Rhodium‐Catalyzed/Copper‐Mediated Selective C2 Alkynylation of Indoles and C1 Alkynylation of Carbazoles with γ‐Substituted tert‐Propargyl Alcohols

Abstract A novel rhodium‐catalyzed/copper‐mediated C2‐selective C−H alkynylation of indoles using γ ‐substituted tert ‐propargyl alcohols as the alkynylating reagent and a removable 6‐methylpyridin‐2‐yl as the directing group has been developed, which provides a viable pathway for direct C2‐selective alkynylation of indoles. Moreover, this strategy could be extended to the C−H alkynylation of carbazoles at the C1 position.