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

作     者：Miao-Miao Chen Ling-Yan Shao Li-Jun Lun Yu-Liang Wu Xiao-Pan Fu Ya-Fei Ji 

作者机构：School of Pharmacy East China University of Science & Technology Shandong Keyuan Pharmaceutical Co. Ltd. Shandong Shanghe Economic Development Zone 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2019年第30卷第3期

页      面：702-706页

核心收录：

学科分类：07[理学] 0703[理学-化学] 

基　　金：the National Natural Science Foundation of China(Nos. 21476074 and 21676088)for financial support 

主　　题：Palladium-catalysis Late-stage functionalization AroYlation Fully substituted pyrazoles C-H bond activation Cyclopalladated intermediate 

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^2-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.