The present invention provides nucleosides an exocyclic amine-protected nucleoside of the formula: A-B where A is a 5′-protected ribose, 5′-protected-2-deoxyribose, 5′-protected-3′-phosphoramidite ribose, or 5′-protected-3′-phosphoramidite-2-deoxyribose moiety; and B is a nucleobase having an exocyclic amine group that is protected with di-tert-butylisobutylsilyl (“BIBS”) protecting group. Use of BIBS protecting group provides an exocyclic amine-protected nucleoside that is stable to a wide variety of reaction conditions associated with oligonucleotide synthesis. The present invention also provides, oligonucleotides comprising the same, and methods for producing the same.
本发明提供了式中的外环胺保护核苷:其中 A 是 5′保护的
核糖、5′保护的-
2-脱氧核糖、5′保护的-3′-亚
磷酰胺
核糖或 5′保护的-3′-亚
磷酰胺-
2-脱氧核糖分子;B 是具有外环胺基团的核碱基,该基团受二叔丁基异丁基
硅烷("BIBS")保护基团的保护。使用 BIBS 保护基团可提供一种外环胺保护核苷,它对与寡核苷酸合成相关的各种反应条件都很稳定。本发明还提供了包含这种核苷酸的寡核苷酸以及生产这种核苷酸的方法。