Citation: Chen Miao-Miao, Shao Ling-Yan, Lun Li-Jun, Wu Yu-Liang, Fu Xiao-Pan, Ji Ya-Fei. Palladium-catalyzed late-stage mono-aroylation of the fully substituted pyrazoles via aromatic C-H bond activation[J]. Chinese Chemical Letters, ;2019, 30(3): 702-706. doi: 10.1016/j.cclet.2018.09.022 shu

Palladium-catalyzed late-stage mono-aroylation of the fully substituted pyrazoles via aromatic C-H bond activation

a.
School of Pharmacy, East China University of Science & Technology, Shanghai 200237, China
b.
Shandong Keyuan Pharmaceutical Co., Ltd., Shandong Shanghe Economic Development Zone, Jinan 251601, China

jyf@ecust.edu.cn

Received Date: 28 August 2018
Revised Date: 22 September 2018
Accepted Date: 29 September 2018
Available Online: 30 March 2018

Figures(9)

The palladium-catalyzed late-stage aroylation of 4-methyl-1, 5-diaryl-1H-pyrazole-3-carboxylates has been developed via direct and exclusive mono-Csp²-H bond activation with broad substrate scope and good functional group tolerance. A dual-core dimeric palladacycle is confirmed by X-ray single crystal crystallography, and probably serves as an active species in the catalytic cycle.
- Palladium-catalysis,
- Late-stage functionalization,
- AroYlation,
- Fully substituted pyrazoles,
- C-H bond activation,
- Cyclopalladated intermediate
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