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Previously we have demonstrated that 3-phenacylmethylenepiperazin-2-ones possess antiinflammatory and analgesic properties in combination with low toxicity [1, 2]. In order to search for a relationship between the structure of piperazin-2-ones and their antiinflammatory and analgesic effects, it would be of interest to introduce a substituent in position 5 or 6 of the piperazinone cycle.For this purpose, we have studied reactions of the methyl esters of aroylpyruvic acids (I) with 1,2-diaminopropane (II) and 1,2-diaminophenylethane (III). Because compounds II and III are nonsymmewically substituted, the reactions may proceed in two pathways with the formation of isomeric piperazinones A and B: H R' N CH-C-R