized by simple in process operation, low in cost, high in product yield, good in product quality and suitable for industrial production.

Description

Technical field [0001] The invention relates to a method for synthesizing antibiotic cefmendol sodium, which belongs to the field of drug synthesis. Cefmendolin sodium is mainly used to prepare injection powder injections and oral preparations and other dosage forms, and is widely used in clinical practice. Background technique [0002] Cefmendol sodium belongs to the second-generation cephalosporin antibiotics, and its chemical name is 7-D-(2-formyloxyphenylacetamide)-3-[(1-methyl-1H-tetrazol-5yl )Sulfomethyl]-3-cephem-4-carboxylic acid sodium salt, this product is the second-generation cephalosporin antibiotic originally developed by Lilly Company of the United States. [0003] Cefmendol Sodium is a prodrug of Cefmendol, its antibacterial activity is only 1 / 5 of Cefmendol. Cefmendol sodium enters the body and rapidly hydrolyzes to Cefmendol, so the antibacterial effects of the two in the body are basically the same. . Cefmendole has a strong antibacterial effect on most gram-po...

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): C07D501/36
Inventor 方长明
Owner 苏州盛达药业有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap