AbstractA practical synthesis (Scheme I) is described for the preparation of a series of 4‐substituted‐3,3‐dimethyl‐1,2,3,4‐tetrahydroisoquinolines (3). Treatment of α‐(1‐amino‐1‐methylethyl)arylmethanols or α‐(1‐amino‐1‐methylethyl)heteroarylmethanols (5) with aromatic aldehydes gave imines7from which amino alcohols8were derived by reduction with potassium borohydride. Acid catalyzed cyclization of8yielded3. An acyl substituent was installed by Friedel‐Crafts acylation as a final step. The biological activities