聚乙二醇二丁二酸酯的合成

Synthesis of polyethylene glycol disuccinate

聚乙二醇在药物合成上有很广泛的用途,但其端羟基的活性相对较低,直接应用受到限制.若将羟基活化为羧基则可以扩大其应用范围;尤其是在合成二聚物时,将疏水链换成亲水的聚乙二醇二丁二酸酯链可以增加桥链的亲水性.为此,以聚乙二醇、丁二酸酐为反应物,以吡啶为溶剂,分别合成了一缩二乙二醇二丁二酸酯、二缩三乙二醇二丁二酸酯、三缩四乙二醇二丁二酸酯.

Polyethylene glycol（PEG） is widely applied to synthesize drug.However,its direct application is limited due to low activity of terminal hydroxyl groups.This means that the application field of PEG can be extended under the condition that the hydroxyl groups are converted to active carboxyl groups.Particularly,it is feasible to enhance the bridge chain＇s hydrophilicity when substituting hydrophobic chain with hydrophilic chain during the synthesis of the polymers.Therefore,diethylene disuccinate,triethylene disuccinate and tetraethylene disuccinate were synthesized by using PEG and succinic anhydride as the starting materials.