Synthesis of Methoxyethyl Nucleoside Dimer Phosphoramidites

Bulletin of the Korean Chemical Society

Yong Han Kang¹  Gi Weon Yu² 

[1] 88 Korea;Department of Applied Chemistry Hanyang University Ansan 155‐

关键词: Phosphoramidite;    Oligonucleotide;    Solid phase synthesis;    Dimer;   

DOI  :  10.1002/bkcs.10749

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Four types of methoxyethyl (MOE) nucleoside phosphoramidites, which are categorized as second‐generation building blocks of antisense oligonucleotide drugs, were synthesized. Also, three types of MOE nucleoside dimer phosphoramidites were synthesized to increase the efficiency and oligomer purity in solid phase synthesis. The block‐like dimer phosphoramidites can prevent or minimize the formation of the (N‐1) mer impurity, thereby affording the fabrication of pure oligonucleotides and reducing the synthesis time by performing coupling reactions in the order of 2 + 2 + 2.

【 授权许可】

Unknown