AI Article Synopsis
- * Researchers present a simple method to create spirocyclic dihydropyridines by using a specific rearrangement process on 4-(1'-hydroxycyclobutyl)pyridines.
- * The findings highlight opportunities for modifying the starting materials and using the resulting compounds, which may lead to faster creation of important medicinal spirocycles.
Article Abstract
The identification of the beneficial pharmacokinetic properties of aza-spirocycles has led to the routine incorporation of these highly rigid and three-dimensional structures in pharmaceuticals. Herein, we report an operationally simple synthesis of spirocyclic dihydropyridines via an electrophile-induced dearomative semi-pinacol rearrangement of 4-(1'-hydroxycyclobutyl)pyridines. The various points for diversification of the spirocyclization precursors, as well as the synthetic utility of the amine and ketone functionalities in the products, provide the potential to rapidly assemble medicinally relevant spirocycles.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9872164 | PMC |
| http://dx.doi.org/10.1021/acs.orglett.2c04095 | DOI Listing |
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