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1957年Heidel berger等[1,2]发展5-氟尿嘧啶作为一种抗代谢药物,用于临床治疗肠癌、胃癌、乳腺癌等多种癌症。虽然疗效较好,但毒副作用大。二十几年来,通过大量5-氟尿嘧啶衍生物的研究,又发现了几种毒性较低的衍生物,如氟尿嘧啶脱氧核苷(FUDR)、呋喃氟尿嘧啶(FT—207)、双喃氟啶(FD—1)[3]等。这些药物也已先后用于临床。研究水溶性的,并且具有活泼的可反应基团的5-氟尿嘧啶衍生物,以便一方面研究其抗肿瘤活性,另一方面用它作为起始物质或单体,进一步制取含5-氟尿嘧啶的高分子抗癌药物无疑也是目前感兴趣的课题。我们用5-氟尿嘧啶分别与甲醛和ω-氯代醇反应,合成了四种
1957 Heidel berger et al [1,2] the development of 5-fluorouracil as an anti-metabolism drugs for the clinical treatment of colon cancer, stomach cancer, breast cancer and other cancers. Although the curative effect is good, but the side effects are big. In the past two decades, several toxic derivatives such as FUDR, FT-207 and FD (FD) have also been discovered through a large number of 5-fluorouracil derivatives. -1) [3] and so on. These drugs have also been used clinically. 5-Fluorouracil derivatives, which are water-soluble and have reactive reactive groups, are studied in order to investigate their anti-tumor activity on the one hand and to use them as starting materials or monomers on the other hand to further prepare 5-fluorouracil-containing Polymer anticancer drugs are undoubtedly the subject of current interest. We used 5-fluorouracil and formaldehyde and ω-chlorohydrin reaction, the synthesis of four