AROMATIC COMPOUND, MODIFICATION CARRIER THAT USES SAME AND IS USED FOR SYNTHESIZING AN OLIGONUCLEOTIDE DERIVATIVE, OLIGONUCLEOTIDE DERIVATIVE, AND OLIGONUCLEOTIDE CONSTRUCT
申请人:Kitade Yukio
公开号:US20120245341A1
公开(公告)日:2012-09-27
The present invention provides an oligonucleotide derivative that enables to easily synthesize an oligonucleotide derivative chemically modified at the 3′-end with two moieties each having a benzene or pyridine structure with a few steps, an aromatic compound serving as a precursor for preparing the modification carrier for synthesizing oligonucleotide derivative, and the oligonucleotide derivative and the oligonucleotide construct using the same, that is chemically modified at the 3′-end with two moieties each having a benzene or pyridine structure, and has good permeability through a cell membrane and excellent nuclease resistance. The modification carrier for synthesizing oligonucleotide derivative, comprising a unit and a carrier carrying the unit directly or via a linker, wherein the unit is represented by the formula (a): wherein, R
1
to R
6
each independently represent hydrogen or a substituent other than hydrogen; Z
1
and Z
2
each independently represent CH or nitrogen; and X represents oxygen or sulfur.
本发明提供了一种寡核苷酸衍生物,使得可以通过几个步骤轻松地合成在3'-端带有两个苯或吡啶结构的化学修饰寡核苷酸衍生物,还提供了作为制备修饰载体的前体的芳香化合物,以及使用相同的化学修饰在3'-端带有两个苯或吡啶结构的寡核苷酸衍生物和寡核苷酸构建物,具有良好的细胞膜渗透性和出色的核酸酶抵抗性。用于合成寡核苷酸衍生物的修饰载体包括一个单元和一个携带该单元的载体,直接或通过连接剂携带该单元,其中该单元由式(a)表示:其中,R1到R6各自独立地表示氢或不是氢的取代基;Z1和Z2各自独立地表示CH或氮;X表示氧或硫。