Palladium-catalyzed intermolecular amination of unactivated C(sp3)-H bonds via a cleavable directing group.
Palladium-catalyzed intermolecular amination of unactivated C(sp3)-H bonds was developed. Using NFSI as both the amino source and the oxidant, this protocol operates under mild conditions with excellent terminal selectivity and a broad substrate scope. Moreover, the directing group can be easily removed to produce 1,2-amino alcohols.
Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China. liupengwhu@whu.edu.cn.
Lianwen
L
Jin
Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China. liupengwhu@whu.edu.cn.
Xiaoli
X
Zeng
Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China. liupengwhu@whu.edu.cn.
Siyang
S
Li
Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China. liupengwhu@whu.edu.cn.
Xuechuan
X
Hong
Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China. liupengwhu@whu.edu.cn.
Guofu
G
Qiu
Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China. liupengwhu@whu.edu.cn.
Peng
http://orcid.org/0000-0002-5164-088X
P
Liu