Synthesis and evaluation of the antidepressant activity of the enantiomers of bupropion

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Abstract
The synthesis of the enantiomers of bupropion, (rac)‐2‐tert‐butylamino‐3′‐chloropropiophenone 1 (Wellbutrin®) is described. The enantiomers were compared with the racemate in both the tetrabenazine‐induced sedation model and the inhibition of uptake of biogenic amine assay. No significant differences were found in their potencies to reverse tetrabenazine‐induced sedation in mice or in their IC50 values as inhibitors of biogenic amine uptake into nerve endings obtained from mouse brain.