Synthesis of new aryl(hetaryl)-substituted tandospirone analogues with potential anxiolytic activity via reductive Heck type hydroarylations |
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| Authors: | Omer Tahir Gunkara Bilgesu Onur Sucu Nuket Ocal Dieter E Kaufmann |
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| Institution: | 1338. Department of Chemistry, Yildiz Technical University, Faculty of Science and Arts, Davutpasa Campus, 34220, Esenler, Istanbul, Turkey
2338. Institute of Organic Chemistry, University of Technology, Leibnizstr. 6, Clausthal, D-38678, Clausthal-Zellerfeld, Germany
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| Abstract: | 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. |
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