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Updated: Mar 10, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Divergent Synthesis of Polymethoxylated 4-Aryl-2-quinolones
Tsukasa Murayama1, Masatoshi Shibuya1, Yoshihiko Yamamoto1
1Department of Basic Medicinal Sciences, Graduate School of Pharmaceutical Sciences, Nagoya University , Chikusa, Nagoya 464-8601, Japan.
Abstract:
Polymethoxylated 4-aryl-2-quinolones were synthesized from the corresponding (o-aminophenyl)propiolates via Cu-catalyzed hydroarylation and subsequent deprotection/lactam formation. Selective iodination of the C3 position of the product followed by coupling reactions of the resulting 3-iodinated 4-aryl-2-quinolone afforded 3-substituted-4-aryl-2-quinolones. Moreover, the N-benzyl protecting group was successfully replaced with other polyoxygenated benzyl groups.
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