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Updated: Aug 20, 2025

Chemical Triphosphorylation of Oligonucleotides
Published on: June 2, 2022
Synthesis of 5'-fluorophosphate-modified short-interfering RNAs
Andrew Varley1, Jean-Paul Desaulniers1
1Faculty of Science, University of Ontario Institute of Technology, Oshawa, Canada.
Abstract:
We have developed an improved scheme for the synthesis of a mono-fluorinated phosphoramidite for the 5'-modification of nucleic acids using standard phosphoramidite chemistry. We describe the first report of a phosphofluoridate modified siRNA strand and have evaluated C18 HPLC for purification of modified strands from unreacted siRNA strands. Lastly, the biological activity of the high purity siRNA strands, when placed on the sense and/or antisense strand, was evaluated to assess the impact of 5' phosphofluoridate modifications on siRNA activity.
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