合成分枝型聚乙二醇的简便新方法

以赖氨酸和mPEG5000为起始物,利用多肽合成中常用的保护、缩合和脱保护等方法合成了在生物医学领域中具有重要应用价值的分枝型聚乙二醇.用该方法形成的分枝型PEG在有机相中以缩合反应的方式一步完成,反应条件温和,且有较高的产率(61%).各步产物的表征都与其结构一致.最终产物分枝型PEG的¹HNMR的表征结果与其结构吻合.

A New Facile Synthesis Method of Branched PEG

The modification of bioactive proteins (peptides, enzymes) by using polyethylene glycol(PEG) has still been a hot filed of research. It has been reported that branched PEG is distinctly superior to linear PEG in the modification of some enzymes. However the existing synthetic methods of branched PEG make it very expensive to be used in research and practice. In this paper, a kind of branched PEG was synthesized via conventional methods used in the synthesis of polypeptide(protection, condensation, and deprotection) using lysine and mPEG5000 as starting materials. In this method, the most important reaction of forming branched PEG was fulfilled in one step by condensation reaction in organic phase. It makes this method remarkably different from other methods. The reaction condition is mild and the yield of the product(61%) is higher. The characterization of products in different steps is consistent with their structures. The 1H NMR spectrum of our end product branched PEG tallies with its structure.