A new two-step route to chiral 3-substituted [1,4]benzodiazepin-2-ones is described, which involves the coupling of 2-nitrobenzyl bromide with a series of amino acids, followed by diazepine ring formation with Fe/AcOH at 110 °C.
3-substituted [1,4]benzodiazepin-2-ones - pyrrolo[2,1-c][1,4]benzodiazepin-2-ones - iron/acetic acid - amino acids - chiral