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从3-硝基-6-甲基-苯胺为原料经过六步反应合成了N-乙酰基-N-{3-[双-(β-氯乙基)-氨基]-6-甲基-苯基}-甘氨酸(Ⅲ_2),并从硝基苯胺以制备Ⅲ_a相似的步骤合成N-乙酰基-N-{3-[双-(β-氯乙基)-氨基]-苯基}-甘氨酸(Ⅲ_b)和N-乙酰基-N-{4-[双-(β-氯乙基)-氨基]-苯基}-甘氨酸(Ⅲ_c).药理试验表明:化合物Ⅲ_a对小白鼠肉瘤-180有显著的抑制作用,但化合物Ⅲ_b和Ⅲ_c无明显作用.Ⅲ_(a-c)对体外组织培养的Hela瘤细胞都无抑制作用.
N-acetyl-N- {3- [bis- (β-chloroethyl) -amino] -6-methyl-benzene was synthesized from 6-methyl- Yl} -glycine (III_2) and N-acetyl-N- {3- [bis- (β-chloroethyl) -amino] -phenyl} -glycine was synthesized from a nitroaniline in a similar procedure to that of III_a Ⅲ_b) and N-acetyl-N- {4- [bis- (β-chloroethyl) -amino] -phenyl} -glycine (Ⅲ_c) .Pharmacological tests showed that compound Ⅲ_a had significant effects on mouse sarcoma-180 Ⅲ_ (ac) had no inhibitory effect on Hela cells in vitro.