2-substituted tetralin derivatives as conformationally restricted butyrophenone analogs

Five related derivatives of 2-(2-piperidinoethyl)tetralin have been synthesized as partially rigid analogs of the neuroleptic butyrophenones. Their in vitro dopamine receptor binding properties and in vivo inhibition of dexamphetamine-induced locomotor activity are described. 1-Phenyl-2-(2-piperidinoethyl)-3,4-dihydronaphthalene hydrochloride (8) is about 1% as potent as haloperidol.