Title:
METHOD FOR PREPARATION OF LNA PHOSPHORAMIDITES
Document Type and Number:
WIPO Patent Application WO2003006475
Kind Code:
A3
Abstract:
The present invention relates to large scale preparation of LNA phosphoramidites using a 2-cyanoethyl-N,N,N',N'-tetra-substituted phosphoramidite and a nucleophilic activator, e.g. 2-cyanoethyl-N,N,N',N'-tetraisopropylphosphoramidite and 4,5-dicyanoimidazole. The method is faster and more cost efficient than previously known methods.
Inventors:
KOCH TROELS (DK)
ROSENBOHM CHRISTOPH (DK)
PEDERSEN DANIEL SEJER (DK)
ROSENBOHM CHRISTOPH (DK)
PEDERSEN DANIEL SEJER (DK)
Application Number:
PCT/DK2002/000488
Publication Date:
February 26, 2004
Filing Date:
July 12, 2002
Export Citation:
Assignee:
SANTARIS PHARMA AS (DK)
KOCH TROELS (DK)
ROSENBOHM CHRISTOPH (DK)
PEDERSEN DANIEL SEJER (DK)
KOCH TROELS (DK)
ROSENBOHM CHRISTOPH (DK)
PEDERSEN DANIEL SEJER (DK)
International Classes:
C07H1/00; C07H19/00; C07H19/10; C07H19/02; C07H19/20; (IPC1-7): C07H1/00; C07H19/02
Domestic Patent References:
| WO1998016540A1 | 1998-04-23 |
Other References:
SATOSHI OBIKA ET AL: "2'-O,4'-C-methylene bridged nucleic acid (2',4'-BNA): Synthesis and triplex-forming properties I", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 9, 2001, pages 1001 - 1011, XP002902764
SATOSHI OBIKA ET AL: "A 2', 4'-Bridged Nucleic Acid containing 2-Pyridone as a Nucleobase: Efficient Recognition of a C-G Interruption by Triplex Formation with a Pyrimidine Motif", ANGEW. CHEM. INT. ED., vol. 40, no. 11, 2001, pages 2079 - 2081, XP002902765
SHOJI HAMAMOTO ET AL: "New Approach to the Synthesis of Deoxyribonucleoside Phosphoramidite Derivatives", CHEMISTRY LETTERS, vol. 8, 1986, pages 1401 - 1404, XP002902766
HAKANSSON A E ET AL: "CONVENIENT SYNTHESES OF 7-HYDROXY-1-(HYDROXYMETHYL)- 3-(THYMIN-1-YL)-2,5-DIOXABICYCLO2.2.1HEPTANES: ALPHA-6-RIBO- AND ALPHA-L-XYLO-CONFIGURED LNA NUCLEOSIDES", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY. EASTON, US, vol. 65, no. 17, 25 August 2000 (2000-08-25), pages 5161 - 5166, XP000973191, ISSN: 0022-3263
SATOSHI OBIKA ET AL: "A 2', 4'-Bridged Nucleic Acid containing 2-Pyridone as a Nucleobase: Efficient Recognition of a C-G Interruption by Triplex Formation with a Pyrimidine Motif", ANGEW. CHEM. INT. ED., vol. 40, no. 11, 2001, pages 2079 - 2081, XP002902765
SHOJI HAMAMOTO ET AL: "New Approach to the Synthesis of Deoxyribonucleoside Phosphoramidite Derivatives", CHEMISTRY LETTERS, vol. 8, 1986, pages 1401 - 1404, XP002902766
HAKANSSON A E ET AL: "CONVENIENT SYNTHESES OF 7-HYDROXY-1-(HYDROXYMETHYL)- 3-(THYMIN-1-YL)-2,5-DIOXABICYCLO2.2.1HEPTANES: ALPHA-6-RIBO- AND ALPHA-L-XYLO-CONFIGURED LNA NUCLEOSIDES", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY. EASTON, US, vol. 65, no. 17, 25 August 2000 (2000-08-25), pages 5161 - 5166, XP000973191, ISSN: 0022-3263
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