苏长会,刘霞,丁志远,崔凯,马洁洁.化学通报,2019,82(2):183-186. |
氨基聚乙二醇-1,2-二硬脂酰甘油磷酰乙醇胺的合成 |
Synthesisi of amine polyethylene glycol-1,2-distearoyl-glycero-3-phosphoethanolamine |
投稿时间:2018-08-15 修订日期:2018-10-08 |
DOI: |
中文关键词: 聚乙二醇 脂质体 磷脂 合成 |
英文关键词:Polyethylene glycol Liposomes Phospholipid Synthesis |
基金项目:江苏省高校自然科学基金 |
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中文摘要: |
以1,2-二硬脂酸甘油酯为原料,与三氯氧磷及乙醇胺反应合成1,2-二硬脂酰甘油磷酰乙醇胺(DSPE);再以聚乙二醇2000(PEG2000)为原料,通过磺酰化、叠氮化反应合成叠氮基聚乙二醇2000(N<sub>3</sub>-PEG2000);DSPE与N<sub>3</sub>-PEG2000在N,N-羰基二咪唑(CDI)作用下生成叠氮基聚乙二醇2000-1,2-二硬脂酰甘油磷酰乙醇胺(N<sub>3</sub>-PEG2000-DSPE);最后通过催化氢化制备氨基聚乙二醇2000-1,2-二硬脂酰甘油磷酰乙醇胺(NH<sub>2</sub>-PEG2000-DSPE),其结构经过IR,MS及<sub>1</sub>H NMR等确证。 |
英文摘要: |
DSPE was synthesized by reactions with Glycerol-1,2-distearate, Phosphorusoxychloride and 2-Aminoethanol as raw materials. N<sub>3</sub>-PEG2000 was achieved by an efficient two step process from readily available PEG2000. Subsequently, N<sub>3</sub>-PEG2000-DSPE was obtained by linking DSPE to N<sub>3</sub>-PEG2000 via CDI. Finally, catalytic hydrogenation of the azidoSgroup yielded the target compound NH<sub>2</sub>-PEG2000-DSPE, which was characterized by IR analysis, <sub>1</sub>H NMR spectroscopy, mass spectrometry. |
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