The invention relates to a novel labeling reactant of formula (I) suitable for labeling an oligonucleotide
1
wherein:
R is a temporary protecting group. A is either a phosphorylating moiety or a solid support tethered to a bridge point Z via a linker arm E. E′ is a linker arm between G and Z. G is a bivalent aromatic structure, tethered to two iminodiacetic acid ester groups N(COOR′″)
2
or G is a structure selected from a group consisting of
2
or
G is a protected functional group. The invention further concerns a method for direct attachment of a conjugate group to an oligonucleotide structure enabling the attachment of a desired number of these groups during chain assembly. The method comprises a Mitsonobu alkylation.
本发明涉及一种新型的标记试剂,其
化学式为(I),适用于标记寡核苷酸,其中:R是临时保护基;A是
磷酸化基团或通过连接臂E与桥点Z相连的固相支撑;E'是G和Z之间的连接臂;G是双价芳香结构,通过两个
亚胺二
乙酸酯基团N(COOR' ")2与之相连,或者G是从2组成的一组中选择的结构,或者G是受保护的功能基团。本发明还涉及一种直接将共轭基团附加到寡核苷酸结构的方法,使得在链组装过程中可以附加所需数量的这些基团。该方法包括Mitsonobu烷基化。