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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 ortho- and meta-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 ortho- and meta-C-H bonds of a phenylethylamine derivative in a streamlined manner.
Li et al. (Thu,) studied this question.