Enantioselective Dearomative Arylation of Isoquinolines

The C1-substituted tetrahydroisoquinolines
and 1,2-dihydroisoquinoline
constitute an important group and are interesting structural motifs
found in many natural products and pharmaceuticals. In this context,
a phosphoric-acid-catalyzed enantioselective dearomative arylation
of isoquinolines was realized, providing the chiral dihydroisoquinolines
with indole substituents at the C1-position in good results (up to
>99% yield and 97% ee). The reaction features mild reaction conditions
and operational simplicity, which make it an attractive approach to
the discovery of biologically interesting α-indolisoquinolines.