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    • 26. 发明授权
    • Intermediates for oligonucleotide synthesis
    • 寡核苷酸合成中间体
    • US06329519B1
    • 2001-12-11
    • US09202294
    • 1999-03-15
    • Stephen Paul CollingwoodHeinz Ernst MoserKarl-Heinz AltmannMark Edward Douglas
    • Stephen Paul CollingwoodHeinz Ernst MoserKarl-Heinz AltmannMark Edward Douglas
    • C07H1920
    • C07H19/04Y02P20/55
    • A compound of formula (I) wherein B1 is a radical of a nucleoside base, R1 is hydrogen or a hydroxy-protecting group, R2 is hydrogen, hydroxy or a 2′-nucleoside-modifying atom or group, R3 is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, and Z is halogen or a group of formula (II) where R4 and R5 are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, or R4 is said group and R5 is hydrogen or R4 and R5 together with the nitrogen atom to which they are attached denote a five- to thirteen-membered heterocyclic ring, or Z is a group of formula (III): Nuc-O—, where Nuc is the residue of a natural or synthetic nucleoside or oligonucleotide after removal of a 5′-hydroxyl group therefrom attached through a 5′-methylene thereof to the indicated oxygen atom.
    • 式(I)的化合物,其中B1是核苷碱基的基团,R1是氢或羟基保护基,R2是氢,羟基或2'-核苷修饰的原子或基团,R3是未取代或取代的 C1至C10烷基,C2至C10烯基,C4至C10环烷基烷基,C6至C10芳基或C7至C13芳烷基,Z为卤素或式(Ⅱ)基团,其中R4和R5各自独立地为未取代或取代的C1 C 10至C 10链烯基,C 4至C 10环烷基烷基,C 6至C 10芳基或C 7至C 13芳烷基,或R 4为所述基团,R 5为氢或R 4和R 5与它们所连接的氮原子一起表示 5至13元杂环,或Z为式(III)的基团:Nuc-O-,其中Nuc是除去其中的5'-羟基之后天然或合成的核苷或寡核苷酸的残基,其通过 其指示氧原子的5'-亚甲基。