Acta Chimica Sinica ›› 1959, Vol. 25 ›› Issue (6): 383-390. Previous Articles     Next Articles

肿瘤的化学治疗Ⅱ. 与普鲁卡因,辛可卡因等局部麻醉剂有关的氮芥类化合物的合成

潘百川, 任云峰, 汪润瑛, 高怡生   

  1. 中国科学院药物研究所
  • 收稿日期:1959-07-30 出版日期:1959-12-15 发布日期:2013-06-03

TUMOUR CHEMOTHERAPY——Ⅱ.NITROGEN MUSTARDS RELATED TO LOCAL ANESTHETICS,PROCAINE,PERCAINE AND OTHERS

PAN PEI-CHAUN, JEN YUN-FENG, WANG YUEN-YIN, KAO YEE-SHENG   

  1. Institute of Materia Medica, Academia Sinica, Shanghai
  • Received:1959-07-30 Online:1959-12-15 Published:2013-06-03

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.