Back to Search Start Over

Convergent synthesis of phosphorodiamidate morpholino oligonucleotides (PMOs) by the H-phosphonate approach.

Authors :
Tsurusaki, Taiki
Sato, Kazuki
Imai, Hiroki
Hirai, Kunihiro
Takahashi, Daisuke
Wada, Takeshi
Source :
Scientific Reports. 11/18/2023, Vol. 13 Issue 1, p1-10. 10p.
Publication Year :
2023

Abstract

Phosphorodiamidate morpholino oligonucleotides (PMOs) are a promising type of antisense oligonucleotides, but their challenging synthesis makes them difficult to access. This research presents an efficient synthetic approach for PMOs using the H-phosphonate approach. The use of phosphonium-type condensing reagents significantly reduced coupling times compared with the current synthetic approach. Furthermore, phosphonium-type condensing reagents facilitated the fragment condensation of PMO, synthesizing up to 8-mer containing all four nucleobases with remarkable coupling efficacy. This is the first report on the convergent synthesis of PMOs. This approach would facilitate the large-scale synthesis of PMOs and accelerate their popularity and accessibility as a next-generation therapy. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
20452322
Volume :
13
Issue :
1
Database :
Academic Search Index
Journal :
Scientific Reports
Publication Type :
Academic Journal
Accession number :
173737473
Full Text :
https://doi.org/10.1038/s41598-023-38698-2