Protection of nucleosides

作者: Bruce S. Ross , Quanlai Song

DOI:

关键词: SelectivityOligonucleotideOrganic chemistryChemistrySolventReagentRegioselectivityNucleoside

摘要: A process of manufacturing protected nucleosides comprises reacting a nucleoside with protecting reagent in the presence regioselective activator to produce regioselectively nucleoside. In some embodiments inventive method, an optionally substituted trityl or pixyl group is selectively added 5'-O-position lutidine as activator/solvent. The method results improved selectivity 5'-O- position over 3’-0-position, thereby improving overall product yield and purity, permitting simplified purification protocols, cases obviating need for chromatography purified suitable automated synthesis oligonucleotides, such primers, probes antisense molecules.

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