OLIGONUCLEOTIDE MANUFACTURING METHOD
    3.
    发明申请

    公开(公告)号:US20180291056A1

    公开(公告)日:2018-10-11

    申请号:US16014536

    申请日:2018-06-21

    Abstract: The present invention aims to provide a more stable and efficient method for producing oligonucleotide, particularly, oligonucleotide having various functional groups linked to the 3′-terminal and the like. Efficient production of oligonucleotide becomes possible by a production method of an oligonucleotide represented by the formula (Ia-2) (each symbol is as defined in the DESCRIPTION) and having a functional group at the 3′-terminal, the method including a step of subjecting an oligonucleic acid with 3′-terminal protected by a silyl-protecting group to 3′-terminal-selective deprotection under desilylation conditions that do not affect protecting groups other than the silyl group, subjecting same to phosphitylation conditions with a phosphoramidite reagent that do not affect protecting groups on the oligonucleic acid to give a 3′-terminal-phosphoramidited oligonucleotide represented by the formula (Ia-1) (each symbol is as defined in the DESCRIPTION), and linking a functional group to the 3′-terminal of the 3′-terminal phosphoramidited oligonucleotide directly or via a linker, and the like.

    OLIGONUCLEOTIDE WITH PROTECTED BASE
    4.
    发明申请
    OLIGONUCLEOTIDE WITH PROTECTED BASE 有权
    带保护基的寡核苷酸

    公开(公告)号:US20130267697A1

    公开(公告)日:2013-10-10

    申请号:US13768486

    申请日:2013-02-15

    Abstract: The present invention provides a protected nucleotide for elongation, which can be purified efficiently and in a high yield by a liquid-liquid extraction operation, and can achieve an oligonucleotide production method by a phosphoramidite method.It has been found that the above-mentioned problem can be solved by a particular oligonucleotide comprising a protected base and/or particular oligonucleotide protected by a branched chain-containing aromatic group at 3′-position.

    Abstract translation: 本发明提供了用于延伸的被保护的核苷酸,其可以通过液 - 液萃取操作有效地和高产率地纯化,并且可以通过亚磷酰胺方法实现寡核苷酸制备方法。 已经发现,上述问题可以通过包含受保护碱和/或在3'-位具有支链含芳族基团保护的特定寡核苷酸的特定寡核苷酸来解决。

    OLIGONUCLEOTIDE PRODUCTION METHOD, AND NUCLEOSIDE, NUCLEOTIDE, OR OLIGONUCLEOTIDE

    公开(公告)号:US20180282365A1

    公开(公告)日:2018-10-04

    申请号:US16009533

    申请日:2018-06-15

    Abstract: Oligonucleotides may be produced by a process, including (1) condensing a nucleoside, nucleotide or oligonucleotide (a) or the like wherein a 5′-hydroxy group is not protected and a nucleoside, nucleotide or oligonucleotide (b) wherein a 5′-hydroxy group is protected in a non-polar solvent to give a reaction solution containing a phosphite triester product (c); (3) oxidizing or sulfurizing the phosphite triester product (c) to give a reaction solution containing an oligonucleotide (d) wherein the 5′-hydroxy group is protected; (4) deprotecting the oligonucleotide (d) to give a reaction solution containing an oligonucleotide (e) wherein the 5′-hydroxy group is not protected; and (6) adding a polar solvent to the reaction solution containing the oligonucleotide (e) and purifying the oligonucleotide (e) by solid-liquid separation or extraction.

    Oligonucleotide with protected base
    6.
    发明授权
    Oligonucleotide with protected base 有权
    具有受保护碱基的寡核苷酸

    公开(公告)号:US09371353B2

    公开(公告)日:2016-06-21

    申请号:US14491683

    申请日:2014-09-19

    Abstract: The present invention provides a protected nucleotide for elongation, which can be purified efficiently and in a high yield by a liquid-liquid extraction operation, and can achieve an oligonucleotide production method by a phosphoramidite method.It has been found that the above-mentioned problem can be solved by a particular oligonucleotide comprising a protected base and/or particular oligonucleotide protected by a branched chain-containing aromatic group at 3′-position.

    Abstract translation: 本发明提供了用于延伸的被保护的核苷酸,其可以通过液 - 液萃取操作有效地和高产率地纯化,并且可以通过亚磷酰胺方法实现寡核苷酸制备方法。 已经发现,上述问题可以通过包含受保护碱和/或在3'-位具有支链含芳族基团保护的特定寡核苷酸的特定寡核苷酸来解决。

    MORPHOLINO OLIGONUCLEOTIDE MANUFACTURING METHOD
    7.
    发明申请
    MORPHOLINO OLIGONUCLEOTIDE MANUFACTURING METHOD 有权
    莫比诺寡糖制备方法

    公开(公告)号:US20160076033A1

    公开(公告)日:2016-03-17

    申请号:US14946991

    申请日:2015-11-20

    Abstract: Using a morpholino nucleotide wherein 5′-hydroxy group or a hydroxy group present on the substituent of the 5′-hydroxy group is protected by a protecting group having an alkyl group having not less than 10 and not more than 300 carbon atoms and/or an alkenyl group having not less than 10 and not more than 300 carbon atoms as a starting material, a method capable of efficiently producing the morpholino oligonucleotide in a high yield by a liquid phase synthesis can be provided.

    Abstract translation: 使用存在于5'-羟基的取代基上的5'-羟基或羟基的吗啉代核苷酸被具有不少于10个且不多于300个碳原子的烷基的保护基保护,和/或 可以提供具有不少于10个且不超过300个碳原子的烯基作为原料,可以通过液相合成以高产率有效地制备吗啉代寡核苷酸的方法。

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