Oxidation process
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United States of America Patent
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Jun 5, 2012
Grant Date -
Jun 3, 2010
app pub date -
Jul 14, 2008
filing date -
Jul 12, 2007
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Abstract
A process for the preparation of an oligonucleotide having at least one phosphate internucleotide linkage I provided. The process comprises the steps of:
- a) forming a nascent oligonucleotide comprising a phosphorus (III) internucleotide linkage; andb) oxidation of the nascent oligonucleotide with aqueous iodine solution thereby to form a phosphorus (V) internucleotide linkage;wherein the oxidation is carried out in the presence of a base, the conjugate acid of said base having a pKa higher than the pKa of the conjugate acid of pyridine. Preferably the base is N-methylimidazole.
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