A two-step sulfurization for efficient solution-phase synthesis of phosphorothioate oligonucleotides

被引:6
作者
Ghisaidoobe, Amar B. T. [1 ]
de Koning, Martijn C. [1 ]
Duynstee, Howard I. [2 ]
Ten Kortenaar, Paul B. W. [2 ]
Overkleeft, Herman S. [1 ]
Filippov, Dmitri V. [1 ]
van der Marel, Gijs A. [1 ]
机构
[1] Gorlaeus Labs, Leiden Inst Chem, NL-2300 RA Leiden, Netherlands
[2] Diosynth Int BV, NL-5340 BH Oss, Netherlands
关键词
D O I
10.1016/j.tetlet.2008.03.025
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A solution-phase approach for the synthesis of phosphorothioate oligonucleotides that circumvents the use of chromatographic purifications of protected phosphorothioate intermediates was developed. Implementation of a two-step sulfurization protocol in the phosphoramidite method allows efficient isolation of the intermediate phosphorothioates by extractions. The viability of this approach is demonstrated by the synthesis of a hexameric phosphorothioate oligonucleotide fragment. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3129 / 3132
页数:4
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