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Updated: Aug 14, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
[Design and synthesis of quinoxaline derivatives and their antitumor activities]
Cui-Hua Zhao1, Yi Chen, Jian Ding
1Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Graduate School of the Chinese Academy of Sciences, Shanghai 201203, China.
Aim:
To design and synthesize novel quinoxaline derivatives as antitumor agents.
Methods:
Using 4-chloro-2-nitroaniline as a starting compound, followed by substitution, reductive cyclization, oxidation, and chlorination, to give the key intermediate 2,7-dichloroquinoxaline (7), which reacted with different phenolic compounds to afford quinoxaline derivatives.
Results:
The structures of the target molecules were characterized by elemental analysis, 1H NMR, MS, and IR.
Conclusion:
At concentration of 1 x 10(-4) mol x L(-1), some of the derivatives showed equal antitumor activities to XK469.
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