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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Main Authors: | , , , , |
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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. |
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Item Description: | 2423-5652 2423-5652 |