Engaging vinylene carbonate in ruthenium-catalyzed regioselective C-4 methylenation and C-8 formylmethylation of isoquinolinones.

Herein, we disclose the first reports on the utilization of vinylene carbonate as a C1 methylene source in ruthenium-catalyzed additive controlled regioselective C4-methylenation and weak chelation-assisted C8-formylmethylation of isoquinolinones. Adopting vinylene carbonate as both a C2 and C1 synthon is an important highlight of this work. Amide carbonyl acts as the traceless directing group in C8-formylmethylation.