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

A Pd-catalyzed late-stage aroylation of 4-methyl-1,5-diaryl-1 H-pyrazole-3-carboxylates has been developed via direct Csp2−H bond activation with exclusive site-selectivity, broad substrate scope and good functional group tolerance. [Display omitted] The palladium-catalyzed late-stage aroylation of...

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Bibliographic Details
Published in:Chinese chemical letters 2019-03, Vol.30 (3), p.702-706
Main Authors: Chen, Miao-Miao, Shao, Ling-Yan, Lun, Li-Jun, Wu, Yu-Liang, Fu, Xiao-Pan, Ji, Ya-Fei
Format: Article
Language:English
Subjects:
AroYlation
C[sbnd]H bond activation
Cyclopalladated intermediate
Fully substituted pyrazoles
Late-stage functionalization
Palladium-catalysis
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Summary:A Pd-catalyzed late-stage aroylation of 4-methyl-1,5-diaryl-1 H-pyrazole-3-carboxylates has been developed via direct Csp2−H bond activation with exclusive site-selectivity, broad substrate scope and good functional group tolerance. [Display omitted] The palladium-catalyzed late-stage aroylation of 4-methyl-1,5-diaryl-1H-pyrazole-3-carboxylates has been developed via direct and exclusive mono-Csp2H 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.
ISSN:1001-8417
1878-5964
DOI:10.1016/j.cclet.2018.09.022