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 

机构地区：[1]State Key Laboratory of Natural Medicines(SKLNM),Department of Medicinal Chemistry,School of Pharmacy,China Pharmaceutical University,Nanjing 210009

出　　处：《CCS Chemistry》2022年第2期616-624,共9页中国化学会会刊（英文）

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).

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

关 键 词：ALKENE 1 1-arylamination PALLADIUM-CATALYZED site-selective nitrogen-containing molecules 

分 类 号：O62[理学—有机化学]