1‐Substituted 2‐Azaspiro[3.3]heptanes: Overlooked Motifs for Drug Discovery

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.