Solution-Phase Synthesis of Phosphorothioate Oligodeoxynucleosides by the Phosphotriester Method
作者:
ISABELLE BARBER,
JEAN-LOUIS IMBACH,
BERNARD RAYNER,
期刊:
Antisense Research and Development
(MAL Available online 1995)
卷期:
Volume 5,
issue 1
页码: 39-47
ISSN:1050-5261
年代: 1995
DOI:10.1089/ard.1995.5.39
数据来源: MAL
摘要:
A "phosphorothioate triester method" was investigated for the solution-phase synthesis of phosphorothioate oligonucleosides. Using fully protected 3′-phosphorothiolate thymidine bearing O-cyanoethyl and S-2,4-dichlorobenzyl groups as phosphorothioate protecting groups, decathymidine nonaphosphorothioate was efficiently assembled through a blockwise procedure. Two side reactions occurred during the deprotection steps: breakage of internucleoside linkages (1.8% per linkage) and formation of phosphate diester linkages (0.9%). Substitution of the dichlorobenzyl group by the more labile 4-nitrobenzyl S-protecting group reduced the extent of internucleoside bond breakage by one-hal
点击下载:
PDF
(1204KB)
返 回