Synthesis Of Febuxostat

Objective:Choicing the synthesis route of Febuxostat.Makingpost-processing operations much more simple and suitable for industrialproduction. Reducing environmental pollution and productioncost.Improving the yield.Methods: With4-hydroxy-benzaldehyde as starting material, Thenwith hydroxylamine hydrochloride formic acid and sodium formate couldoccur reductive amination reaction to get hydroxyl benzene benzylcyanide.Then Product with thioacetamide reaction could get4-hydroxythiobenzamide, Next Cyclization reaction, Duff reaction, reductiveamination, Etherification reaction.The last step was alkaline hydrolysis,finally prepared antipodagric febuxostat.Results:The structure of the target compounds were confirmed by IR,1HNMR,13CNMR,MS.Total yield has been increased15%than Japanesepatent.Sample witch from this process has been used in clinnical research.Conclusion:synthesis route and method is reasonable.suitable forindustrial production.