The preparation of two kinds of nitrogen mustards related to local anesthetics was described.The compounds were (1).β-diethyl-amino-ethyl-p-bis-(2-chloroethyl) amino benzoate (Ⅳ, procaine-mustard), in which the p-amino-group of procaine (Ⅱ) was replaced by bis-(2-chloroethyl) amino group (Ⅰ).Similarly, nitrogen mustards Ⅴ, Ⅶ, Ⅷ, Ⅸa, Ⅸb and Ⅸc related to thiocaine and other anesthetics have also been prepared.(2).N-β-diethylamino-ethyl 2-n-butoxy-6-bis-(2-chloroethyl)amino-cinchoninic acid amide (ⅩⅥ, percaine-mustard), which was obtained by introducing Ⅰ to the molecule of percaine (ⅩⅢ).By doing so, the authors are in the hope to obtain a drug which, when appling directly to tumour tissue will not only act locally so as to prevent the normal tissue from being poisoned but will exert also the pain-relieving action.