Difluoromethylthioester compounds are yet another important kind of organofluorine compound and are reported here for the first time. They can be efficiently synthesized from various aldehydes. The synthetic method features mild reaction conditions, good tolerance of functional groups, broad substrate scope, and importantly, no metal is involved in the reaction. The approach has the potential to become an important tool for the late-stage functionalization of advanced synthetic intermediates, and should have many applications in medicinal chemistry.

The utilization of the transient directing strategy into the direct oxidative dehydrogenative arylation of aldehydes with arenes was reported for the first time. Featured by mild reaction conditions, good functional group compatibility, and great regioselectivity, the method should find broad applications in new medicine and material development and discovery processes.

A direct and efficient approach to the synthesis of monofluoromethylthioesters from aldehydes has been developed. The synthetic method features mild reaction conditions, good tolerance of functional groups, a broad substrate scope, and especially no metal involved in the reaction. The approach has the potential to be an important tool for the late‐stage functionalization of advanced synthetic intermediates, and may find many applications in medicinal chemistry.magnified image