摘要/Abstract

通过在水相中可见光下2-氨基苯甲酰胺与苄醇氧化制备喹唑啉酮的环化反应, 应用廉价易得、操作简单的单质碘作为光催化剂, 在室温下反应获得较好收率的产物. 目标产物的最高产率可达92%, 为喹唑啉酮类化合物的合成提供了一种绿色经济的方法. 运用此策略合成的N-(2-氟-5-甲基苯基)-6-(2,2,2-三氟乙氧基)蝶啶-4-胺对肿瘤细胞具有明显的抑制活性.
关键词: 可见光, 单质碘, 喹唑啉酮, 氧化剂, 催化剂
A novel visible-light-introduced reaction for the construction of quinazolinone derivatives via radical cyclization of 2-aminobenzamides with benzyl alochols under water phase has been developed. The reaction has been achieved in high yield under mild conditions by using I₂ as photocatalyst, which is cheap, available and easy to handle. A variety of quinazolinones were obtained in yields up to 92%. It might provide a promising protocol for the synthesis of quinazolinone derivatives. Its application was performed by the synthesis of N-(2-fluoro-5-methylphenyl)-6-(2,2,2-trifluoroethoxy)pteridin-4-amine, which displayed significant inhibitory activity.
Key words: visible light, Iodine, quinazolinone, oxidant, catalyst


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