A new procedure for N1-alkylation of imidazolidin-4-ones and its NMR characterization

• N1-alkylation of imidazolidin-4-ones under basic conditions.
• Chemical stabilization of imidazolidin-4-one ring.
• New peptidomimetic derivatives of antimalarial drug primaquine.

N1-unsubstituted imidazolidin-4-ones of primaquine (PQ) can be stabilized by N1-alkylation under basic conditions. Here we report the development, with our conditions, of peptidomimetic derivatives of PQ with l-amino acid and alkyl derivatives. The new derivatives represent potential new therapeutics for use against protozoan parasites, through enzymatic protection of aminopeptidases.

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