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隣甲氧基-对[双-(2-氯乙基)-氨基]-苯丙氨酸(Ⅰ)对多种动物肿瘤有明显的抑制作用,临床试用结果表明:它对某些肿瘤有较好的疗效,为了简化合成方法,提高产率,我们进一步研究了(Ⅰ)的合成方法,本文报导了以间氨基-苯甲醚(Ⅳ)为原料,通过六步反应合成了(Ⅰ),总产率为29％左右,产品的理化性质及抗肿瘤作用均与已知物相同,此外还研究了自(隣甲氧基-对[双-(2-羟乙基)-氨基])-苄基-甲酰氨基-丙二酸乙酯(Ⅱ)制备(Ⅰ)的条件,发现(Ⅱ)在二氯甲烷中以五氯化磷氯化的结果较好,可分得结晶状的氯化产物(Ⅲ),后者水解卽得(Ⅰ),产品的纯度及产率均比用亚硫酰氯或氧氯化磷法为佳。
Ortho-methoxy-p- [bis- (2-chloroethyl) -amino] -phenylalanine (Ⅰ) on a variety of animal tumors were significantly inhibited, clinical trial results show that: it is more for some tumors In order to simplify the synthesis method and improve the yield, we further studied the synthesis method of (Ⅰ). In this paper, we report the synthesis of (Ⅰ) with 6-step reaction using m-amino- The total yield of about 29%, the physical and chemical properties of the product and anti-tumor effect are the same as known, in addition to also from the (o-methoxy - p - [2 - hydroxyethyl) - amino] Benzyl-formamido-malonic acid ethyl ester (II) was used to prepare (I). It was found that (II) chlorination with phosphorus pentachloride in methylene chloride gave better results and the crystalline form of chlorine The product (III), the latter hydrolysis obtained (I), product purity and yield than thionyl chloride or phosphorus oxychloride method is better.