Method for synthesizing ribonucleic acid H-phosphonate monomer, and oligonucleotide synthesis in which said monomer is used
US11174279B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Jun 20, 2017 |
| Grant date | Nov 16, 2021 |
| Priority date | — |
| Expiry date | Feb 16, 2038 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention pertains to a method for synthesizing a ribonucleic acid H-phosphonate monomer, and a method for performing oligonucleotide synthesis in which said monomer is used. The present invention pertains to a method for manufacturing an inexpensively manufacturable H-phosphonate nucleoside derivative in which selective protection is provided to position 2′ of a ribonucleoside monomer required in RNA oligonucleotide synthesis. The present invention is characterized in that: hydroxyl groups in position 2′ and position 3′, which have slightly different reactivity, are caused to react with an aromatic acyl halide at low temperature to selectively esterify position 2′; and subsequently the hydroxyl group at position 3′ in one pot is captured by a phosphityl group to prevent position 2′ and position 3′ transfer of the acyl group.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.