Site-selective C-H activation and regiospecific annulation using propargylic carbonates

Herein we describe an unprecedented Ru-II-catalyzed site-selective and regiospecific annulation of benzoic acids with propargylic carbonates. The weakly coordinating carboxylic acid moiety outperformed other typically used directing groups in C-H activation, including ketone, nitrile, sulfonamide, amide and strongly coordinating nitrogen heterocycles. This is an important step towards the application of C-H activation reactions in complex (functional) real-world molecules.