Lactones, XXV: Synthesis and 5‐HT₂‐Receptor Affinity of Some Fluorophenylated α‐Aminomethyllactones

Abstract

Antagonists displaying high affinity for both dopaminergic D2-and serotonergic 5-HT2-receptors, e.g. risperidone, are potential candidates for a more effective treatment of schizophrenia and are currently undergoing clinical trials2). Some fluorophenylated a-aminomethyl-y-lactones, which can be considered as "lactonized" neuroleptics, show moderate up to high (18: pKi = 7.77) affinity at the dopamine D2-binding site'). Now we report on the synthesis of derivatives containing the two structural units (9,lO) of ketanse-rine3) in the a-position and their affinity at the serotonin 5-HT2-receptor in comparison to some "lactonized" neuroleptics. H 0 0 Ketanserin 0 Risperidone N -0