Selective N-mono-alkylation of 6-aminouracils with alcohols: An environmentally benign protocol for synthesis of 6-alkylaminouracils

A highly selective N-alkylation of 6-aminouracils with alcohols achieved by using iridium catalysis on the basis of borrowing hydrogen methodology is presented. Reactions of 6-aminouracils and alcohols in the presence of [Cp*IrI2]2 were found to afford 6-monoalkyluracils selectively in high yield (up to 99%), mostly in a short reaction time (2 h). These results provide a new, green, and efficient protocol to access 6-alkylaminouracils, which are very important intermediates for synthesis of biologically active molecules.

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