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目的:发展一种基于6-氨基己醇的新亚磷酰胺单体,用于寡聚脱氧核苷酸(ODN)-肽缀合物的连接臂合成。方法:利用正交保护法,将6-氨基己醇的氨基以4,4′-二甲氧基三苯甲基(DMT)保护,合成亚磷酰胺单体6,并研究其在ODN-肽缀合物合成中的效率。结果:利用新单体6获得了预期的ODN7以及ODN-肽缀合物8~10,得到了1H-NMR、32P-NMR和MALDI-TOF的确证。结论:基于6-氨基己醇的亚磷酰胺单体6适合ODN固相合成的条件,收率较高,为合成ODN-肽缀合物和对ODN进行其他修饰提供了一种选择。
OBJECTIVE: To develop a new phosphoramidite monomer based on 6-aminohexanol for the tether synthesis of oligodeoxynucleotide (ODN) -peptide conjugates. Methods: The amino group of 6-aminohexanol was protected by 4,4’-dimethoxytrityl (DMT) using orthogonal protection method to synthesize the phosphoramidite monomer 6 and to study its effect on ODN-peptide The efficiency of conjugate synthesis. Results: The expected ODN7 and ODN-peptide conjugates 8-10 were obtained with the new monomer 6, confirming 1H-NMR, 32P-NMR and MALDI-TOF. CONCLUSION: The 6-aminohexanol-based phosphoramidite 6 is suitable for the solid-phase synthesis of ODN with high yield. It provides an alternative for the synthesis of ODN-peptide conjugates and other modifications to ODN.