Synthesis of Indolo[2,1‑a]isoquinolines by Nickel-Catalyzed Mizoroki–Heck/Amination Cascade Reaction

An efficient Mizoroki–Heck/amination cascade reaction of o-dihaloarenes with cyclic imines was realized by combining nickel and a sterically bulky N-heterocyclic carbene ligand. This protocol provides access to a variety of indole­[2,1-a]­isoquinolines from readily available starting materials. This cascade approach could be applied to produce straightforward synthesis of the natural product cryptowoline.