Chiral Brønsted acid-catalyzed enantioselective three-component Povarov reaction.
The three-component Povarov reaction of aldehydes (2), anilines (3), and benzyl N-vinylcarbamate 4 in the presence of 0.1 equiv of chiral phosphoric acid 5 afforded cis-2,4-disubstituted tetrahydroquinolines (1) in good yields and excellent enantiomeric excesses. The shortest synthesis of torcetrapib reported to date, which features this key three-component reaction, is documented.
Liu
Hua
H
Institut de Chimie des Substances Naturelles, CNRS, 91198 Gif-sur-Yvette Cedex, France.
Dagousset
Guillaume
G
Masson
Géraldine
G
Retailleau
Pascal
P
Zhu
Jieping
J