Development of siRNA for therapeutics: efficient synthesis of phosphorothioate RNA utilizing phenylacetyl disulfide
Vasulinga T Ravikumar1, Mark Andrade, Recaldo L Carty
1Isis Pharmaceuticals, Inc., 2282 Faraday Avenue, Carlsbad, CA 92008, USA. vravikumar@isisph.com
Bioorganic & Medicinal Chemistry Letters
|February 17, 2006
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.
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