Palladium‐Catalyzed C2‐Selective Alkynylation of Indoles with Bromoalkynes

Abstract The Pd(II) catalyzed direct C2 alkynylation of indoles bearing N ‐2‐pyrimidyl or N ‐2‐pyridinyl moiety as a site‐specific directing group was developed with alkynyl halide. A highly regioselective manner can be achieved on a range of indole substrates with excellent functional group tolerance.