Synthesis of sp-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 sp 3 -rich heterocyclic fragments encompassing polar exit vectors poised for fragment-to-lead (F2L) development. Herein, we present sp 3 -rich fragments, that display optimal physicochemical properties and exit vectors ideal for fragment-based lead discovery.