The synthesis and evaluation of the major metabolites of mazapertine

AB Reitz, ME McDonnell, EW Baxter, EE Codd…

Index: Reitz, Allen B.; McDonnell, Mark E.; Baxter, Ellen W.; Codd, Ellen E.; Wu, Wu-Nan Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 14 p. 1927 - 1930

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Citation Number: 10

Abstract

Several of the key metabolites of mazapertine, a novel antipyschotic agent, were prepared in order to firmly establish their chemical structure and to obtain samples for biological testing. Hydroxymazapertine 3 was synthesized via a multi-step procedure starting from 5-fluoro-2- nitrophenol (8). Alcohol 4 was originally proposed for one of the major metabolites, but the confirmed structure after synthesis was isomer 20.