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Preparative and analytical separation of the zopiclone enantiomers and determination of their affinity to the benzodiazepine receptor binding site
Authors:Gottfried Blaschke  Georg Hempel  Walter E Müller
Abstract:We report the preparative separation of rac-zopiclone using malic acid as the resolving agent. Furthermore, two different methods for the analytical determination of zopiclone enantiomers by HPLC on chiral stationary phases are described. The benzodiazepine receptor binding of the isolated enantiomers was investigated. Half-maximal inhibitory concentrations of (+)- and (?)-zopiclone were 21 or 1,130 nmol/liter, respectively, indicating a more than 50 times higher affinity of the (+)-enantiomer toward the receptor. © 1993 Wiley-Liss, Inc.
Keywords:zopiclone  chiral liquid chromatography  enantioseparation  fractional crystallization  cyclopyrrolone  benzodiazepine receptor binding
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