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

被引:0
作者
Miao-Miao Chen [1 ]
Ling-Yan Shao [1 ]
Li-Jun Lun [2 ]
Yu-Liang Wu [2 ]
Xiao-Pan Fu [1 ]
Ya-Fei Ji [1 ]
机构
[1] School of Pharmacy, East China University of Science & Technology
[2] Shandong Keyuan Pharmaceutical Co., Ltd., Shandong Shanghe Economic Development Zone
基金
中国国家自然科学基金;
关键词
Palladium-catalysis; Late-stage functionalization; AroYlation; Fully substituted pyrazoles; C-H bond activation; Cyclopalladated intermediate;
D O I
暂无
中图分类号
O621.251 [];
学科分类号
070303 ; 081704 ;
摘要
The palladium-catalyzed late-stage aroylation of 4-methyl-1,5-diaryl-lH-pyrazole-3-carboxylates has been developed via direct and exclusive mono-Csp;-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.
引用
收藏
页码:702 / 706
页数:5
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