高分子药物研究 Ⅷ.主链含5-氟尿嘧啶聚磷酸酯的合成

高分子药物研究 Ⅷ.主链含5-氟尿嘧啶聚磷酸酯的合成 CHEMOTHERAPEUTIC POLYMERS Ⅷ, Synthesis of polyphosphates containing 5-fluorouracil in the main Chain 范昌烈 first-author 麦才淞 余蕙 向家宁 丁齐柱 卓仁禧 氯乙醇、3-氯丙醇、4-氯丁醇在吡啶中分别与O-乙基二氯磷酸酯反应得到了O-乙基,0,O-二（氯乙基）磷酸酯（Ⅰ a ）.O-乙基,O,O-二（3-氯丙基）磷酸酯（Ⅰ b ）.O-乙基,O,O-二（4-氯丁基）磷酸酯（Ⅰ c ）.Ⅰ a 、Ⅰ b 、Ⅰ c 在碳酸钾存在下于DMF中分别与5-氟尿嘧啶缩聚得到三个新的主链含5-氟尿嘧啶的聚磷酸酯这类聚合物极易溶于水,并有较好的抗肿瘤活性。 Three new phosphates, 0-ethyl, 0, 0-diehl6roethyl phosphate, 0 ethyl, 0, 0-dichloro-n-propyl phosphate, 0 ethyl, 0, 0-dichloro-n butyl phosphate, were synthesized. Condensation polymerization of these compounds with 5 fluorouracil were respectively carried out in the presence of anhydrous potassium carbonate using DMF as solvent. The new polymers Obtained were purified by reprecipitation from the methanol/ether system. As determined by dynamic osmomerry, the average molecular weights of these polymers are about 2900-3900. The structures were identified by IR, UV, 1 H NMR spectra and elementalanalysis. All the polymers have good water solubility and exhibit significant antitumer activity. 1985-02-01 2021-04-01 2