State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, P. R. China.
Org Lett. 2021 Apr 16;23(8):2846-2852. doi: 10.1021/acs.orglett.1c00226. Epub 2021 Mar 25.
Here we describe an unprecedented metal-free C(sp)-H aroylation of amines via visible-light photoredox catalysis, which provides a straightforward route for the construction of a useful α-amino aryl ketone skeleton. Additionally, a number of selected products exhibit good biological activity for protecting PC12 cell damage, which shows that this skeleton has the potential to become a new neuroprotective agent. Finally, a series of mechanism experiments indicate that this transformation undergoes a photoredox catalytic radical-radical cross-coupling pathway.
在这里，我们通过可见光光氧化还原催化描述了一种前所未有的胺的 C(sp)-H 芳基化反应，为构建有用的α-氨基芳基酮骨架提供了一种直接途径。此外，一些选定的产物对保护 PC12 细胞损伤表现出良好的生物活性，这表明该骨架有可能成为一种新的神经保护剂。最后，一系列的机理实验表明，这种转化经历了光氧化还原催化的自由基-自由基交叉偶联途径。
