Oxidation process
AssigneeAvecia Biotechnology Inc.
InventorNanda D Sinha
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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; and b) 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.
Claims18
A process for the preparation of an oligonucleotide having at least one phosphate internucleotide linkage comprising the steps of:
- a) forming a nascent oligonucleotide comprising a phosphorus (III) internucleotide linkage;
- and
- b) 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.
A process for the preparation of an oligonucleotide comprising at least one phosphate internucleotide linkage, the process comprising oxidising a phosphorus (III) internucleotide linkage with aqueous iodine solution 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.
Dependencies are inferred from the claim text.