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The synthesis of N, N'-l,4-bis( 4-methylphenyl) sulfonyl-liomopiperzine was studied with N-methylpyirolidone as solvent, NaOH as acid binding agent and 1,3-dichloropropane as cyclization reagent. The effects of reaction time, the molar ratio of reactants, reaction temperature, and the amount of sodium hydroxide on the yield of N,N'-1,4-bis(4-methylphenyl) sulfonyl-homopiperzine were investigated. The result showed that the order of effects was as follows: alkali amount > temperature > molar ratio of reactants. The yield could reach 81.93% under the conditions of 5 mmol N,N-bis(toluenesulfonyl)-1,2-ethylenediamine, 7.969 mmol 1,3-dichloropropane and 0.548 g sodium hydroxide,123 °C react 40 min. The kinetic analysis of the synthesis of N,N-1,4-bis(4-methylphenyl) sulfonyl-homopiperzine was carried out at 115, 125, 135 °C according to the second-order reaction mechanism, and the activation energy of this reaction was 76. 233 kJ/mol. [ABSTRACT FROM AUTHOR]