Diastereoselective synthesis and structure–affinity relationships of σ1 receptor ligands with spirocyclic scaffold

Org. Biomol. Chem., 2023, 21,7730-7752
DOI: 10.1039/D3OB01169K, Paper
Tobias Winge, Dirk Schepmann, Judith Schmidt, Constantin Daniliuc, Ernst-Ulrich Würthwein, Bernhard Wünsch
According to DFT calculations, the synthesis of spirocyclic σ1 ligands involves two aza-Michael additions or a [4 + 2] cycloaddition. Dispiro ligand with a high number of sp3 C-atoms shows promising σ1 affinity, selectivity and physicochemical properties.
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