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

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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… Click to show full abstract

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.

Keywords: cis configured; rare cis; trace amine; taar1; configured disubstituted; amine associated

Journal Title: Mendeleev Communications
Year Published: 2021

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