A four-step synthesis of 5-[N, N-bis (2-chloroethyl) amino]-1-methyl-2-nitroimidazole from 1- methyl-2-nitroimidazole is described. This compound showed similar hypoxia-selective cytotoxicity to the dinitrobenzamide mustard SN 23862 in UV4 cells (ca. 40-fold), and superior selectivity (> 7-fold) in repaircompetent AA8 cells.