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

Azithromycin tartrate preparation method

A technology of azithromycin and tartrate, applied in the field of preparation of azithromycin tartrate, can solve problems such as being unsuitable for large-scale use, and achieve the effects of easy large-scale use, simple production process and high yield

Active Publication Date: 2007-10-17
XINCHANG GUOBANG CHEM IND +1
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, this method is not suitable for large-scale use

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
  • Azithromycin tartrate preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1, the preparation method of azithromycin tartrate: drop into 60ml dehydrated alcohol 31.2g of azithromycin dihydrate, 6g of tartaric acid (the mol ratio of azithromycin dihydrate and tartaric acid is 1: 1), 25 ℃ of stirring reaction one hour. After the reaction, add 1 g of activated carbon and stir for 10 minutes for adsorption; filter to obtain the filtrate, add 120 ml of ethyl formate dropwise to the above filtrate, stir for half an hour after dropping, filter, and dry the filtrate at 60°C for 2 hours , to obtain 37.0 g of azithromycin tartrate with a yield of 99.4%, m.p.132-138°C.

Embodiment 2

[0016] Embodiment 2, the preparation method of azithromycin tartrate: drop into 60ml absolute methanol 31.2g of azithromycin monohydrate, tartaric acid 4.8 (the molar ratio of azithromycin dihydrate and tartaric acid is 1: 0.8), 10 ℃ of stirring reaction one hour. After the reaction, add 1 g of activated carbon, stir for 10 minutes for adsorption, filter to obtain a filtrate, add 240 ml of ethyl formate dropwise to the above filtrate, stir for half an hour after dropping, filter, and dry the filtrate at 60°C for 2 hours , to obtain 27.2 g of azithromycin tartrate, with a yield of 73.0%, m.p.132-138°C.

Embodiment 3

[0017] Embodiment 3, the preparation method of azithromycin tartrate: drop into azithromycin dihydrate 31.2g, tartaric acid 7.2g (the mol ratio of azithromycin dihydrate and tartaric acid is 1: 1.2) in 60ml n-propanol, 40 ℃ of stirring reaction one hour . After the reaction, add 1 g of activated carbon, stir for 10 minutes for adsorption, filter to obtain the filtrate, add 30 ml of methyl acetate dropwise to the above filtrate, stir for half an hour after dropping, filter, and dry the filtrate at 60°C for 2 hours , to obtain 36.9 g of azithromycin tartrate with a yield of 99.2%, m.p.132-138°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 provides a process for preparing azithromycin tartrate, which comprises, using low grade C1-C4 alcohols as solvent, reacting azithromycin monohydrate or azithromycin dehydrate and tartaric acid in the solvent at a reaction temperature of 0-70 deg. C, charging low grade C2-C6 esters for precipitation, then carrying out filtering and drying.

Description

technical field [0001] The invention relates to a preparation method of azithromycin (Azithromycin) tartrate. Background technique [0002] Azithromycin is a semi-synthetic aza-15-membered ring macrolide antibiotic with the following structural formula: [0003] [0004] Compared with the parent raw material erythromycin A, azithromycin has the advantages of relatively stable acid, high concentration in body tissues, long duration of action, broad antibacterial spectrum, and low side effects. However, like erythromycin, its solubility in water is very small, and it cannot be directly made into injections and oral soluble powders. [0005] In 1984, US4474468 first invented the water-soluble salt of azithromycin - dihydrochloride. Azithromycin and pyridine hydrochloride were reacted in dichloromethane, and after evaporating the solvent, freeze-dried to separate azithromycin dihydrochloride from the aqueous solution, but the yield of this method was very low, only 54.4%. ...

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 Patents(China)
IPC IPC(8): C07H17/08
Inventor 潘伯安刘玉国王卫平
Owner XINCHANG GUOBANG CHEM IND