Abstract A novel 4-anilinoquinazoline dimer linked by a carbon–carbon bond in the C-7 position was synthesized via a one step Suzuki cross-coupling reaction. All structures of new compounds were characterized by 1 H NMR, 13 C NMR, and HRMS. The inhibition rate of the synthetic 4-anilinoquinazoline dimer 8 against epidermal growth factor receptor-tyrosine kinase enzymes (EGFR) in vitro was 44.4% at the concentration of 5.5 μmol/L.