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

Azithromycin production technology

A technology of azithromycin and production process, applied in the field of drug synthesis, can solve the problems of low final yield, difficult to control the reaction, long process, etc., and achieve the effects of high yield, increased yield, and complete crystallization

Inactive Publication Date: 2015-09-09
HUANGSHI SHIXING PHARMA
View PDF4 Cites 14 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The current production of azithromycin is to obtain erythromycin 6,9-imine ether through Beckmann rearrangement reaction of erythromycin oxime, and then undergo reduction reaction and methylation reaction to finally crystallize azithromycin. The process is long and the reaction is difficult to control. lead to low final yield

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0013] The invention provides a kind of azithromycin production process, its step comprises:

[0014] (1) Synthesis of erythromycin oxime: react erythromycin thiocyanate and hydroxylamine at 30-60°C for 10-36 hours, then neutralize with alkali to obtain erythromycin oxime;

[0015] (2) Synthesis of erythromycin A-6,9-imine ether: dissolve the erythromycin oxime obtained in step (1) in the acetone-water system so that the mass ratio of acetone to water is 0.5~0.8:2~2.5 , add methanesulfonyl chloride and sodium hydroxide, react at pH 9.7-10.5, 3-5°C for 3-4 hours, and centrifuge;

[0016] (3) Synthesis of 9-deoxy-9a-aza-9a-homoerythromycin: add the product obtained in step (2) to water, adjust the pH to 5.5-6.5 at 0-5°C, and add potassium borohydride after completely dissolving After 2-4 hours of reaction, add dichloromethane, adjust the pH to 9.5-10.0 and separate the liquid, keep the organic layer, add the organic layer to water and hydrolyze it at pH 1.0-1.5, and adjust the ...

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 provides an azithromycin production technology. The azithromycin production technology comprises (1), erythromycin oxime synthesis, (2), erythromycin A-6,9-iminoether synthesis, (3), 9-deoxo-9a-aza-9a-homoerythromycin synthesis, (4), azithromycin synthesis and (5), refining. The azithromycin production technology realizes strict control of an acetone-water ratio in erythromycin A-6,9-iminoether synthesis, guarantees dispersibility of erythromycin oxime in a system, is convenient for reaction control, improves a yield and can be industrialized easily. In 9-deoxo-9a-aza-9a-homoerythromycin synthesis, pH is controlled in a range of 1.0-1.5 in reduction product acidolysis so that reduction product hydrolysis is thorough, a yield is improved and post-treatment troubles are reduced. In a methylation reaction for azithromycin synthesis, a crystallization water dropwise addition rate and a dropwise addition total amount are strictly controlled so that crystallization is complete, granularity is uniform and an azithromycin yield is improved.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a production process of azithromycin. Background technique [0002] In recent years, due to the rise of β-lactamase strains produced by common respiratory pathogens such as influenza bacillus, pneumococcus, and Moraxella catarrhalis, the increase of other pathogenic microorganisms such as mycoplasma, chlamydia, and Legionella infections, as well as the increase in immunodeficiency patients Mycobacterium avium, The emergence of Toxoplasma infection has brought attention to the clinical application of macrolide antibiotics. [0003] Azithromycin is one of the modified macrolide derivatives. It is a broad-spectrum macrolide antibiotic obtained after modifying the structure of erythromycin. It mainly binds to the bacterial 50S ribosomal subunit to block The translocation of peptides prevents the synthesis of bacterial peptides and achieves antibacterial effects. Azithromycin has the 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): C07H17/00C07H1/00
CPCC07H17/00C07H1/00C07H1/06
Inventor 卢元东汪寅华金建平
Owner HUANGSHI SHIXING PHARMA
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