N-(3-Chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine, the key intermediate of the anticancer drug Afatinib and Dacomitinib, was synthesized via the addition of 2-bromo-4-fluoro-5-nitrobenzonitrile with 3-chloro-4-fluoroaniline, following cascade amination and condensation-cyclization with formamide catalyzed by cuprous iodide under microwave irradiation. The optimal reaction conditions were investigated. The reaction results showed that 2-bromo-N-(3-chloro-4-fluorophenyl)-4-fluoro-5-nitrobenzimidamide in 93.8% yield was synthesized when 20% cuprous iodide (mole fraction) was used as catalyst, molar ratio of 3-methoxyaniline and 3,3-dimethoxypropionate was 1:1, refluxed for 20 min under microwave irradiation. Subsequently, the target product, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine was obtained with a yield of 84.5% in the presence of 10% cuprous iodide/4-hydroxyl-L-proline (mole fraction), and with n(2-bromo-N-(3-chloro-4-fluorophenyl)-4-fluoro-5-nitrobenzimidamide):n(formamide) of 1:2 at 80℃ for 10 min under microwave irradiation.