Direct Integration of Phthalazinone and Succinimide Scaffolds via Rh(III)‐Catalyzed C−H Functionalization

The development of new methods for the direct synthesis of bioactive molecules is a pivotal topic in organic and medicinal chemistry. Herein, we describe the rhodium(III)‐catalyzed C−H functionalization of N‐aryl phthalazinones with maleimides. The complete site‐selectivity and broad functional group tolerance are observed. Notably, this protocol allows the direct integration of phthalazinones and succinimides, which are vital motifs found in bioactive natural products and pharmaceuticals. Integration of Bioactive Scaffolds: The rhodium(III)‐catalyzed C−H functionalization of N‐aryl phthalazinones with maleimides is described for the direct integration of phthalazinones and succinimides, which are vital motifs found in bioactive natural products and pharmaceuticals.