Four compounds of 4-(3′-Chlorophenylamino)-6-methoxy quinazoline compounds, including 7-(3-(4-nitrophenoxy)propoxy)-N-(3′-chlorophenyl)-6-methoxyquinazolin-4-amine,7-(3-(3-nitrophenoxy)propoxy)-N-(3′-chlorophenyl)-6-methoxyquinazolin-4-amine,4-(3-(4-(3′-chlorophenylamino)-6-methoxyquinazolin-7-yloxy)propoxy)-3-methoxybenzaldehyde、3-(3-(4-(3′-chlorophenylamino)-6-methoxyquinazolin-7-yloxy)propoxy)-4-methoxyb- enzaldehyde, were synthesized from N′-(5-(3-chloropropoxy)-2-cyano-4-methoxyphenyl)-N, N-dimethylformamidine by cyclization，etheration, in the yield of 51.3%、60.3%、85.4% and 79.4% respectively. Their structures were characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis. Preliminary bioassay indicated that some compounds possess antitumor activity to Bcap-37 cells in vitro by MTT method. The antiproliferation activity of compound Ιa to Bcap-37cells at the concentration of 10 μmol?L-1 was 83.4%.