Simple magnesium catalyst mediated γ-butyrolactams in desymmetrization of meso-aziridines.
The first α-sp(2)-carbon of carbonyl compounds attacked catalytic desymmetrization reaction of aziridines is disclosed. A simple in situ generated magnesium catalyst from 3,3'-bromine-8H-BINOL and dibutylmagnesium was employed. It is interesting that the bromine atom on the chiral ligand plays a key role in introducing a high level of enantioselectivities and high reaction efficiency. Both enantiomers of the ring-opening product could be smoothly obtained by using (R)- and (S)-L7.
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Lanzhou University, Lanzhou, 730000, China. yangdx@lzu.edu.cn.
Dan
D
Li
Department of Chemistry, Tsinghua University, Beijing 100084, China. liudongsheng@tsinghua.edu.cn.
Yijie
Y
Wang
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Lanzhou University, Lanzhou, 730000, China. yangdx@lzu.edu.cn.
Linqing
L
Wang
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Lanzhou University, Lanzhou, 730000, China. yangdx@lzu.edu.cn.
Jie
J
Wang
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Lanzhou University, Lanzhou, 730000, China. yangdx@lzu.edu.cn.
Pengxin
P
Wang
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Lanzhou University, Lanzhou, 730000, China. yangdx@lzu.edu.cn.
Kezhou
K
Wang
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Lanzhou University, Lanzhou, 730000, China. yangdx@lzu.edu.cn.
Li
L
Lin
Department of Chemistry, Tsinghua University, Beijing 100084, China. liudongsheng@tsinghua.edu.cn.
Dongsheng
D
Liu
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Jiangxx5@mail. sysu.edu.cn.
Xianxing
X
Jiang
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Lanzhou University, Lanzhou, 730000, China. yangdx@lzu.edu.cn.
Dongxu
D
Yang