Study On The Process Of Febuxostat

Febuxostat is new anti-gout agents devolopped by Takeda Pharmaceutical Company Limited?It is a selective xanthine oxudase inhiitor?This medicine was listed in February 2009 in USA,and in February 2013 in China.Febuxostat was the only one approved medicine for the ability to decrease serum urate to treat gout after1964.The main research of this paper is to refine and optimize the process based on the literature route,so as to develop a process suitable for industrial production.The specific content: Taking 4-Hydroxy-thiobenzimidic acid as the starting material,after cyclization,formylation,addition elimination,dehydration,substitution and hydrolysis,finally getting Febuxostat.This topic mainly optimizes the solvent of cyclization,the solvent of the methylation,the order of synthesising the cyanide and the isobutyl group,and studies the ratio and temperature of each step in detail.The process is cheap and the total yield of five steps reaches 61%,especially for simple operation,it is especially for industrial production.