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以醌类作为芳香反应底物,通过有机催化实现恶唑烷酮的对映选择性形式芳基化反应。

Organocatalytic enantioselective formal arylation of azlactones using quinones as the aromatic partner.

作者信息

Li Guofeng, Sun Wangsheng, Li Jingyi, Jia Fengjing, Hong Liang, Wang Rui

机构信息

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China.

出版信息

Chem Commun (Camb). 2015 Jun 30;51(56):11280-2. doi: 10.1039/c5cc03677a.

Abstract

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.

摘要

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。

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