The invention relates to a synthesis method of a drug for treating leukemia. The synthesis method comprises that 1, a compound 3-methyl-3-oxetanemethanol and sodium metal undergo a reaction to produce 3-sodium methoxide-3-methyl-3-oxetane, 2, 4-amino-3-nitrochlorobenzene is added into the product obtained by the step 1 so that reddish-orange solids (A1) are obtained, a compound 8-benzyloxyquinolin-2-chlorine and A1 undergo a reaction to produce orange solids A2, 3, the compounds A2, 13g of palladium / carbon and formic acid undergo a reaction, formamidine acetate is added into the reaction product, and the mixture is subjected to reflux and drying so that white-like (or yellow) solids A3 are obtained, and 4, the compounds A3 and benzenesulfonyl chloride undergo a reaction, the product is dried to form maize-yellow solids A4, BINAP, A4, tert-butyl piperidin-4-yl-carbamate and potassium carbonate undergo a reaction, the reaction product is dried to form A5, and the A5 is refined through the step 5 so that a pure product is obtained. In the steps 1 and 2, a one-pot method is used.