Selective Hydroxylation of C(sp3 )-H Bonds in Steroids
Hossay Abas1, Peter Blencowe1, Joanna L Brookfield1
1Cancer Research Horizons, Babraham Research Campus, Cambridge, CB22 3AT, UK.
Abstract:
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(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.
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