Radical C(sp3)-H Bond Functionalization for the Construction of Heterocyclic Frameworks

Direct functionalization of inert C(sp3)-H bonds has long been considered one of the most challenging transformations in organic synthesis due to their high bond dissociation energies, low acidity, and poor orbital accessibility. Nevertheless, the ability to transform ubiquitous C(sp3)-H bonds without prefunctionalization offers significant advantages in atom economy, step efficiency, and structural diversification. In this study, radical generation and control were strategically utilized to develop efficient synthetic methods for various heterocyclic frameworks based on C(sp3)-H (and Si-H) bond functionalization.