Synthesis of Aza-Bridged Perhydroazulene Chimeras of Tropanes and Hederacine A

J Org Chem. 2023 Apr 7;88(7):4675-4686. doi: 10.1021/acs.joc.3c00169. Epub 2023 Mar 20.

Abstract

We report the synthesis of two novel azaperhydroazulene tropane-hederacine chimeras A and B, which contain an 8-azabicyclo[3.2.1]octane ring and a 7-azabicyclo[4.1.1]octane ring, respectively. The synthesis of both chimeras was achieved by epoxide ring opening and was governed by the stereochemistry of the hydroxy-epoxide unit. Finally, a density functional theory study was conducted to explain the regioselectivity of the cyclization and the importance of the stereochemistry of the hydroxyl group.