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Synthesis of Fully Protected Nucleoside- Folic Acid Conjugated Phosphoramidites and Their Incorporation into Antisense Oligonuleotides
Authors:Balkrishen Bhat  Guity Balow  Andrei Guzaev  P. Dan Cook  Muthiah Manoharan
Affiliation:Department of Medicinal Chemistry , Isis Pharmaceuticals 2292 Faraday Avenue , Carlsbad, CA, 92008, USA
Abstract:Abstract

A novel synthesis of the nucleoside-folic acid conjugates has been accomplished. This approach allowed us to synthesize several analogs, which were converted to phosphoramidites and successfully incorporated into therapeutically active antisense oligonucleotides.
Keywords:
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