ИСТИНА

Piperidines occupy privileged place among the variety of the heterocycles, being structural motif of many alkaloids, biologically active molecules and pharmaceutically relevant compounds. We have elaborated stereoselective construction of piperidine skeleton of 6-substituted piperidine-2,4-diones and 6-amino-2,3-dihydropyridine-4-(thi)ones by effective 3-steps transformation of homoallylamines where the key step is enolate-type rearrangement [1-4]. Piperidinones are excellent models for design of different biologically active compounds. In particular, by the combination of adamantyl and piperidinone fragments was obtained the molecules with potent activity against rimantadine-resistant Influenza A (H1N1) virus strains [5], and the introduction of 2-aminopyrimidine moiety into piperidine-2,4-diones and 6-amino-2,3-dihydro-4-pyridinones leads to novel inhibitors of heat shock protein 90 (analogues of Novartis drug candidate HSP990) belonging to the last generation drugs perspective for treatment of oncological, viral, fungal and parasitic diseases. This work was supported by the Russian Science Foundation (grant № 15-13-00109).