Phosphoramidites for synthetic RNA in the reverse direction, efficient RNA synthesis and convenient introduction of 3'-end ligands, chromophores and modifications of synthetic RNA
US8541569B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Feb 19, 2010 |
| Grant date | Sep 24, 2013 |
| Priority date | — |
| Expiry date | Mar 8, 2031 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention provides building blocks and methods for synthesizing very pure RNA in a form that can efficiently be modified at the 3′ end. Reverse RNA monomer phosphoramidites have been developed for RNA synthesis in 5′→3′ direction, leading to very clean oligo synthesis that allows for the introduction of various modifications at the 3′-end cleanly and efficiently. Higher coupling efficiency per step have been observed during automated oligo synthesis with the reverse RNA amidites disclosed herein, resulting in a greater ability to achieve higher purity and produce very long oligonucleotides. The use of the reverse RNA phosphoramidites in the synthetic process of this invention leads to oligonucleotides free of N+1 species.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.