Diastereomeric process control in the synthesis of 2'-O-(2-methoxyethyl) oligoribonucleotide phosphorothioates as antisense drugs

被引：9
|
作者：
Ravikumar, VT [1 ]
Cole, DL [1 ]
机构：
[1] ISIS Pharmaceut, Carlsbad, CA 92008 USA
来源：
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2003年 / 22卷 / 5-8期
关键词：
coupling; stereochemistry; process control; oligomerization; activators; phosphate protecting group;
D O I：
10.1081/NCN-120023089
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：
Coupling of 2'-O-methoxyethylsubstituted nucleoside phosphoramidites to 5'-hydroxyl group of a nucleoside or nucleotide on solid support is under stereochemical process control and is independent of scale, concentration, synthesizer, ratio of amidite diastereomers, solid support etc. However, activators and phosphate protecting groups do play a role in influencing the ratio of phosphorothioate diesters obtained by sulfurization of phosphite triesters.
引用
收藏
页码：1639 / 1645
页数：7
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