Efficient N -arylation of 4-chloroquinazolines en route to novel 4-anilinoquinazolines as potential anticancer agents.

Microwave-mediated N -arylation of 4-chloroquinazolines in THF/H 2 O rapidly and efficiently afforded a library of novel 6-halo-2-phenyl-substituted 4-anilinoquinazolines. The methodology was compatible with numerous ortho- , meta- , and para -substituted N -methylanilines as well as substituted anilines and furnished the corresponding 4-anilinoquinazolines in good yields. Preliminary screening of the synthesized compounds against tumor cells (HCT-116 and T98G) showed promising antiproliferative properties.