A General Approach to Spirocyclic Piperidines via Castagnoli–Cushman Chemistry

2022

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DOI 10.1055/s-0040-1719878
Data confidence 70 medium
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Abstract

Abstract 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 amine-associated­ receptor 1 (TAAR1), an important target for CNS disease.