An efficient multi-component synthesis of N-1-alkylated 5-nitrouracils from α-amino acids

Abstract The preparation of N -1 selectively alkylated uracil intermediates usually requires selective protection at N -3 followed by alkylation at N -1 and subsequent removal of the protecting group. In this Letter, we show the limitations of this approach when quaternary C centres at N -1 became a key target for the programme. To access this key substructure, we developed an efficient multi-component reaction (MCR) from readily available α-amino acid precursors.