用于治疗的小干扰RNA（siRNA）的开发：利用苯乙酰二硫化物（PADS）高效合成硫代磷酸酯RNA。
Development of siRNA for therapeutics: efficient synthesis of phosphorothioate RNA utilizing phenylacetyl disulfide (PADS).
作者信息
Ravikumar Vasulinga T, Andrade Mark, Carty Recaldo L, Dan Amy, Barone Steve
机构信息
Isis Pharmaceuticals, Inc., 2282 Faraday Avenue, Carlsbad, CA 92008, USA.
出版信息
Bioorg Med Chem Lett. 2006 May 1;16(9):2513-7. doi: 10.1016/j.bmcl.2006.01.081. Epub 2006 Feb 14.
PMID:16481168
Abstract
Efficient synthesis of phosphorothioate RNA (PS-RNA) is demonstrated by using phenylacetyl disulfide (PADS) in a mixture of pyridine and acetonitrile (1:1, v/v) for 3 min. Sulfurization is achieved with >99.8% stepwise efficiency. This reagent also performs efficiently during synthesis of RNA containing PS:PO mixed backbone.
摘要
通过在吡啶和乙腈（1:1，v/v）的混合物中使用苯乙酰二硫化物（PADS）3分钟，证明了硫代磷酸酯RNA（PS-RNA）的高效合成。硫化的逐步效率达到>99.8%。该试剂在含有PS:PO混合主链的RNA合成过程中也能有效发挥作用。
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