The condensation of mitomycin A (I) with 2-(2-pyridyldithio)ethylamine (II) by means of triethylamine in methanol gives 7-N-[2-(2-pyridyldithio)ethyl]mitomycin C (III), which is then allowed to react with gamma-L-glutamylcysteamine (IV) in methanol. The gamma-L-glutamylcysteamine (IV) is obtained by deprotection of N,N'-bis[N-benzyloxycarbonyl-gamma-(alpha-benzyl)-L-glutamyl]cystamine (V) with anisole and trifluoroacetic acid giving the deprotected cystamine (VI), which is then reduced to the cysteamine (IV) with ethyl mercaptane.