Process for the preparation of oligonucleotides using modified oxidation protocol
AssigneeHoffmann-La Roche Inc.
InventorsAlec Fettes, Achim Geiser, Leonhard Jaitz, Hongrim Choi, Kyeong Eun Jung, Sung Won Kim
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AssigneeHoffmann-La Roche Inc.
InventorsAlec Fettes, Achim Geiser, Leonhard Jaitz, Hongrim Choi, Kyeong Eun Jung, Sung Won Kim
Estimating the term…
The invention relates to a process for the production of a mixed P═O/P═S backbone oligonucleotide comprising a selective oxidation of an intermediary phosphite triester compound of formula I into a phosphodiester compound of formula II according to the scheme with an oxidation solution obtained by mixing iodine, an organic solvent and water, characterized in that the oxidation solution has been aged for a time period that is sufficient to selectively oxidize the phosphite triester compound of formula I into the phosphodiester compound of formula II without oxidizing the phosphorothioate internucleotide linkages.
A process of selectively oxidizing an intermediary phosphite triester in a mixed phosphodiester/phosphorothioate backbone oligonucleotide comprising:
Dependencies are inferred from the claim text.