Study on the Preparation of Epoxide Intermediate of Tulathromycin
Tulathromycin is a novel macrolide semisynthetic antibiotic for animals,which has been approved for use in the prevention and treatment of porcine respiratory disease in China.However,ketonic and epoxidized production of tulathromycin has some disadvantages such as low yield,a lot of side effects and impurities,difficult purification,and unconducive industrial production.In this paper,demethylazithromycin was used as raw material.The 2-hydroxyl group and 6-amino group protected by trifluoroacetic anhydride were used to produce the double-protected demethylazithromycin.The carbonyl group synthesized from 4-hydroxyl group using Swern-Oxidation was then epoxidized by sulfur Ylide to produce the intermediate epoxide of tulathromycin.Tulathromycin is synthesize by directly Swern-Oxidation,which does not need to be purified after double-protected pr process.This method has many advantages such as continuous,simple and reliable process,high yield,inexpensive and convenient raw materials,green,safe and environmentally friendly conditions,few side effects and suitable for industrial production.
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