1.
Org Lett
; 21(12): 4831-4836, 2019 06 21.
Artigo
em Inglês
| MEDLINE
| ID: mdl-31180222
RESUMO
An atroposelective Friedländer heteroannulation reaction of 2-aminoaryl ketones with α-methylene carbonyl derivatives has been developed for the first time with chiral phosphoric acid as an efficient organocatalyst. The desired enantioenriched axially chiral polysubstituted 4-arylquinoline architectures were prepared with good to high yields and enantioselectivities (up to 94% yield and up to 97% ee). Furthermore, the products can be readily derivatized to afford an array of new quinoline-containing heteroatropisomers, which hold great potential in asymmetric catalysis and drug discovery.