Diastereoselective synthesis of 1,3-di- and 1,3,3-trisubstituted diaziridines coupled with neurotransmitter amino acids

The pH-controlled one-pot three-component condensation of carbonyl compounds, amino acid ethyl esters and hydroxylamine-O-sulfonic acid in water–ethanol mixture at 0–5 ̊C diastereoselectively affords conjugates of 1,3-di- or 1,3,3-trisubstituted diaziridines with neurotransmitter amino acids.