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Cobalt(II)-Catalyzed Selective C2–H Heck Reaction of Native (N–H) Indoles Enabled by Salicylaldehyde Ligand

Jia-Wei Li,Shuai Shi,Xiao-Hong Chen,Mao-Gui Huang,Yong-Liang Ban,Hui Zhang,Yue-Jin Liu

Direct functionalization of native (N–H) indoles via C–H activation remains a challenge. Herein, we report a salicylaldehyde-promoted cobalt-catalyzed selective C2–H Heck reaction of native (N–H) indoles with both active and unactivated olefins in the presence of free N–H bonds. A series of structurally diverse C2-alkenylated native (N–H) indoles including natural product and drug derivatives were prepared directly and effectively without additional preprotection and deprotection procedures.