Condensation of N-(2-furanylcarbonyl)piperazine (I) with 4-chloro-3-(methylsulfonyl)benzoic acid (II) at 120 C produced the disubstituted piperazine (III). After activation of the carboxy group as the imidazolide (IV) upon treatment with 1,1'-carbonyldiimidazole and N-methylmorpholine, treatment with guanidine hydrochloride (V) and NaH in hot DMF yielded the corresponding benzoyl guanidine, which was finally isolated as the methanesulfonate salt.