Asymmetric construction of densely functionalized three-dimensional aza-tetracyclic scaffolds for drug discovery

Abstract

Asymmetric construction of densely functionalized three-dimensional aza-tetracyclic scaffolds were achieved by intramolecular Diels–Alder reaction of bicyclic precursors derived from L-tyrosine. Three substituents were systematically introduced into the developed scaffolds in...

Synthesis of the diazatricycloundecane scaffold via gold(i)-catalysed Conia-ene-type 5-exo-dig cyclization and stepwise substituent assembly for the construction of an sp3-rich compound library

“…14 We have also developed compound libraries based on unique three-dimensional bridged scaffolds. 15 Diazatricyclododecene 2 , a bridged-tricyclic scaffold, is one of our developed three-dimensional scaffolds and has been synthesised by the gold( i )-catalysed Conia-ene reaction with the cyclization precursor 1 to provide the compound library 3 (Fig. 1A).…”