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.