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化学学报
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化学学报 ›› 1962, Vol. 28 ›› Issue (3): 173-180. 上一篇    下一篇

论文

肿瘤的化学治疗 Ⅶ.对-、間-及邻-[双-(2-氯乙基)氨甲基]苯丙氨酸双盐酸盐的合成

任雲峰, 高怡生   

  1. 中国科学院药物研究所
  • 修回日期:1962-01-19 发布日期:2013-06-03

TUMOUR CHEMOTHERAPY Ⅶ. SYNTHESIS OF ρ-,m-and o-[BIS-(2-CHLOROETHYL)-AMINOMETHYL]-PHENYLALANINE DIHYDROCHLORIDE

JEN YUN-FENG, KAO YEE-SHENG   

  1. Institute of Materia Medica, Academia Sinica
  • Revised:1962-01-19 Published:2013-06-03

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自二甲苯开始,经六步反应,合成对-、间-及邻-[双-(2-氯乙綦)氨甲基]苯丙氨酸双盐酸盐(Ⅲa,Ⅲb及Ⅲc,其代号分别为AT-290,AT-582及AT-581)。上述化合物对某些动物肿瘤具明显的抑制作用(其中Ⅲa并已介绍至临床试用)。

In the present investigation the synthesis of p-[bis-(2-chloroethyl)aminomethyl]-phenyl-alanine dihydrochloride (IIIa, designated as AT-290) has been described.As can be seen from the structure, it is derived from the nitrogen mustard HN2(Ⅳ R=H) by substituting one hydrogen atom of the methyl group with the p-phenylalanine moiety.Since the para position of the benzene ring is of importance in a number of metabolic functions of phenylalanine, the meta-and oTtho-isomer of Ⅲa, namely,m-[bis-(2-chloroethyl)amino-methyl]-phenylalanine dihydrochloride (Ⅲb, AT-582) and o-(bis-(2-chloroethyl)aminome-thyl]-phenylalanine dihydrochloride (Ⅲc, AT-581) were also synthesized.