The enantiomers of 9-hydroxyrisperidone, the major metabolite of risperidone and the active component of the
antipsychotic drug Invega®, were synthesized by efficient methods. Their optical rotation and enantiomeric purity were
characterized for the first time. The absolute configurations were assigned by comparing 1H NMR chemical shifts of
Mosher esters of a key stereoisomeric intermediate. Thus, the stereoisomeric center of (+)-9-hydroxyrisperidone has been
assigned as the S configuration, and its enantiomer has the configuration R.
Keywords: Invega®, 9-hydroxyrisperidone enantiomers, chiral HPLC, absolute configuration, synthesis.
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