1-Substituted 2-Azaspiro[3.3]heptanes: Overlooked Motifs for Drug Discovery
Angew. Chem. 2017, 129 (30), 8865–8869
The 2-substituted piperidine core is found in drugs (18 FDA-approved drugs), however, their spirocyclic analogues remain unknown. Described here is the synthesis of spirocyclic analogues for 2-substituted piperidines and a demonstration of their validation in drug discovery.