biostudies-literatureMortensen KTCarlsbergfondetNy CarlsbergfondetRoyal SocietyUK Research and InnovationBiotechnology and Biological Sciences Research CouncilEngineering and Physical Sciences Research Council4591-4595https://www.ebi.ac.uk/biostudies/studies/S-EPMC10246434biostudies-literatureUnknown21(22)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.Organic & biomolecular chemistrySynthesis of sp³-rich heterocyclic frameworks by a divergent synthesis strategy.PMC10246434EP/P020291/1Wong DSYSpring DRMortensen KTKing TASore HFfalseSynthesis 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.2023-01-01T00:00:00Z2023 Jun2025-04-04T08:06:50.811Z2025-04-04T08:06:50.811ZS-EPMC102464343720345710.1039/d3ob00351e