Synthesis and evaluation of the anticonvulsant activity of a series of 2-amino-1-phenyl-1-propranols derived from the metabolites of the antidepressant bupropion

Article abstract of DOI:10.1016/S0960-894X(96)00577-X

A series of 2-amino-1-phenyl-1-propanols that are structurally related to known metabolites of bupropion, 1 (Wellbutrin) were synthesized and evaluated as potential anticonvulsants. The (R*,R*)-2-tert-butylamino-1-(3-trifluoromethylphenyl) propanol 20 had an ED₅₀ of 16.5 ± 2.8 mg/kg ip in mice in the maximal electroshock screen and was chosen for further evaluation.