Solid phase synthesis of phosphorothioate oligonucleotides utilizing diethyldithiocarbonate disulfide (DDD) as an efficient sulfur transfer reagent

被引:23
作者
Cheruvallath, ZS [1 ]
Kumar, RK [1 ]
Rentel, C [1 ]
Cole, DL [1 ]
Ravikumar, VT [1 ]
机构
[1] ISIS Pharmaceut, Carlsbad, CA 92008 USA
关键词
oligonucleotides; phosphorothioates; sulfurization; solid phase synthesis; DDD;
D O I
10.1081/NCN-120022050
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
Diethyldithiodicarbonate (DDD), a cheap and easily prepared compound, is found to be a rapid and efficient sulfurizing reagent in solid phase synthesis of phosphorothioate oligodeoxyribonucleotides via the phosphoramidite approach. Product yield and quality based on IP-LC-MS compares well with high quality oligonucleotides synthesized using phenylacetyl disulfide (PADS). which is being used for manufacture of our antisense drugs. graphics.
引用
收藏
页码:461 / 468
页数:8
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