Abstract. The development of a facile, single-step method for the synthesis of 1,4-disubstituted piperazine-2,6-diones (4) in excellent yields from the corresponding aliphatic, aromatic and heteroaromatic primary amines and iminodiacetic acids (1) is described. A possible mechanism is discussed and the presence of intermediate 6a is confirmed by high-resolution proton NMR spectroscopy. The subsequent two-step conversion of dione 4a into the deoxygenated 4-unsubstituted piperazine 10 in high yield provides an attractive alternative to the currently available (heter0)arylpiperazine synthetic methods.
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