The acylation of piperazine (II) with 4-nitrobenzoyl chloride (I) afforded a mixture of monoacylated (III) and diacylated (IV) products, which were separated by chromatography. Subsequent alkylation of monosubstituted piperazine (III) with 4-nitrophenethyl bromide (V) in the presence of K2CO3 and NaI yielded the title compound.