Ru59063 is clinically used to treat prostate cancer and has a good effect. In this study, 4-amino-2- ( trifluoromethyl ) benzonitrile was used as raw material to prepare thioisocyanate by thiophosgene, and then [3+2] cycloaddition reaction with 2-aminoisobutyrate methyl ester hydrochloride was carried out to construct thiohydantoin ring, and then Ullmann C-N coupling reaction with halogenated ether was carried out. Finally, a total of 4 steps of hydroxyl deprotection were carried out to obtain Ru59063, with an overall yield of 61.5 %. Compared with the traditional method, the yield of this method is increased by more than 40 %, and no cyanide is used, It is more convenient and safer to prepare Ru59063.