A rapid and convenient method for synthesis of anilinoquinazoline: an improved synthesis of erlotinib derivatives

4-anilinoquinazolines have been widely studied as anticancer agents. despite the widespread use of this class of compounds, the reported syntheses of 4-anilinoquinazolines require multistep and lowyielding reaction pathways. in this study, a novel strategy to prepare 4-anilinoquinazoline derivatives based on the cyclization of anthranilic acid is described. by using dichloroanthranilic acid, the quinazoline ring was etherified in order to mimic the erlotinib structure as a tyrosine kinase inhibitor. the new compounds contain different substitutions at the meta-positions of the quinazoline ring instead of the ortho- positions of erlotinib. ten new 4-anilinoquinazoline derivatives were sysnthesized (21-30) in only 4 steps with desirable yields.