聚乙二醇支载四分枝琥珀酰亚胺的合成

Synthesis of four-branches succinimide on poly(ethylene glycol)

以分子量3 400的双羟基聚乙二醇(PEG)作为可溶性载体,与甲基磺酰氯反应得PEG支载的甲基磺酸酯,在碳酸铯的作用下,与5-羟基间苯二甲酸甲酯反应并在氢化铝锂作用下还原得PEG支载的四分枝羟基化合物,继续与丁二酸酐反应得到PEG支载的四分枝羧基化合物,在N-羟基琥珀酰亚胺作用下,制备结构新颖的功能基为琥珀酰亚胺的PEG支载的枝化状化合物,总产率为73.04%,产物经IR,1H NMR和13C NMR分析,结果与其结构相吻合.

As a soluble support,PEG3 400 with double hydroxy reacted with methylsulfonylchloride afford to a PEG-supported methylsulphonic ester.Under the presence of cesium carbonate,PEG-supported methylsulphonic ester was treated with dimethyl 5-hydroxyisophthalate,and then reduced by lithium aluminum hydride to obtain a four-branched PEG-supported hydroxyl compound.This compound continued to react successively with succinic anhydride and N-hydroxysuccinimide.Ultimately,the novel PEG-supported four-branches compound was gained,with succinyl as its functional groups.The overall yield was 73.04%.The structure of PEG-supported branches compound was confirmed by means of IR,1H NMR and 13C NMR.