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1-Substituted 2-Azaspiro[3.3]heptanes: Overlooked Motifs for Drug Discovery
Authors:Alexander A. Kirichok  Dr. Iryna Shton  Dr. Maria Kliachyna  Dr. Iryna Pishel  Dr. Pavel K. Mykhailiuk
Affiliation:1. Enamine Ltd./Bienta, Chervonotkatska 78, 02094 Kyiv, Ukraine;2. Taras Shevchenko National University of Kyiv, Chemistry Department, Volodymyrska 64, 01601 Kyiv, Ukraine
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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