Synthesis of new 1-Aryl-4-(biarylmethylene)piperazine ligands, structurally related to adoprazine (SLV313)

Abstract

A series of new 1-aryl-4-(biarylmethylene)piperazines has been synthesized. These ligands are structurally related to SLV-313, a potential atypical antipsychotic having potent D2 receptor antagonist and 5-HT 1A receptor agonist properties. Buchwald-Hartwig coupling reactions of 1-boc-piperazine with appropriate aryl halides and subsequent removal of the boc group rendered arylpiperazines. The reductive amination of the latter with suitable biarylaldehydes accomplished the synthesis of these ligands. © 2012 Verlag der Zeitschrift für Naturforschung, Tübingen.