水溶性聚[N-(2-羟乙基)-L-谷酰胺]的合成

Synthesis of water-soluble poly[N-(2-hydroxyethyl)-L-glutamine]

目的 :合成具有良好水溶性、生物相容性、低毒和可生物降解的高分子材料 ,以期作为键合药物的载体 .方法 :以L -谷氨酸为单体 ,经r -羧基的苄基保护 ,与光气 /甲苯液反应制备L-谷氨酸苄酯的羧酸酐 ,均聚得L -谷氨酸苄酯 (PBLG) ,然后经由 2 -氨基乙醇胺解得聚 [N - ( 2 -羟乙基 ) -L -谷酰胺 ](PHEG) .结果 :对所合成物进行了UV、IR、HNMR、相对分子质量、羟基含量的表征 ,证实此物为PHEG .结论 :合成的聚 [N - ( 2 -羟乙基 ) -L -谷酰胺 ]的侧链上具有大量的羟基 ,具有优良的水溶性和反应活性 。

Aim: To get a water-soluble, low-toxic, biocompatible, and biodegradable drug carrier . Methods: Poly (γ-benzyl-L-glutamate) (PBLG) was prepared by polymerization of the N-carboxyl anhydride of γ-benzyl-L-glutamate which was first synthesized by glutamic acid with benzyl alcohol . Poly-[N-(2-hydroxyethyl)-L-glutamine] (PHEG) was then obtained by aminolysis of PBLG with 2-aminoethanol. Results: The data of IR, UV, HNMR, Mr, and content of hydroxyl of PHEG were determined. Conclusion: PHEG contained a lot of hydroxyl groups and was readily water-soluble and reactive. The compound may be used as drug carrier.[