Site-Selective Palladium-Catalyzed 1,1-Arylamination of Terminal Alkenes

作     者：Chunhua Han Libo Cai Dongquan Zhang Rui Pan Qiuyu Li Aijun Lin Hequan Yao 

作者机构：State Key Laboratory of Natural Medicines(SKLNM)Department of Medicinal ChemistrySchool of PharmacyChina Pharmaceutical UniversityNanjing 210009 

出 版 物：《CCS Chemistry》 (中国化学会会刊（英文）)

年 卷 期：2022年第4卷第2期

页      面：616-624页

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

基　　金：supported by the National Science Foundation of China(no.22071267) the National Science and Technology Major Project“Key New Drug Creation and Manufacturing Program,”China(no.2020ZX09201015) the Innovation Team of the“DoubleFirst Class Initiative”(nos.CPU2018GY04 and CPU2018GY35) the Foundation of the Open Project of State Key Laboratory of Natural Medicines(no.SKLNMZZ202023) 

主　　题：alkene 1,1-arylamination palladium-catalyzed site-selective nitrogen-containing molecules 

摘      要：Many of the commonly used pharmaceuticals and biologically active natural products are nitrogencontaining ***,the transitionmetal-catalyzed or the radical-mediated 1,2-carboamination of alkenes has been well explored to access amine ***,synthetic strategies toward the 1,1-carboamination of alkenes are severely ***,we describe a method to achieve the 1,1-arylamination using readily available building blocks enabled by palladium *** sequential three step-Heck arylation,metal migration,followed by aza-1,6-Micheal addition process exhibits excellent chemo-and *** showcase the potential as a method for diversity-oriented drug discovery,the modification of numerous structurally complex bioactive molecules was also successfully performed.