Pd(ii)-catalyzed remote regiodivergent - and -C-H functionalizations of phenylethylamines.

Site selectivity control is of vital importance in the direct functionalization of inert C-H bonds. Reported here is a novel example of remote regiodivergent - and -C-H bond functionalizations of phenylethylamine derivatives by using a novel 2-cyanobenzoyl group as the original directing functionality, where the regioselectivity was adjusted by a methylation. The potential of the method was exemplified by sequential functionalizations of both - and -C-H bonds of a phenylethylamine derivative in a streamlined manner.