METHOD FOR PREPARING OLIGONUCLEOTIDE BY USING MODIFIED OXIDIZATION PROTOCOL

To provide a method for producing mixed P=O/P=S skeleton oligonucleotide.SOLUTION: A method includes selective oxidation of an intermediate phosphite triester compound of formula I to a phosphodiester compound of formula II according to a scheme using oxidation solution obtained by mixing iodine, or...

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Bibliographische Detailangaben
Hauptverfasser:	JUNG KYEONG EUN, LEONHARD JAITZ, CHOI HONGRIM, KIMU SUN WON, ACHIM GEISER, ALEC FETTES
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	CHEMISTRY DERIVATIVES THEREOF METALLURGY NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY SUGARS
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Beschreibung
Zusammenfassung:	To provide a method for producing mixed P=O/P=S skeleton oligonucleotide.SOLUTION: A method includes selective oxidation of an intermediate phosphite triester compound of formula I to a phosphodiester compound of formula II according to a scheme using oxidation solution obtained by mixing iodine, organic solvent and water, where the oxidation solution is aged for a sufficient time in order to selectively oxidize the phosphite triester compound of formula I into the phosphodiester compound of formula II without oxidizing inter phosphorothioate nucleotide bond.SELECTED DRAWING: None 【課題】混合Ｐ＝Ｏ／Ｐ＝Ｓ骨格オリゴヌクレオチドを製造するための方法を提供する。【解決手段】ヨウ素、有機溶媒および水を混合することによって得られる酸化溶液を用いたスキーム：TIFF2024112974000010.tif43134に従って、式Ｉの中間ホスファイトトリエステル化合物の、式ＩＩのホスホジエステル化合物への選択的酸化を含み、酸化溶液が、ホスホロチオエートヌクレオチド間結合を酸化することなく、式Ｉのホスファイトトリエステル化合物を式ＩＩのホスホジエステル化合物に選択的に酸化するのに十分な時間エイジングされていることを特徴とする、方法に関する。【選択図】なし