WO2004108081A3 - Oligonucleotide synthesis with alternative solvents - Google Patents

Oligonucleotide synthesis with alternative solvents Download PDF

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Publication number
WO2004108081A3
WO2004108081A3 PCT/US2004/017083 US2004017083W WO2004108081A3 WO 2004108081 A3 WO2004108081 A3 WO 2004108081A3 US 2004017083 W US2004017083 W US 2004017083W WO 2004108081 A3 WO2004108081 A3 WO 2004108081A3
Authority
WO
WIPO (PCT)
Prior art keywords
oligonucleotide
nucleoside
oligonucleotide synthesis
alternative solvents
triester
Prior art date
Application number
PCT/US2004/017083
Other languages
French (fr)
Other versions
WO2004108081A2 (en
Inventor
Max N Moore
Mark Andrade
Recaldo Carty
Anthony Scozzari
Achim Krotz
Original Assignee
Isis Pharmaceuticals Inc
Max N Moore
Mark Andrade
Recaldo Carty
Anthony Scozzari
Achim Krotz
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Isis Pharmaceuticals Inc, Max N Moore, Mark Andrade, Recaldo Carty, Anthony Scozzari, Achim Krotz filed Critical Isis Pharmaceuticals Inc
Priority to CA2540692A priority Critical patent/CA2540692C/en
Priority to EP04753825A priority patent/EP1660512A4/en
Publication of WO2004108081A2 publication Critical patent/WO2004108081A2/en
Publication of WO2004108081A3 publication Critical patent/WO2004108081A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/04Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical

Abstract

The invention provides for methods of manufacturing an oligonucleotide comprising a pentavalent phosphate triester. In particular, the method comprises providing a 5' blocked-nucleoside, deblocking the 5' blocked-nucleoside to form a 5' OH-nucleoside, coupling the 5' OH-nucleoside with a phosphoramidite to form and oligonucleotide comprising a trivalent phosphite triester; and oxidizing the oligonucleotide comprising a trivalent phosphite triester to the oligonucleotide comprising a pentavalent phosphate triester. In some embodiments, the wash between any of the steps above is with at least one solvent wash comprising a toluene.
PCT/US2004/017083 2003-06-02 2004-06-02 Oligonucleotide synthesis with alternative solvents WO2004108081A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CA2540692A CA2540692C (en) 2003-06-02 2004-06-02 Oligonucleotide synthesis with alternative solvents
EP04753825A EP1660512A4 (en) 2003-06-02 2004-06-02 Oligonucleotide synthesis with alternative solvents

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US47546003P 2003-06-02 2003-06-02
US60/475,460 2003-06-02

Publications (2)

Publication Number Publication Date
WO2004108081A2 WO2004108081A2 (en) 2004-12-16
WO2004108081A3 true WO2004108081A3 (en) 2005-06-02

Family

ID=33511680

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/017083 WO2004108081A2 (en) 2003-06-02 2004-06-02 Oligonucleotide synthesis with alternative solvents

Country Status (4)

Country Link
US (1) US7276599B2 (en)
EP (1) EP1660512A4 (en)
CA (1) CA2540692C (en)
WO (1) WO2004108081A2 (en)

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US7276599B2 (en) 2007-10-02
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EP1660512A4 (en) 2009-12-23

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