A NEW METABOLIC REACTION OF NITROGEN MUSTARDS

We studied the substituent effect on the metabolism of ortho-, meta- and para-alkoxyaniline mustards. Surprisingly, very high yields of N-chloroethylaniline derivatives from the dechloroethylation reaction of para-alkoxyaniline mustards were obtained. N-2-Chloroethylaniline derivatives converted spontaneously into aziridines in microsomal solution. The order of the reaction rate of mustards in microsomal solution had a good parallel relationship with that of the antitumor activity of corresponding aniline mustards.