Access to organoboron derivatives of lead molecules is highly appealing because they can be readily converted to families of derivatives through divergent post-functionalization reactions exploiting the unique reactivity of their C − B bonds. Ideally, such organoboron intermediates can be prepared by borylation of a single C−H bond in available starting materials, thereby allowing the direct derivatisation of existing libraries of bioactive compounds.

Transfer C−H borylation of alkenes bears the potential to unlock a range of attractive transformations for modular synthesis and late-stage derivatization of complex molecules. Based on the mechanistic design, we have recently discovered am efficient a Rh(I)-catalyzed transfer C−H borylation that is applicable to various terminal and internal alkenes (Chem Catal. 2022, 2, 762).