Angew. Chem. 2017, 129 (30), 8865–8869
DOI: 10.1002/ange.201703801
Mykhailiuk P.; Kirichok A.; Shton I.; Kliachyna M.; Pishel I.
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.