A General Approach to Spirocyclic Piperidines via Castagnoli-Cushman Chemistry
Peshkov A.A. Makhmet A. Bakulina O. Kanov E. Gainetdinov R. Peshkov V.A. DarIn D. Krasavin M.
16 May 2022Georg Thieme Verlag
Synthesis (Germany)
2022#54Issue 112604 - 2615 pp.
Unsaturated spirocyclic lactams stemming from a variant of the three-component Castagnoli Cushman reaction successfully underwent hydrogenation to enable access to fully saturated spirocyclic lactams. The subsequent lactam reduction gave rise to 2-spiro piperidine building blocks. The latter can be further elaborated in compound libraries and, on their own, show propensity to activate trace amineassociated receptor 1 (TAAR1), an important target for CNS disease.
Castagnoli-Cushman , compound libraries , spirocyclic motifs , trace amine-associated receptor 1 agonists
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Institute of Chemistry, Saint Petersburg State University, 26 Universitetskii prospect, Peterhof, 198504, Saint Petersburg, 199034, Russian Federation
L. N. Gumilyov Eurasian National University, Department of Chemistry, Faculty of Natural Sciences, Nur-Sultan, 010000, Kazakhstan
Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg, 199034, Russian Federation
Nazarbayev University, Department of Chemistry, School of Sciences and Humanities, Nur-Sultan, 010000, Kazakhstan
Immanuel Kant Baltic Federal University, Kaliningrad, 236016, Russian Federation
Institute of Chemistry
L. N. Gumilyov Eurasian National University
Institute of Translational Biomedicine
Nazarbayev University
Immanuel Kant Baltic Federal University
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