Transformable Sulfoximine Assisted One-Pot Double Annulation of Vinylic C–H Bonds with Unactivated Alkynes

The methylphenyl sulfoximine (MPS)
directing group (DG) successfully
promotes the one-pot double annulation of acrylic acids with alkynes
under Ru catalysis, which is unprecedented. Diverse arrays of pyrido-fused-isoquinolinone
skeletons are fabricated from acrylamides, creating two C–C
and two C–N bonds in a single operation. The unsymmetrical
annulation with two distinct alkynes is presented. The recovery of
methylphenyl sulfoxide, a precursor of MPS, validates the synthetic
adaptability of transformable-DG (TfDG) in C–H activation.