Mitsunobu coupling of 1,5-pentanediol (II) with two molecules of 4-hydroxybenzonitrile (I) in the presence of diisopropyl azodicarboxylate (DIAD) and triphenylphosphine afforded diether (III). Subsequent reduction of the nitrile groups of (III) using LiAlH4 gave the bis(benzylamine) derivative (IV), which was coupled with 3-cyanobenzenesulfonyl chloride (V) to provide sulfonamide (VI). The nitrile groups of (VI) were finally converted to the required bis amidino derivative by treatment with Weinreb reagent, prepared from trimethylaluminum and ammonium chloride.