METHOD FOR PRODUCING MONOMER FOR SINGLE-STRANDED NUCLEIC ACID MOLECULE

    公开(公告)号:EP3450439A1

    公开(公告)日:2019-03-06

    申请号:EP17789327.8

    申请日:2017-04-17

    IPC分类号: C07F9/572

    摘要: A compound represented by formula (3):

    or an enantiomer thereof, which is a monomer that can be used for the production of a single-stranded nucleic acid molecule capable of suppressing the expression of a target gene, can be obtained by:
    reacting a compound represented by formula (1):

    or an enantiomer thereof with 6-hydroxyhexanoic acid in a solvent in the presence of an additive such as 1-hydroxybenzotriazole and a condensing agent, and then mixing the resultant reaction mixture, water, and a base such as alkali metal hydroxide to produce a compound represented by formula (2) :

    or an enantiomer thereof; and
    reacting the compound represented by formula (2) or an enantiomer thereof with 2-cyanoethyl-N,N,N',N'-tetraisopropylphosphorodiamidite in a solvent in the presence of a coupling activator such as a diisopropylaminetetrazole salt.