One-Step Synthesis of THIQ via a Catellani Strategy

Tetrahydroisoquinoline (THIQ), an important heterocyclic scaffold, is prevalent in bioactive natural products and therapeutic agents. Growing efforts have been devoted to the efficient preparation of this valuable scaffold. However, current strategies usually rely on specially functionalized complex substrates. Recently, our group developed a modular one-step three-component synthesis of THIQs via a Catellani/Heck/aza-Michael cascade, using simple aryl iodides, aziridines, and olefins as the starting materials.