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发明公开
CN101768263A 一种可用于制备长循环脂质体的巯基化聚乙二醇的合成方法 失效 - 权利终止

一种可用于制备长循环脂质体的巯基化聚乙二醇的合成方法
摘要：
本发明公开了一种如式I所示的化合物的制备方法。所述的方法包括步骤：(1)将聚乙二醇单甲醚和琥珀酸酐混合于氯仿中，在60-90℃条件下得到如式II所示的化合物；(2)将式II化合物、N-羟基琥珀酰亚胺、脱水剂和有机碱混合，得到如式III所示的化合物；所述的脱水剂选自1-乙基-3-(3-二甲氨基丙基)-碳酰二亚胺盐酸盐、N，N-二异丙基碳二亚胺、或N，N-二环己基碳二亚胺；所说的有机碱选自N-甲基吗啉、三乙胺、吡啶、或二甲氨基吡啶；(3)将式III化合物和半胱氨酸混合，得到如式IV所示的化合物；和(4)将式IV化合物和二硫苏糖醇混合，得到如式I所示的化合物。本发明还提供了可靠的式I所示的化合物的鉴定方法。n＝3-125。
摘要（英）：

The invention discloses a method for preparing a compound as disclosed in Formula I. The method comprises the following steps: (1) mixing methoxy polyethylene glycol and succinic anhydride with chloroform, thereby obtaining a compound as disclosed in Formula II at 60-90 DEG C; (2) mixing the compound as disclosed in Formula II, N-hydroxyl succinimide, a dehydrator and organic base to obtain a compound as disclosed in Formula III, wherein the dehydrator is selected from 1-ethyl-3-(3-dimethylin propyl)-carbonyl diimine hydrochlorate, N,N-diisopropyl carbodiimide or N,N-dicyclohexylcarbodiimide, and the organic base is selected from N-methyl morpholine, triethylamine, pyridine or dimethylamino pyridine; (3) mixing the compound as disclosed in Formula III with cysteine to obtain a compound as disclosed in Formula IV; and (4) and mixing the compound as disclosed in Formula IV with dithiothreitol to obtain the compound as disclosed in Formula I. The invention also provides a reliable method for verifying the compound as disclosed in Formula I. n is equal to 3-125.

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