Selective Hydroxylation of C(sp3)-H Bonds in Steroids

Steroids are highly prevalent structures in small-molecule therapeutics, with the level of oxidation being key to their biological activity and physicochemical properties. These C(sp(3))-rich tetracycles contain many stereocentres, which are important for creating specific vectors and protein binding orientations. Therefore, the ability to hydroxylate steroids with a high degree of regio-, chemo- and stereoselectivity is essential for researchers working in this field. This review will cover three main methods for the hydroxylation of steroidal C(sp(3))-H bonds: biocatalysis, metal-catalysed C-H hydroxylation and organic oxidants, such as dioxiranes and oxaziridines.

Automated summary

Steroids are common structures in small-molecule therapeutics, and their oxidation level is crucial for their biological activity and physicochemical properties. These tetracyclic structures with multiple stereocenters play a vital role in creating specific vectors and protein binding orientations. Therefore, the ability to selectively hydroxylate steroids is essential for researchers in this field. This review will discuss three main methods for hydroxylation: biocatalysis, metal-catalyzed C-H hydroxylation, and organic oxidants such as dioxiranes and oxaziridines.