4-ARYLPIPERIDINE DERIVATIVES AND USE THEREOF FOR PREPARING A MEDICAMENT FOR THE TREATMENT OF CNS DISEASE

Abstract

Title compds. [I; R1 = H, (unsatd.) alkyl; X = O, S, N; R2 = (CH2)nY; n = 1-4; Y, Ar = substituted aryl], were prepd. Thus, 4-(4-fluorophenyl)-4-[(4-trifluoromethyl)benzyloxy]piperidine hydrochloride (prepn. from 4-bromofluorobenzene, N-benzyl-4-piperidone, and 4-trifluoromethylbenzyl bromide given) bound to serotonin transporter in rat frontal cortex membranes with Ki = 26.8 pM; binding to dopamine transporter was negligible