Synthesis and biological evaluation of bicyclic and tricyclic substituted nortropane derivatives: discovery of a novel selective α1D-adrenergic receptor ligand Original Research Article

A range of 3,6,6-trisubstituted nortropane derivatives based upon 6β-phenyltropane-3β,6 α-diol have been synthesised from 6β-hydroxytropinone, including some novel related tricyclic hemi-ketal and tricyclic ketal compounds. Derivatives were assessed for pharmacological affinity and selectivity at α1-adrenergic receptors, and 6β-phenyl-8-azabicyclo[3.2.1]octan-3-spiro-2′-(1′,3′-dioxolane)-6-ol, a novel lead compound selective for the alpha1D-adrenergic receptor, is reported.