臭氧化合成聚乙二醇醛基衍生物
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摘要
以甲氧基聚乙二醇为原料,通过烯烃化得到甲氧基聚乙二醇烯烃,最后经臭氧化反应得到甲氧基聚乙二醇醛基衍生物。通过核磁共振波谱仪(NMR)和基质辅助激光解吸电离飞行时间质谱(MALDI-TOF-MS)对产物的结构和性能进行了表征。结果表明,该方法合成的产物纯度高,无副产物,甲氧基聚乙二醇乙醛和聚乙二醇丙醛的产率分别高达98%和99%,取代度分别为90. 87%～99. 91%和98%～100%。
Methoxypolyethylene glycol olefin was obtained by olefination of methoxypolyethylene glycol,and followed by ozonation to give methoxypolyethylene glycol aldehyde derivative. The properties of products were characterized by nuclear magnetic resonance spectroscopy (NMR) and matrix-assisted laser desorption/ionization time of flight mass spectrometry (MALDI-TOF-MS). The results show that the product has high purity and no by-products. The yields of methoxy polyethylene glycol acetaldehyde and polyethylene glycol propionaldehyde are as high as 98% and 99%,respectively,and the degrees of substitution are 90. 87% ～99. 91% and 98% ～ 100%,respectively.
Methoxypolyethylene glycol olefin was obtained by olefination of methoxypolyethylene glycol,and followed by ozonation to give methoxypolyethylene glycol aldehyde derivative. The properties of products were characterized by nuclear magnetic resonance spectroscopy (NMR) and matrix-assisted laser desorption/ionization time of flight mass spectrometry (MALDI-TOF-MS). The results show that the product has high purity and no by-products. The yields of methoxy polyethylene glycol acetaldehyde and polyethylene glycol propionaldehyde are as high as 98% and 99%,respectively,and the degrees of substitution are 90. 87% ～99. 91% and 98% ～ 100%,respectively.
引文
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[3]Choe Y,Conover C D,Wu D C,et al.Anticancer Drug Delivery Systems:Multi-loaded N4-acyl Poly(ethylene glycol)Prodrugs of Ara-C.Ⅱ.Efficacy in Ascites and Solid Tumors[J].J Control Release,2002,79(1):55-70.
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