The widespread inclusion of heterocyclic moieties in popular agrochemicals and pharmaceuticals is indicative of the current leanings in modern small molecule discovery. Late stage functionalization of C–H bonds has become increasingly relied on over the past decade to help target these moieties, however, non-directed activation of a desired C–H bond still remains a challenge. In response to this limitation, the design and use of directing groups has become extremely important despite their shortcomings. Previously, oxidative addition has served a similar roll for directed annulations over the last 30 years. This work details new methodology to leverage boron-promoted transmetallation as a traceless directing group for the activation and functionalization of adjacent C–H bonds.

Leveraging transmetallation of boryl species for C–H annulation

ACS Fall 2021

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