Sulfide‐Catalyzed Trifluoromethylthiolation‐Cyclization of Tryptamine Derivatives

Trippy triptamines: An SCF3 group can be incorporated in tryptamine derivatives via a sulfide-catalyzed cascade trifluoromethylthiolation-cyclization. A series of C(3)-CF3S pyrrolidinoindolines were obtained in moderate to good yields under mild conditions. Furthermore, some enantioselectivity was observed when using chiral sulfide thiocineole as a catalyst.

A catalytic method for the incorporation of an SCF3 group to tryptamine derivatives was developed via a sulfide-catalyzed cascade trifluoromethylthiolation-cyclization. A series of C(3)-CF3S pyrrolidinoindolines were obtained in moderate to good yields under mild conditions. Furthermore, some enantioselectivity was observed when using chiral sulfide thiocineole as a catalyst.