Regioselective coupling of methyl 3,4-diaminobenzoate (I) with 3-cyanobenzoyl chloride (II) afforded benzamide (III). Further coupling of (III) with 4-tert-butylbenzoyl chloride (IV) gave diamide (V). Conversion of the methyl ester group of (V) into the benzyl ester analogue (VII) was effected by hydrolysis with LiOH, followed by treatment of the resulting carboxylic acid (VI) with benzyl bromide. Addition of hydroxylamine to the cyano group of (VII) gave rise to amidoxime (VIII). Subsequent hydrogenation of (VIII) over Pd/C produced the title amidine.