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

Abstract 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. magnified image