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peared to modify the biological properties to the greatest extent2). It has been concluded that the retention of activity of such derivatives requires the nitrogen atom to have a basic character. Therefore iV-alkyl derivatives are of interest3~5). This paper describes the synthesis of new compounds belonging to this class and obtained via nucleophilic addition of daunorubicin amino group to the active double bond of iV-substituted maleimides. The latter substances, with the most popular representative iV-ethylmaleimide, are used in biochemical experiments for modification of sulfhydryl-containing bioactive molecules under mild reaction conditions6>7). They have also been shown to react with amino groups and form the corresponding addition products6). Synthesis of iV-alkyl derivatives of daunorubicin is presented in Chart 1. In a typical synthesis, 0.056 ml of triethylamine was added with stirring to a cooled solution of daunorubicin hydrochloride (225 mg, 0.4 mmol) in DMF(2.5 ml). Then, 7V-ethylmaleimide (300 mg, 2.4 mmol) was added in 3 portions within 5 hours and the reaction allowed to proceed at room temp for 24 hours. To the resulting solution H2O (10 ml) was added and the product extracted with EtOAc (2 x 100 ml). The separated organic layer was washed twice with H2O(10 ml),

Synthesis of new N-alkyl daunorubicin derivatives via Michael addition to substituted maleimides.