A new method for introducing amidate linkages in oligonucleotides using phosphoramidite chemistry

被引：5

作者：

Davis, PW ^{[1
]}

Osgood, SK ^{[1
]}

机构：

[1] ISIS Pharmaceut, Carlsbad, CA 92008 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(99)00467-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cyanoethyl-protected phosphotriester links in oligonucleotides made with standard phosphoramidite chemistry were converted to phosphoramidate linkages during oligonucleotide synthesis on solid support. The cyanoethyl group was removed with piperidine, and the resulting phosphodiester was activated with p-tosyl chloride. An amine nucleophile displaced the tosyl to yield a phosphoramidate linkage. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2691 / 2692

页数：2

共 7 条

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[2]

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[3] ARYLSULFONYL CHLORIDES IN THE PRESENCE OF N-METHYLIMIDAZOLE AS EFFICIENT CONDENSING REAGENTS IN PHOSPHOTRIESTER OLIGONUCLEOTIDE SYNTHESIS [J].