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 

机构地区：[1]School of Pharmacy, East China University of Science & Technology [2]Shandong Keyuan Pharmaceutical Co., Ltd., Shandong Shanghe Economic Development Zone

出　　处：《Chinese Chemical Letters》2019年第3期702-706,共5页中国化学快报（英文版）

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

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.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.

关 键 词：Palladium-catalysis Late-stage FUNCTIONALIZATION AroYlation Fully SUBSTITUTED PYRAZOLES C-H bond activation Cyclopalladated intermediate 

分 类 号：O6[理学—化学]