A practical and convenient method for synthesizing antitumor compounds, N-alkyl-N- nitrosoureas, regioselectively nitrosated on the nitrogen atom bearing the alkyl group is proposed. N-Alkyl-N-nitrosocarbamates are interesting intermediates in these syntheses and yield, by reaction with amino compounds, the regioselectively nitrosated N-alkyl-N- nitrosoureas. As an interesting example, N, N'-bis [(2-chloroethyl) nitrosocarbamoyl] ...