An expeditious route to the synthesis of the enantioenriched tetracyclic core of ergot alkaloids via an organocatalytic aldol reaction

Abstract

A concise route to the synthesis of the enantiopure tetracyclic scaffold of ergot alkaloids has been developed via a key organocatalytic aldol reaction using paraformaldehyde as the C1-unit in the presence of thiourea ligand followed by a Pd-catalyzed directed coupling.