A Novel Synthesis of Oligonucleotide–Peptide Conjugates with a Base-Labile Phosphate Linker between the Two Components According to the Allyl-Protected Phosphoramidite Strategy
作者:Akira Sakakura、Yoshihiro Hayakawa
DOI:10.1016/s0040-4020(00)00376-8
日期:2000.6
the hydroxyl of a serine or threonine residue of a peptide by a phosphodiester bond. This synthesis utilizes the phosphoramidite method with allyl for the phosphate linkages and the C-terminal of the peptide and allyloxycarbonyl for the nucleoside bases and the N-terminal of the peptide. In this synthesis, the removal of the allylic protecting groups and the detachment of the products was achieved under
已经完成了对碱基不稳定的核苷酸-肽结合物的有效合成,其中两个组分通过磷酸二酯键直接连接在核苷酸的末端羟基和肽的丝氨酸或苏氨酸残基的羟基之间。该合成利用亚磷酰胺方法,其中烯丙基用于肽的磷酸键和C-末端,烯丙氧基羰基用于肽的核苷碱基和N-末端。在该合成中,在非碱性或温和的碱性条件下实现了烯丙基保护基的去除和产物的分离,从而使不稳定的磷酸酯连接基不引起明显的分解,因此以高纯度获得了目标缀合物。高产。