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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。
Objective To synthesize hepatic targeting macromolecular prodrugs of galactosylated chitosan-fluorouracil conjugates (GC-FUA). Methods The lactose was coupled to chitosan (CS) by amide bond to obtain galactosylated chitosan (GC), and the fluorouracil (FUA) modified by bromoacetic acid was bonded to GC to obtain the target product GC- FUA, the structure was characterized by NMR and FT-IR and the degree of lactose acyl substitution (DSGC) and the degree of substitution of FUA (DSFUA) were determined by1H-NMR. Results The polymer carrier GC with different degree of lactyl substitution and GC-FUA with different degrees of substitution of FUA were obtained by controlling the reaction conditions. Conclusion The liver-targeting macromolecular prodrug GC-FUA was successfully synthesized.