E. Yu. Levashova, A. A. Firsov, O. Yu. Bakulina, A. A. Peshkov, E. V. Kanov, R. R. Gainetdinov, M. Yu. Krasavin, “Rare <i>cis</i>-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1)”, Mendeleev Commun., 2021, Volume 31, Issue 4,Pages <nobr>488

This article is cited in 8 papers

Communications

Rare cis-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1)

E. Yu. Levashova^a, A. A. Firsov^a, O. Yu. Bakulina^a, A. A. Peshkov^a, E. V. Kanov^a, R. R. Gainetdinov^a, M. Yu. Krasavin^ab

^a Institute of Chemistry, St. Petersburg State University, St. Petersburg, Russian Federation
^b Immanuel Kant Baltic Federal University, Kaliningrad, Russian Federation

Abstract: Rare cis-configured 2,4-disubstituted 1-alkylpyridines were envisioned as ligands for trace amine associated receptor 1 (TAAR1). They were synthesized in diastereomerically pure form with the decarboxylative Castagnoli–Cushman reac-tion followed by two reduction events. Despite showing no affinity to TAAR1 as was anticipated, these novel, druglike and CNS-focused compounds will be of much utility in sub-sequent lead generation pursuits.

Language: English

DOI: 10.1016/j.mencom.2021.07.016

	*Supplementary materials:*
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