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. 2017 Jul 17;56(30):8865-8869.
doi: 10.1002/anie.201703801. Epub 2017 Jun 19.

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

Alexander A Kirichok  1 , Iryna Shton  1 , Maria Kliachyna  1 , Iryna Pishel  1 , Pavel K Mykhailiuk  2   1
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1-Substituted 2-Azaspiro[3.3]heptanes: Overlooked Motifs for Drug Discovery

Alexander A Kirichok et al. Angew Chem Int Ed Engl. .

Abstract

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.

Keywords: drug discovery; heterocycles; small rings; spirocycles; synthetic methods.

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