Room temperature, metal-catalyzed oxidative acylation of electron-deficient heteroarenes with alkynes, its mechanism and application studies

Herein, we report an original one-step, simple, room-temperature, regioselective Minisci reaction for the acylation of electron-deficient heteroarenes with alkynes. The method has broad functional group compatibility and gives exclusively monoacylated products in good to excellent yields. The mechanistic pathway was analyzed based on a series of experiments confirming the involvement of a radical pathway. The 18O-labeling experiment suggested that water is a source of oxygen in the acylated product, and head space GC–MS experiment shows the C–C cleavage occurs via release as CO2.