目的合成两种具有肠上皮细胞靶向的三甲基壳聚糖-Vit B12偶联物,并测定Vit B12的修饰度。方法分别以丁二酸和PEG2000为间隔基制备三甲基壳聚糖-Vit B12偶联物。结果与结论合成了两种不同间隔基的三甲基壳聚糖-Vit B12偶联物;目标偶联物及重要中间体经1HNMR、MS和UV确证;两种偶联物中Vit B12的修饰度分别为3.3%、3.1%。
OBJECTIVE To synthesize two kinds of intestinal epithelial cells targeting N-trimethyl chitosan-Vit B12 conjugates and determine the level of Vit B12 substitution on the conjugates.METHODS Vit B12 was conjugated with N-trimethyl chitosan via two kinds of spacers:succinic acid and PEG2000.RESULTS and CONCLUSION Two kinds of N-trimethyl chitosan-Vit B12 conjugates were successfully synthesized.The chemical structures of the target conjugations and intermidiates were characterized by 1HNMR,MS and UV.The degree of Vit B12 substitution on the conjugations were 3.3% and 3.1%,respectively.