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

Abstract

AbstractSteroids are highly prevalent structures in small‐molecule therapeutics, with the level of oxidation being key to their biological activity and physicochemical properties. These C(sp3)‐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(sp3)−H bonds: biocatalysis, metal‐catalysed C−H hydroxylation and organic oxidants, such as dioxiranes and oxaziridines.