Synthesis of new aryl(hetaryl)-substituted tandospirone analogues with potential anxiolytic activity via reductive Heck type hydroarylations

GÜNKARA Ö. T. , Sucu B. O. , Ocal N. , Kaufmann D. E.

CHEMICAL PAPERS, cilt.67, ss.643-649, 2013 (SCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 67 Konu: 6
  • Basım Tarihi: 2013
  • Doi Numarası: 10.2478/s11696-013-0338-4
  • Sayfa Sayıları: ss.643-649


Tandospirone (I), developed as an anxiolytic drug, is an aryl-piperazine compound that binds to both 5-HT1A and dopamine D4 receptors. Palladium-catalysed hydroarylation reactions of tandospirone analogues containing an oxygen bridge and 3-(trifluoromethyl)phenyl or 2,3-dichlorophenyl groups were studied in order to find a new stereoselective access to a series of new exo-aryl(hetaryl)-substituted derivatives with potential biological activity.