Journal of Medicinal Chemistry p. 1482 - 1489 (1987)
Update date:2022-08-16
Topics:
Wentland
Bailey
Alexander
Castaldi
Ferrari
Haubrich
Luttinger
Perrone
A unique combination of α2-adrenoreceptor antagonist and serotonin-selective reuptake inhibitory activities has been identified in a series of 2-substituted 4,5-dihydro-1H-imidazole derivatives. This combination of blocking activities has provided one of these derivatives, napamezole hydrochloride (2), with potential as an antidepressant. A discussion of the syntheses of these compounds includes a convenient method for the conversion of nitriles to imidazolines with ethylenediamine and trimethylaluminum.
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