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Updated: Jun 22, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis of novel quinoxaline derivatives and its cytotoxic activities
Shinji Tanimori1, Takeshi Nishimura, Mitsunori Kirihata
1Department of Bioscience and Informatics, Graduate School of Life and Environmental Sciences, Osaka Prefecture University, 1-1 Gakuencho, Nakaku, Sakai, Osaka 599-8531, Japan. tanimori@bioinfo.osakafu-u-ac.jp
Abstract:
Substituted dihydroquinozalin-2-ones (1-16) have been synthesized easily by the use of copper-catalyzed coupling method. The reactions of 2-haloanilines with a variety of alpha-amino acids in the presence of copper (I) iodide gave corresponding 3-substituted dihydroquinozalin-2-ones in up to 86% yield. Some new quinoxalin-2-ones (2, 4, 5, 13 and 16) have moderate cytotoxic activity toward HeLaS3 cell lines at 4.9-18.1microM.
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