AbstractThe 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 intermediate6ais confirmed by high‐resolution proton NMR spectroscopy. The subsequent two‐step conversion of dione4ainto the deoxygenated 4‐unsubstituted piperazine10in high yield provides an attractive alternative to the currently available (hetero)arylpiperazine synt