Organocatalytic and highly enantioselective direct alpha-amination of aromatic ketones.
The first highly enantioselective direct alpha-amination of aryl ketones was reported to be catalyzed by organic primary amines derived from cinchona alkaloids. Excellent enantioselectivities (88-99% ee) have been achieved for a broad spectrum of aryl ketones. The presence of 4 A molecular sieves was of great assistance for the high conversions and enantiocontrol.
Liu
Tian-Yu
TY
Key Laboratory of Drug-Targeting of Education Ministry and Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, and State Key Laboratory of Biotherapy, West China Hospital, Chengdu, China.
Cui
Hai-Lei
HL
Zhang
Yan
Y
Jiang
Kun
K
Du
Wei
W
He
Zhao-Quan
ZQ
Chen
Ying-Chun
YC
D000586:Amination; D000588:Amines / Q000737:chemistry*; D002384:Catalysis; D006841:Hydrocarbons, Aromatic / Q000737:chemistry*; D007659:Ketones / Q000737:chemistry*; D009930:Organic Chemicals / Q000138:chemical synthesis / Q000737:chemistry; D013237:Stereoisomerism
D000588:Amines; D006841:Hydrocarbons, Aromatic; D007659:Ketones; D009930:Organic Chemicals