The synthetic technique of TG101209 for treating bone marrow hyperplastic tumor was studied.2-Chloro-4-amino-5-methyl-pyrimidine(B) was prepared by chlorination and substitution reaction of 2,4-dihydroxy-5-methylpyrimidinnel, phosphorus oxychloride and ammonium hydroxide.B reacted with 3-bromo-N-t-butyl benzenesulfonic amide (C) to give 3-[(2-chloro-5-methyl-4-pyrimidinyl) amino]-N-t-butylbenzenesulfonic amide (D) by Buchwald coupling reaction.D reacted with CH3OH-HCl in the methanol to afford 3- [(2-chloro-5-methyl-4-pyrimidinyl) amino]-N-tert-butylbenzenesuiphonamide hydrochloride (E). (N-tert-butyl-3-(5-methyl-2-[4-(4-methyl-1-piperazinyl)-phenylamino]-pyrimidine-4-ylamino)-benzenesulfonamide)(TG101209) was synthesized by nucleophilic substitution reaction of the intermediate (E) and 1-methyl-4-(4-aminophenyl)piperidine (G). The overall yield was 30.9%. HPLC purity was 99.7%. (N-tert-butyl-3-(5-methyl-2-[4-(4-methyl-1-piperazinyl)-phenylamino]-pyrimidin-4-ylamino)-benzenesulfonamide)(TG101209) was synthesized by nucleophilic substitution reaction of the intermediate (E) and (G).The overall yield was 30.9%.HPLC purity is 99.7%.