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234. Org. Lett. 2021, 23, 2846–2852

date:2021-05-12

Metal-Free α-C(sp3)–H Aroylation of Amines via a Photoredox Catalytic Radical–Radical Cross-Coupling Process

Guo-Qiang Xu*, Teng-Fei Xiao, Guo-Xuan Feng, Chen Liu, Baoxin Zhang, and Peng-Fei Xu*

https://pubs.acs.org/doi/10.1021/acs.orglett.1c00226












Abstract

Here we describe an unprecedented metal-free C(sp3)–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.