Synthesis of 3,4‐Dihydroisoquinolines by a C(sp³)H Activation/Electrocyclization Strategy: Total Synthesis of Coralydine

Abstract

Thanks to CH activation: 3-Aryl-3,4-dihydroisoquinolines (2) are synthesized from bromobenzenes (1) by a sequence comprising a C(sp3)H activation, a Curtius rearrangement, and a tandem electrocyclic ring-opening/6π electrocyclization. This method is applied to the synthesis of various isoquinoline-containing molecules, including the tetrahydroprotoberberine alkaloid coralydine.