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...

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Bibliographic Details
Main Authors: Zahra Haghighijoo (Author), Zahra Rezaei (Author), SamanehTaheri (Author), Meisam Jani (Author), Soghra Khabnadideh (Author)
Format: Book
Published: Shiraz University of Medical Sciences, 2015-09-01T00:00:00Z.
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Summary: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.
Item Description:2423-5652
2423-5652