A series of tyrosine kinase inhibitors which showed antitumor activity were synthesized with 4-chloro-6,7-dimethoxy quinazoline, ethyl 8-bromooctanoate, n-butylbromide and other raw materials, the structuralmodification of N-(3-chloro-4-alkoxyphenyl)quinazolin-4-amine (ARRY-334543) was based on structure-activity relationship of quinazoline derivatives.Structure of these compounds were characterized by NMR and MS , and anti-tumor activity test of the compounds were conducted. Both target compound IX a ~ b posed antitumor activity to MCF-7, BGC-823, A549, DU145 and H1975 cells. Particularly, compound IX a showed the best antitumor activity which 50% concentration inhibition (GI50) is 0.37 μmol/L.