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August 1, 1987Journal of Medicinal ChemistryOpen Access

Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives

Mark P. Wentland Denis M. Bailey E. John Alexander Michael J. Castaldi Richard A. Ferrari Dean R. Haubrich Daniel A. Luttinger Mark H. Perrone

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Abstract

A unique combination of alpha 2-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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Wentland et al. (1987) studied this question.

synapsesocial.com/papers/6a992239f3ae593e01363378 https://doi.org/10.1021/jm00391a034

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