Rh(III)-catalyzed ortho-C-H functionalization of N-arylphthalazinones with cyclic enones

Rh(III)-catalyzed direct ortho-C-H bond functionalization of N-arylpthalazinones with cyclic enones has been developed for the synthesis of arylated cyclic ketones. A novel class of 2-(2-(3-oxocycloalkyl)aryl)-2,3-dihydrophthalazine-1,4-dione derivatives were synthesized in good to excellent yields with a broad substrate scope and good functional group tolerance. This reaction represents the first ortho-C-H functionalization of N-arylpthalazinones with cyclic enones by transition metal catalysis.