4.8 Article

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

Journal

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 56, Issue 30, Pages 8865-8869

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201703801

Keywords

drug discovery; heterocycles; small rings; spirocycles; synthetic methods

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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.

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