Synthesis of Sp3-Rich Heterocyclic Frameworks by a Divergent Synthesis Strategy

Fragment-based lead discovery (FBLD) often relies on flat, aromatic compounds which display undesirable physicochemical properties with limited exit vectors for fragment growth. Herein, we report concise synthetic strategies to sp3-rich heterocyclic fragments encompassing polar exit vectors poised for fragment-to-lead (F2L) development.