Pd-Catalyzed Direct Alkynylation of C-H Bonds in Benzenes

Significance

A palladium-catalyzed ortho-alkynylation of aromatic C-H bonds in anilides is described. The resulting silylated aromatic alkynes can be readily deprotected to be subsequently used in Sonogashira-type reactions. This new methodology demonstrates functional group tolerance and affords the respective ortho-alkynylated anilides in good to very good yields.