Chen Liang, Huang Rong, Kong Ling-Bin, Lin Jun, Yan Sheng-Jiao
Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, P. R. China.
ACS Omega. 2018 Jan 26;3(1):1126-1136. doi: 10.1021/acsomega.7b01856. eCollection 2018 Jan 31.
A one-step protocol without transition-metal catalysts with simple post-treatment for the synthesis of 1,3-diazaheterocycle-fused [1,2-]quinoline derivatives via the cascade reaction of 2-fluorobenzaldehyde () and heterocyclic ketene aminals () was developed. In the one-step cascade reaction, C=C and C-N bonds were constructed, and the targeted compound can be efficiently obtained by filtering without column chromatography. This protocol describes a valuable route to concisely and feasibly obtain 1,3-diazaheterocycle-fused [1,2-]quinoline derivatives. The synthetic methodology is particularly attractive because of the following features: low-cost solvent, mild temperature, atom economy, high yield, and potential biological activity of the product.
开发了一种无需过渡金属催化剂且后处理简单的一步法，通过2-氟苯甲醛（）与杂环烯酮缩胺（）的串联反应合成1,3-二氮杂环稠合[1,2-]喹啉衍生物。在一步串联反应中，构建了C=C键和C-N键，通过过滤无需柱色谱即可高效获得目标化合物。该方法描述了一种简洁可行地获得1,3-二氮杂环稠合[1,2-]喹啉衍生物的有价值途径。该合成方法特别具有吸引力，原因如下：低成本溶剂、温和温度、原子经济性、高收率以及产物潜在的生物活性。
