Abstract:Febuxostat was prepared by 4-hydroxybenzonitrile via sulfuration, cyclization, formylation, cyanation, alkylation and hydrolysis. The cyanation and alkylation reaction were performed by one-pot reaction in improved process, and the key factors, such as concentration of hydrochloric acid, reaction time, temperature, the ratio of methane sulfonic acid to trifluoroacetic acid, were explored. The improved process was convenient, mild reaction condition, and the total yield was as high as 65.7%.