文献类型：期刊文献

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

作者：Chen, Miao-Miao[1];Shao, Ling-Yan[1];Lun, Li Jun[2];Wu, Yu-Liang[2];Fu, Xiao-Pan[1];Ji, Ya-Fei[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China;[2]Shandong Keyuan Pharmaceut Co Ltd, Shandong Shanghe Econ Dev Zone, Jinan 251601, Shandong, Peoples R China

年份：2019

卷号：30

期号：3

起止页码：702

外文期刊名：CHINESE CHEMICAL LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000462106900038)，CCR-EXPANDED(收录号:WOS:000462106900038)】；

基金：We gratefully thank the National Natural Science Foundation of China (Nos. 21476074 and 21676088) for financial support.

语种：英文

外文关键词：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-1H-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. (C) 2018 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.