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

摘要

A novel rhodium-catalyzed/copper-mediated C2-selective C-H alkynylation of indoles using -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.