Adrenergic Agents, II¹⁾: 1‐Aryl‐N²‐alkyl‐ethanediamines as Isosters of Adrenergic Arylethanolamines

A family of 1‐aryl‐N²‐alkyl‐ethanediamines 1 isosteric with the N‐alkyl‐arylethanolamines are described. Although the prepared compounds were generally less potent than the N‐alkyl‐arylethanolamines, the 1‐aryl‐N'‐(phenylmethyl)‐N‐alkyl‐1,2‐ethanediamines derivatives 6, are more active than the debenzylated free amino analogs 1, which may be indicative of the importance of the lipophilicity of the substituent at the alpha position to the aromatic ring.