Higenamine (I), a cardiotonic principle of Aconite root, was synthesized from 4-methoxy-phenylacetic acid (II) and β-(3, 4-dimethoxyphenyl)-ethylamine (IV). Condensation ofIV with 4-methoxyphenylacetyl chloride (III) was followed by cyclodehydration yielding 1-(4′-methoxybenzyl)-6,7-dimethoxy-3,4-dihydroisoquinoline (VI). Reduction ofVI to 1, 2, 3, 4-tetrahydroisoquinoline (VII) and subsequent demethylation provided desired product higenamine, 1-(4′-hydroxybenzyl)-6, 7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline.