Abstract

A synthesis of 2′-fluoro and 2′-methoxy N6-methyladenosine phosphoramidites and their successful incorporation into oligonucleotides is reported. 2′-fluoro and 2́-methoxy modifications of sugars in siRNAs are known to aid stability and N6-methylation modifies the potency of therapeutic silencing RNAs (siRNA). We demonstrate that a combination of those modifications incorporated into the antisense strand of siRNA leads to efficient knockdown of a target gene in cells. This work broadens the available pool of chemical modifications of therapeutic siRNAs and provides tools for their efficient synthesis.

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