Demonstrated
herein is an unprecedented thioamide-directed cobalt
(Co)-catalyzed umpolung annulation of sulfoximines enabled aryl thioamide
with ynamide for the synthesis of highly substituted 2-amidoindenones.
The cyclization is regioselective, making β-C–C and α-C–CO
bonds. The transformation is even successful on a gram scale, exhibiting
broad scope with labile functional group tolerance and constructing
43 unusual 2-amidoindenones of structural diversity. Control experiments
and mechanistic investigation validate the regioselectivity outcome
in this transformation.