The condensation of ethyl allophanate (I) with diphenylhydrazine (II) produced 1,2-diphenylurazole (III). Alkylation of (III) with N-(2-bromoethyl)phthalimide (IV) in the presence of potassium tert-butoxide afforded the 4-(2-phthalimidoethyl)urazole (V), and the subsequent hydrazinolysis of the phthalimide group of (V) yielded the amino derivative (VI). Then, coupling of (VI) with N-(benzyloxycarbonyl)arginine (VII) via activation with 1,1'-carbonyldiimidazole (CDI) furnished amide (VIII). Deprotection of the N-benzyloxycarbonyl group of (VIII) to give (IX) was effected by catalytic hydrogenation over Pd/C.

Condensation of piperazinyl dibenzoazepinone (X) with 3,3-tetramethyleneglutaric anhydride (XI) produced piperazide (XII). Further condensation of (XII) with arginine derivative (IX) using CDI yielded the title compound.