RS-Goitrin can be conveniently prepared by a simplification of the Ettlinger procedure. Goitrin is a moderate inhibitor of purified bovine adrenal dopamine beta-hydroxylase. The administration of goitrin leads to a depression of brain norepinephrine and to an elevation of heart and adrenal dopamine.

The synthesis of benzimidazolone analogs of DOPA and α‐methyl‐DOPA and of the benzimidazole and benzimidazolone analogs of 6‐hydroxy‐DOPA is reported. These compounds showed a moderate amount of dopamine β‐hydroxylase and tyrosine hydroxylase inhibitory activity but did not significantly alter tissue catacholamine levels.

2‐Methoxy‐5‐nitro‐benzylbromid (I) liefert mit Acetamido‐malonsäureester ein Kondensationsprodukt (IIa), das zu (IIb) reduziert und acetyliert wird.