A rhodium-catalysed three-component reaction to access C1-substituted tetrahydroisoquinolines

Abstract

A rhodium-catalyzed three-component reaction of diazo compounds, anilines and C,N-cyclic azomethine imines via trapping of transient ammonium ylides was developed. This reaction provided a simple and convenient approach for the synthesis of pharmaceutically intriguing tetrahydroisoquinoline derivatives in moderate to good yields (36–85%) with good diastereoselectivities (up to 95 : 5 dr) under mild reaction conditions.