Tang Jia-Jun, Zhao Meng-Yang, Lin Ying-Jun, Yang Li-Hua, Xie Long-Yong
College of Chemistry and Bioengineering, Hunan University of Science and Engineering, Yongzhou 425100, China.
Molecules. 2024 Feb 25;29(5):997. doi: 10.3390/molecules29050997.
The incorporation of amide groups into biologically active molecules has been proven to be an efficient strategy for drug design and discovery. In this study, we present a simple and practical method for the synthesis of amide-containing quinazolin-4(3)-ones under transition-metal-free conditions. This is achieved through a carbamoyl-radical-triggered cascade cyclization of N3-alkenyl-tethered quinazolinones. Notably, the carbamoyl radical is generated in situ from the oxidative decarboxylative process of oxamic acids in the presence of (NH)SO.
将酰胺基团引入生物活性分子已被证明是药物设计和发现的一种有效策略。在本研究中,我们提出了一种在无过渡金属条件下合成含酰胺喹唑啉-4(3)-酮的简单实用方法。这是通过N3-烯基连接的喹唑啉酮的氨基甲酰基自由基引发的级联环化实现的。值得注意的是,氨基甲酰基自由基是在(NH)SO存在下由草氨酸的氧化脱羧过程原位产生的。