New preparation method of tiamulin
A tiamulin and reaction technology, which is applied in the field of preparation of medicinal chemicals, can solve the problems of bad odor, restriction on the production of tiamulin, and very high requirements on the production environment
Inactive Publication Date: 2014-05-14
QINGDAO UNIV OF SCI & TECH
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Problems solved by technology
[0004] The biggest problem in this process is the use of 2-diethylaminoethanethiol. 2-Diethylaminoethanethiol has a foul smell. Its application in the world is limited, and it must be checked and used in China. The requirements for the production environment are very high. , which significantly limits the production of tiamulin
Method used
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Experimental program
Comparison scheme
Effect test
Embodiment
[0016] Add 40ml of methanol and 8g of 2-diethylaminoethanol chloride into the reaction flask, then add 5.5g of thiourea to reflux for 3 hours, add 20g of pleuromutilin chloride, and react at 50°C for 3 hours. Extract with ethyl acetate, dry over anhydrous sodium sulfate, evaporate ethyl acetate to obtain tiamulin with a yield of 91.7%.
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Abstract
The invention relates to a new preparation method of tiamulin. The method comprises the following steps of: firstly, adding chloride of 2-diethylaminoethanol in thiourea in a solvent for reacting to obtain a solution system, and then adding chloride of pleuromutilin in the solution system, controlling the reaction temperature and the reaction time, extracting by using the solvent after the reaction is accomplished, dewatering, drying and evaporating the solvent to obtain tiamulin. The reaction yield can be more than 80%. According to the method, 2-diethylaminoethanethiol which has fetid smell is abolished, so that the new preparation method has a good commercial prospect.
Description
technical field [0001] The invention relates to a preparation method of medicinal chemicals, in particular to a new preparation method of tiamulin. Background technique [0002] Tiamulin is fermented by the higher fungus Basidiomycetes Pleurotus mutilus to obtain pleuromutilin, and then chemically synthesized to obtain hydrogenated fumarate. It is a special diterpene antibiotic for livestock and poultry. It was first proposed by Kavangh in Australia in 1951 and extensively studied in the 1960s. It is one of the top ten veterinary antibiotics in the world. The antibacterial spectrum is similar to that of macrolide antibiotics, mainly against Gram-positive bacteria, and has strong inhibitory effects on Staphylococcus aureus, Streptococcus, Mycoplasma, Actinobacillus pleuropneumoniae, Treponema dysentery, etc. The effect on mycoplasma is stronger than that of macrolides. It has weak effect on Gram-negative bacteria, especially intestinal bacteria. Tiamulin is rapidly absorbe...
Claims
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Patent Type & Authority Patents(China)
IPC IPC(8): C07C323/52C07C319/14
Inventor 吴汝林吴广启王凡业
Owner QINGDAO UNIV OF SCI & TECH
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