【摘要】 目的合成肝靶向大分子前药半乳糖化壳聚糖-氟尿嘧啶偶合物(GC-FUA)。方法将乳糖酸以酰胺键偶合到壳聚糖(CS)上,得到半乳糖化壳聚糖(GC),再将经溴乙酸修饰的氟尿嘧啶(FUA)键合到GC上,得到目标产物GC-FUA,通过NMR和FT-IR对结构进行表征,并用1H-NMR测定乳糖酰基取代度(DSGC)和FUA取代度(DSFUA)。结果通过控制反应条件得到了乳糖酰基取代度不同的高分子载体GC,以及FUA取代度不同的偶合物GC-FUA。结论成功地合成了肝靶向大分子前药GC-FUA。更多还原

【Abstract】 OBJECTIVE To synthesize a liver-targeting prodrug named N-galactosylated-chitosan-5-fluorouracil acetic acid conjugate(GC-FUA).METHODS Lactobionic acid was firstly coupled with chitosan(CS),and then reacted with 5-fluorouracil acetic acid(FUA) modified with bromoacetate.The structure was confirmed by NMR and FT-IR.The degrees of substitution(DS) of lactosyl group and FUA moiety were calculated by 1H-NMR.RESULTS GC-FUA with different DS of lactosyl group and FUA moiety were synthesized via different reaction conditions.CONCLUSION The liver-targeting polymeric prodrug was obtained successfully.更多还原