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目前抗癌药的主要缺点是毒性高,治疗幅度不广,因此在实际使用上受到很大的限制。近年来为了改进这类药物的性能,研究了很多氮芥的有机化合物,这方面的工作已获得了初步成效。例如,某些具有双(β-氯乙基)氨基的氨基酸、肽类及醣类已应用于临床;将双(β-氯乙基)氨基导入二氧嘧啶、嘌啉、胆固醇及一系列喹啉类抗瘧药的分子,亦可获得效果胜于氮芥的抗肿瘤药物。本文报导某些具有对-双(β-氯乙基)氨基亚苄基衍生物的合成。这类化合物可以順利地由对-双(β-氯乙基)氨基苯甲醛(Ⅰ)与具有活泼亚甲基的化合
At present, the main disadvantage of anticancer drugs is high toxicity, the treatment rate is not wide, so in actual use subject to great limitations. In recent years, in order to improve the performance of these drugs, many nitrogen mustard organic compounds studied in this work has achieved initial success. For example, certain amino acids, peptides and carbohydrates with bis (beta-chloroethyl) amino groups have been used clinically; bis (beta-chloroethyl) amino groups have been introduced into dioxopyrimidines, Anti-malarial drug molecules, but also get better than nitrogen mustard antitumor drugs. Some reported the synthesis of p-bis (β-chloroethyl) aminobenzylidene derivatives. Such compounds can be successfully prepared from p-bis (β-chloroethyl) aminobenzaldehyde (Ⅰ) with a compound having an active methylene group