The invention comprises GalNAc phosphoramidite derivatives of the formula I
wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/or optical isomers thereof. The invention further comprises a process for the preparation of the GalNAc phosphoramidite derivatives of the formula I and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.
本发明包括式 I 的 GalNAc 亚
磷酰胺衍
生物
其中 R1 是羟基保护基团,n 是 0 至 10 的整数,m 是 0 至 20 的整数及其相应的对映体和/或光学异构体。本发明还包括制备式 I 的 GalNAc 亚
磷酰胺衍
生物的工艺及其在制备具有治疗价值的 GalNAc 簇寡核苷酸共轭物中的用途。