ArticleCurrent protocols2025
Synthesis of 4'-C-α-Aminoethoxy-2'-O-Methyl-5-Methyl- and 5-Propynyl-Uridine Phosphoramidites for Structurally Optimized Antisense Oligonucleotides.
Article in Current protocols, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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2 citing papers in PubMed.
- Article
- Synthesis of 4'-C-α-Aminoethoxy-2'-O-Methyl-5-Methyl- and 5-Propynyl-Uridine Phosphoramidites for Structurally Optimized Antisense Oligonucleotides.Current protocols · 2025Article
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Abstract
Chemical modifications are fundamental to improving the physicochemical and biological performance of oligonucleotide (ON) therapeutics by enhancing their hybridization affinity, nuclease resistance, and metabolic stability. Among the various sugar modifications developed, 4'-carbon (4'-C) substitutions have attracted significant attention for their ability to reinforce the sugar-phosphate backbone while preserving the natural C3'-endo conformation and Watson-Crick base pairing. The 4'-C-α-aminoethoxy (4'AEo) framework, in particular, provides steric protection against nuclease degradation without impairing RNase H activity, making it a valuable scaffold for next-generation antisense oligonucleotides (ASOs). This article presents optimized and reproducible synthetic protocols for two novel 4'-C-modified uridine phosphoramidite building blocks, 4'AEo
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