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

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.

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