Non‐Heme‐Type Ruthenium Catalyzed Chemo‐ and Site‐Selective C−H Oxidation

Herein, we developed a Ru(II)(BPGA) complex that could be used to catalyze chemo‐ and site‐selective C−H oxidation. The described ruthenium complex was designed by replacing one pyridyl group on tris(2‐pyridylmethyl)amine with an electron‐donating amide ligand that was critical for promoting this type of reaction. More importantly, higher reactivities and better chemo‐, and site‐selectivities were observed for reactions using the cis‐ruthenium complex rather than the trans‐one. This reaction could be used to convert sterically less hindered methyne and/or methylene C−H bonds of a various organic substrates, including natural products, into valuable alcohol or ketone products. Non‐heme ruthenium catalysis for selective C−H oxidation is described. The newly designed cis‐Ru(BPGA) complex bearing an glycinamide unit promotes oxidation of methyne and methylene C−H bonds selectively with iodosylbenzene as the terminal oxidant. The catalytic system can be applied for a wide range of organic molecules including natural products to provide valuable alcohols or ketones with high chemo‐ and site‐selectivity.