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化学学报
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化学学报 ›› 1964, Vol. 30 ›› Issue (4): 369-380. 上一篇    下一篇

论文

肿瘤的化学治疗 ⅩⅩ.与双(β-氯乙基)氨甲基苯丙氨酸有关化合物的研究(一)2-(或3-)双-(β-氯乙基)氨甲基-4-羟基-苯丙氨酸双盐酸盐的合成

任云峯, 高怡生   

  1. 中国科学院药物研究所
  • 投稿日期:1963-10-28 发布日期:2013-06-03

TUMOUR CHEMOTHERAPY ⅩⅩ. STUDIES ON BIS (β-CHLOROETHYL)-AMINOMETHYLPHENYLALANINE 1. SYNTHESES OF 2-(OR 3-)[BIS-(β-CHLOROETHYL) AMINO]-METHYL-4-HYDROXYPHENYLALANINE DIHYDROCHLORIDES

JEN YUN-FENG, KAO YEE-SHENG   

  1. Institute of Materia Medica, Academia Sinica
  • Received:1963-10-28 Published:2013-06-03

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1.从间-及邻-甲酚碳酸乙酯(Ⅵ)开始,分别柽七步反应,获得Ⅳ及Ⅴ。化合物Ⅳ(AT-786)及Ⅴ(AT-916)对小鼠艾氏腹水及大鼠Jensen肉瘤具明显抑制作用。2.从3-醛基-4-羟基-氯苄(ⅩⅤ)开始,分别经七或六步反应,以及从对-乙氧羰氧基氯苄(ⅩⅩⅢ)开始,经三步反应,亦可获得Ⅴ。

In a previous paper[1] of this series of investigations the syntheses of p-,m-,and o-(bis-(β-chloroethyl)-amino]-methyl-phenylalanine dihydrochlorides (Ⅱ, designated as AT-290, AT-582, and AT-581 respectively) by substituting one hydrogen atom of the methyl group of HN2 with the phenylalanyl group, had been described. In this investigation, 2-and 3-[bis-β-chloroethyl)-amino]-methyl-4-hydroxyphenylalanine dihydrochlorides (Ⅳ and Ⅴ, designated as AT-786 and AT-916 respectively) had been synthesized, however, by substituting one hydrogen atom of the methyl group of HN2 with the tyrosinyl group.