Pd-catalyzed direct C–H bond functionalization of spirocyclic σ1 ligands: generation of a pharmacophore model and analysis of the reverse binding mode by docking …

C Meyer, D Schepmann, S Yanagisawa…

Index: Schlaeger, Torsten; Schepmann, Dirk; Wuerthwein, Ernst-Ulrich; Wuensch, Bernhard Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 6 p. 2992 - 3001

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Citation Number: 33

Abstract

To explore the hydrophobic binding region of the σ1 receptor protein, regioisomeric spirocyclic thiophenes 9–11 were developed as versatile building blocks. Regioselective α- and β-arylation using the catalyst systems PdCl2/bipy/Ag2CO3 and PdCl2/P [OCH (CF3) 2]