Rare cis-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1) |
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| Institution: | 1. Institute of Chemistry, St. Petersburg State University, 199034 St. Petersburg, Russian Federation;2. Immanuel Kant Baltic Federal University, 236016 Kaliningrad, Russian Federation |
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| 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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