以1-[二-(4-氟苯)甲基]哌嗪及氯乙酸乙酯为原料,经取代、肼解、环化制得3-[4-二-(4-氟苯)甲基哌嗪]-4-氨基-1,2,4-三氮唑-5-硫酮(5),5和取代芳香醛经缩合反应制得了22个Schiff碱6(a~v),其收率为73-85%。合成的22个目标化合物通过熔点测定和质谱、红外光谱、核磁共振氢谱分析、元素分析对其结构进行确证.经体外抗肿瘤活性测试表明除了化合物6(n,o)外,其余所有化合物均具有较好的活性,在化合物浓度为20ug/m L时,其抑制率高达99%。 3- [4-Bis- (4-fluorophenyl) methyl group was obtained from 1- [bis- (4-fluorophenyl) methyl] piperazine and ethyl chloroacetate by substitution, hydrazinolysis and cyclization 22 Schiff base 6 (a ~ v) were prepared by condensation reaction of 5 and substituted aromatic aldehydes by piperazine-4-amino-1,2,4-triazole-5-thione (5) 73-85%. Twenty-two target compounds were synthesized and their structures were confirmed by melting point analysis, mass spectrum, IR, 1H NMR and elemental analysis.The in vitro anti-tumor activity showed that all the compounds except compound 6 (n, o) Has good activity, the compound concentration of 20ug / m L, the inhibition rate as high as 99%.