6-Bromo-2-naphthylamine (II) was prepared from the corresponding naphthol (I) by treatment with ammonium hydroxide. Coupling of amine (II) with 4-[(methoxycarbonyl)methoxy]benzoic acid (III) by means of 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) provided amide (IV). This was converted to nitrile (V) by displacement of the bromide with CuCN in hot 1,3-dimethyl-2-imidazolinone. Addition of H2S to the cyano group of (V) produced thioamide (VI), which was further alkylated with iodomethane to yield the thioimidate (VII). Amidine (VIII) was then prepared by treatment of (VII) with ammonium acetate. Finally, selective hydrolysis of the methyl ester group of (VIII) by means of NaOH gave rise to the title compound.