Selective Synthesis of Alkynylated Isoquinolines and Biisoquinolines via RhIII Catalyzed C–H Activation/1,3-Diyne Strategy

Described herein is a convenient and highly selective synthesis of alkynylated isoquinolines and biisoquinolines from various aryl ketone O-pivaloyloxime derivatives and 1,3-diynes via rhodium-catalyzed C–H bond activation. In this transformations, alkynylated isoquinolines, 3,4′- and 3,3′-biisoquinolines could be obtained respectively through changing the reaction conditions. Mechanistic investigation revealed that the C–H activation of aryl ketone O-pivaloyloxime was the key step to this reaction.