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

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.

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

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