Asymmetric Organocatalytic Synthesis of Bisindoles – Scope and Derivatizations

Starting from 3‐vinylindoles and glyoxolate imines, we created a library of diverse 4,6‐bis(1 H ‐indole‐3‐yl)piperidine 2‐carboxylates by using 10 mol‐% of a chiral phosphoric acid. Utilising electron‐withdrawing groups on the starting material during the reaction led to the formation of Povarov‐type structures, which extended the previous library of molecules. Furthermore, we could demonstrate that consecutive reactions like reductions, cross coupling reactions or click reactions on bisindoles are feasible.