ARYLOXYACETAMIDINES OF MEDICINAL INTEREST

The synthesis of new aryloxyacetamidines of potential medicinal interest as antihypertensives was undertaken. The preparation of the unsubstituted, N‐methyl and N,N‐dimethyl amidines was carried out by the Pinner synthesis or a modification of this process. The N,N,N′‐trimethylaryloxyacetamidines necessitated preparation by another procedure. Fifteen amidines and nine intermediates not previously reported in the literature have been prepared and characterized. 2‐Thymoloxyacetamidine, 2‐(2,6‐xylyloxy)acetamidine, 2‐(2,6‐dichlorophenoxy)acetamidine, 2‐(2,6‐dimethoxyphenoxy)acetamidine, 2‐benzyloxyacetamidine, and their N‐methyl and N,N‐dimethyl derivatives were evaluated for their potential cardiovascular effects. None of these compounds showed any potent pharmacological activities in a general screen or when tested as norepinephrine‐depleting agents or as adrenergic neuron‐blocking agents. Copyright © 1969 Wiley‐Liss, Inc., A Wiley Company