An alternative advantageous protocol for efficient synthesis of phosphorothioate oligonucleotides utilizing phenylacetyl disulfide (PADS)

被引:7
作者
Kumar, R. Krishna [1 ]
Olsen, Phil [1 ]
Ravikumar, Vasulinga T. [1 ]
机构
[1] ISIS Pharmaceut, Carlsbad, CA 92008 USA
关键词
SOLID-PHASE SYNTHESIS; SULFUR-TRANSFER REAGENT; ANTISENSE OLIGONUCLEOTIDES; 3H-1,2-BENZODITHIOL-3-ONE 1,1-DIOXIDE; STEREOCONTROLLED SYNTHESIS; MANUFACTURE;
D O I
10.1080/15257770601112739
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Phosphorothioate oligonucleolides could be svnthesized using a 0.2 M solution of phenylacetyl disulfide (PADS) in a mixture of pyridine and acelonitrile (1:1, v/v) with > 99.9% step-wise efficiency. Unlike most other sulfurizing reagents that need to be stable in solution for performance, PADS needs to degrade and "age" in solution and hence performs efficiently even after storing the solution the room temperature for over a month. High yield and quality of of oligonucleotides are produced thereby offering an alternative attractive protocol for use of this efficient sulfurizing reagent.
引用
收藏
页码:181 / 188
页数:8
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