Title:
PROCESSES FOR PREPARING OLIGONUCLEOTIDES
Document Type and Number:
WIPO Patent Application WO/2022/006871
Kind Code:
A1
Abstract:
Disclosed are processes for preparing oligonucleotides. The process comprises: (a) converting a compound of Formula X-1 into a compound of Formula X-2: where R10 is a residue of an oligonucleotide (e.g., a phosphorodiamidate morpholino oligomer); R11 is an amine protecting group; wherein the compound of Formula X-1 is not bound to a solid support; and; (b) optionally removing protecting groups in the compound of Formula X-2 to obtain the oligonucleotide. The synthetic processes described herein are advantageous in many aspects, including but not limited to improved yields and purities of target phosphorodiamidate morpholino oligomers with reduced 4-nitrostyrene adduct impurities. (X-1), (X-2)
Inventors:
HU CHENCHEN (CN)
ZHAO QIANG (CN)
LI QING (CN)
YANG JIMIN (CN)
ZHAO QIANG (CN)
LI QING (CN)
YANG JIMIN (CN)
Application Number:
PCT/CN2020/101401
Publication Date:
January 13, 2022
Filing Date:
July 10, 2020
Export Citation:
Assignee:
CHANGZHOU SYNTHEALL PHARMACEUTICALS CO LTD (CN)
SHANGHAI STA PHARMACEUTICAL R&D CO LTD (CN)
SHANGHAI STA PHARMACEUTICAL R&D CO LTD (CN)
International Classes:
C07D487/04; C07D519/00
Domestic Patent References:
| WO2001002417A1 | 2001-01-11 |
Foreign References:
| CN105228999A | 2016-01-06 | |||
| CN105392884A | 2016-03-09 | |||
| CN101861318A | 2010-10-13 | |||
| US20110059014A1 | 2011-03-10 | |||
| CN102702265A | 2012-10-03 |
Attorney, Agent or Firm:
SHANGHAI BESHINING LAW OFFICE (CN)
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