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Synthetic method of erythromycin estolate

A technology based on erythromycin and a synthesis method, applied in the field of pharmaceutical synthesis, can solve problems such as unfavorable environmental impact, impact on product quality, low water content in acetone, etc., and achieve uniform product particle size, improve solvent utilization rate, and improve product yield. Effect

Active Publication Date: 2015-06-24
HUANGSHI SHIXING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] First; the reaction solvent acetone must ensure that the water content is very low, and the requirements for the solvent are strict, resulting in high production costs;
[0006] Second, the desulfurization process is complex and costly, requiring the use of expensive potassium salts, which is detrimental to the environment;
[0007] Thirdly, using potassium carbonate for desulfurization, the alkalinity of the system is high, which is easy to destroy the erythromycin base (the erythromycin base is easy to remove a sugar group when the pH value is ≥ 11), which affects the product quality;

Method used

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  • Synthetic method of erythromycin estolate
  • Synthetic method of erythromycin estolate
  • Synthetic method of erythromycin estolate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 20g of water and 50g of erythromycin thiocyanate to 140g of acetone, raise the temperature to 35-38°C, stir for 5 minutes, add 9g of triethylamine to desulfurize erythromycin thiocyanate into free erythromycin base, and dissolve the system ;

[0026] Add 13.5g propionic anhydride at 35-38°C and react for 120 minutes to generate erythromycin propionate; filter;

[0027] Then add dodecyl sulfate solution (dodecyl sulfate solution is prepared as dodecyl sulfate: water = 17g: 90g) and keep warm for 60 minutes to generate etodomycin;

[0028] Add 50g of water at 35-38°C to make the solution cloudy, and stir for 60 minutes to precipitate a large amount of Etoerythromycin;

[0029] Add 500g of water to cool down to 5-10°C for crystallization, centrifuge for 60 minutes, wash the filter cake with water and dry it to obtain 61g of erythromycin eptomycin. The weight yield is 61 / 50=122%.

[0030] The product produced by the above process is white crystalline powder; almost o...

Embodiment 2

[0038] Add 28g of water and 50g of erythromycin thiocyanate to 175g of acetone, raise the temperature to 38-42°C, stir for 10 minutes, add 8g of triethylamine to desulfurize erythromycin thiocyanate into free erythromycin base, and dissolve the system ;

[0039] Add 15g of propionic anhydride at 38-42°C and react for 120 minutes to generate erythromycin propionate; filter;

[0040] At 38-42°C, add dodecyl sulfate solution (dodecyl sulfate solution is prepared as dodecyl sulfate: water = 19g: 100g) and keep it warm for 40 minutes to generate etoerythromycin;

[0041] Add 50g of water at 38-42°C to make the solution turbid, and continue to stir for 40 minutes to precipitate a large amount of Etoerythromycin;

[0042] Add 400g of water to cool down to 5-10°C for crystallization, centrifuge for 60 minutes, wash the filter cake with water and then dry it to obtain 62g of erythromycin ethodomycin. The weight yield was 124%.

[0043] The obtained sample was confirmed by structure ...

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Abstract

The invention discloses a synthetic method of erythromycin estolate. The synthetic method comprises following steps: erythromycin thiocyanate is taken as a main raw material, acetone-water is taken as a solvent, triethylamine is subjected to desulphurization, and then erythromycin estolate is synthesized by subjecting desulfurated triethylamine, propionic anhydride and dodecyl sulfate to one-port method. The synthetic method is capable of simplifying production processes significantly, reducing production cost, and increasing product quality, and is suitable for industrial production. Yield reaches 120 to 125% (weight yield).

Description

technical field [0001] The invention relates to a method for synthesizing erythromycin, which belongs to the technical field of medicine synthesis. Background technique [0002] Etoerythromycin is the dodecyl sulfate of erythromycin propionate, which is more stable in gastric acid than erythromycin. Clinically, it is used as an alternative drug for the treatment of the following infections in patients with penicillin allergy: acute tonsillitis, acute pharyngitis, and sinusitis caused by hemolytic streptococcus and pneumonia; scarlet fever and cellulitis caused by hemolytic streptococcus; diphtheria and Carriers of diphtheria; gas gangrene, anthrax, tetanus; actinomycosis; syphilis; listeriosis, etc. Etoerythromycin can be quickly absorbed on an empty stomach or orally after food, with a high protein binding rate of 90-99%. After oral administration, it is decomposed into erythromycin propionate in the gastrointestinal tract, and part of it is hydrolyzed into free erythromy...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/08C07H1/00
Inventor 卢元东汪寅华
Owner HUANGSHI SHIXING PHARMA
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