Synthesis method of tiamulin

A tiamulin and synthesis method technology, applied in the field of chemical synthesis of veterinary raw materials, can solve the problems of difficult diethylaminoethanethiol, high price, bad smell, etc., and achieve the effect of simple operation and low cost

Active Publication Date: 2015-09-09
SHAANXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The main problem of this method is that diethylaminoethanethiol, which is expensive, smelly and difficult to buy, must be used in the reaction process, which limits the production of tiamulin

Method used

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  • Synthesis method of tiamulin
  • Synthesis method of tiamulin
  • Synthesis method of tiamulin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] 1. Add 31.97g (0.42mol) thiourea to the methyl isobutyl ketone solution containing 213.07g (0.4mol) pleuromutilin p-toluenesulfonate, stir and react at 60°C for 1.5 hours, then add 30.42g (0.16mol) of sodium metabisulfite, 120g of distilled water, reflux at 90°C for 1 hour, separate the layers, and remove the water layer to obtain a methyl isobutyl ketone solution of pleuromutilin.

[0024] 2. Add 92.93g (0.54mol) 2-diethylamino-1-chloroethane hydrochloride, 21.60g (0.54mol) to the methyl isobutyl ketone solution of pleuromutilin obtained in step 1 NaOH and 240 g of distilled water were stirred at 60° C. for 2 hours, the water layer was removed, and the organic layer was concentrated to dryness under reduced pressure to obtain 170.24 g of tiamulin with a total yield of 86.2%.

Embodiment 2

[0026] In step 2 of embodiment 1, the 2-diethylamino-1-chloroethane hydrochloride used is replaced with equimolar 2-diethylamino-1-bromoethane hydrobromide, other steps and implementation Same as Example 1, 162.74 g of tiamulin was obtained, and the total yield was 82.4%.

Embodiment 3

[0028] In step 2 of Example 1, the 2-diethylamino-1-chloroethane hydrochloride used is replaced with equimolar 2-diethylamino-1-chloroethane bisulfate, and other steps are the same as in the examples 1 was the same, and 159.89 g of tiamulin was obtained, with a total yield of 81.0%.

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Abstract

The invention discloses a synthesis method of tiamulin. According to the method, firstly, p-toluene sulfonic acid pleuromutilin ester prepared by pleuromutilin is converted into sulpho-pleuromutilin. After that, sulpho-pleuromutilin reacts with the salt of an ethyl amino ethane derivative to generate tiamulin. The method is simple to operate, low in cost, and environment-friendly. The total recovery of tiamulin is over 80%. Therefore, the method is applied to the industrial production of tiamulin.

Description

technical field [0001] The invention relates to a chemical synthesis method of a veterinary raw material drug, in particular to a method for synthesizing tiamulin. Background technique [0002] The chemical structure of tiamulin is shown below: [0003] [0004] Tiamulin is one of the top ten veterinary antibiotics. Its antibacterial spectrum is similar to that of macrolide antibiotics. It is mainly resistant to Gram-positive bacteria. , Treponema dysentery, etc. have a strong inhibitory effect; the effect on mycoplasma is stronger than that of macrolides. Tiamulin is rapidly absorbed in animals, with high blood concentration, wide distribution in the body, and low residue. It is mainly used to prevent and treat chicken chronic respiratory disease, swine mycoplasma pneumonia, actinomyces pleuropneumonia and treponemal dysentery. When used in low doses, it can promote animal growth and improve feed utilization. The drug has been widely used all over the world and is re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C323/52C07C319/14
Inventor 李宝林李凡石李本浩刘敏刘娟
Owner SHAANXI NORMAL UNIV
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