Palladium-catalyzed oxidative C-H activation/annulation of N -alkylanilines with bromoalkynes: access to functionalized 3-bromoindoles.

A straightforward approach to the synthesis of 3-bromoindoles via palladium-catalyzed oxidative C-H activation/annulation of N -alkylanilines with bromoalkynes has been described. This protocol features high atom economy, excellent chemo- and regioselectivities, and good functional group tolerance. Moreover, the resultant 3-bromoindoles can be transformed to various functionalized indole derivatives, which demonstrates the practicability of this method in organic synthesis.