Li Guofeng, Sun Wangsheng, Li Jingyi, Jia Fengjing, Hong Liang, Wang Rui
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China.
Chem Commun (Camb). 2015 Jun 30;51(56):11280-2. doi: 10.1039/c5cc03677a.
A new method for the catalytic enantioselective formal arylation of azlactones using quinones as the aromatic partner was developed for the first time. Under mild conditions, the domino Michael/aromatization/cyclization reaction worked well to afford the corresponding products in moderate to high yields with excellent enantioselectivities, some of which have promising cytotoxicity against cancer cells and antibacterial activities.
首次开发了一种以醌类作为芳基化试剂,用于催化乙内酰脲的对映选择性形式芳基化的新方法。在温和条件下,多米诺Michael/芳构化/环化反应顺利进行,以中等到高的产率和优异的对映选择性得到相应产物,其中一些产物对癌细胞具有有前景的细胞毒性和抗菌活性。