Diastereoselective Access to cis‐1,4‐Disubstitued Tetrahydro‐γ‐carbolines via a [Cp*RhCl2]2‐Catalyzed Formal [3+3]‐Cycloaddition

A [Cp*RhCl2]2‐catalyzed formal [3+3]‐cycloaddition involving sequential ring opening of aziridines initiated by C−H activation and Michael addition has been developed for the construction of cis‐1,4‐disubstitued tetrahydro‐γ‐carbolines. The advantages of this strategy include broad substrate scope, excellent cis‐diastereoselectivities, highly functionalized products, and mild conditions.