Rhodium-Catalyzed Direct C-H Phosphorylation of (Hetero)arenes Suitable for Late-Stage Functionalization

Efficient rhodium-catalyzed direct C-H phosphorylation of (hetero)arenes was developed. Various directing groups and a wide range of substrates, including heterocycles, can be utilized in this C-H phosphorylation process, allowing for the rapid installation of the phosphonate group into medicinally and biologically important privileged scaffolds. The efficient and straightforward method could serve as a new tool to streamline late-stage C-H functionalization for preparing aryl phosphonates, which are important structural motif in synthetic and medicinal chemistry.