Jingyi Zhan, Xinni Tang, Xuyao Zhong, Wenjie Hu, Lei Yang
ABSTRACT Herein, we report that directed C–H silylation of indoles and a pyrrole derivative with hydrosilanes in aqueous media under air was achieved under iridium catalysis. This reaction enables the introduction of a silyl group at the C2 position of a wide range of indoles. The protocol represents the first example of a transition metal‐catalyzed C–H silylation in aqueous media as a sustainable solvent for C–H functionalization of indoles.