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    • 4. 发明申请
    • INTERMEDIATES FOR OLIGONUCLEOTIDE SYNTHESIS
    • 寡核苷酸合成的中间体
    • WO1997047636A2
    • 1997-12-18
    • PCT/GB1997001490
    • 1997-06-03
    • NOVARTIS AGCOLLINGWOOD, Stephen, PaulMOSER, Heinz, ErnstALTMANN, Karl-HeinzDOUGLAS, Mark, Edward
    • NOVARTIS AG
    • C07H19/04
    • C07H19/04Y02P20/55
    • A compound of formula (I) where B is a radical of a nucleoside base, R is hydrogen or a hydroxy-protecting group, R is hydrogen, hydroxy or a 2' nucleoside-modifying atom or group, R 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 R and R 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 R is said group and R is hydrogen, or R and R 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B 1是核苷碱基,R 1是氢或羟基保护基,R 2是氢,羟基或2'核苷修饰原子或 基团,R 3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) R 4和R 5各自独立地为未取代或取代的C 1至C 10烷基,C 2至C 10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 和R 5是氢,或者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是式(III)的基团: Nuc-O-,其中Nuc是去除通过其5'亚甲基连接到指定氧原子上的5'-羟基后天然或合成核苷或寡核苷酸的残基。
    • 10. 发明申请
    • INTERMEDIATES FOR OLIGONUCLEOTIDE SYNTHESIS
    • 寡核苷酸合成的中间体
    • WO9747636A3
    • 1998-02-12
    • PCT/GB9701490
    • 1997-06-03
    • NOVARTIS AGCOLLINGWOOD STEPHEN PAULMOSER HEINZ ERNSTALTMANN KARL-HEINZDOUGLAS MARK EDWARD
    • COLLINGWOOD STEPHEN PAULMOSER HEINZ ERNSTALTMANN KARL-HEINZDOUGLAS MARK EDWARD
    • C07H19/06C07H19/04C07H19/16C07H21/00
    • C07H19/04Y02P20/55
    • A compound of formula (I) where B is a radical of a nucleoside base, R is hydrogen or a hydroxy-protecting group, R is hydrogen, hydroxy or a 2' nucleoside-modifying atom or group, R 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 R and R 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 R is said group and R is hydrogen, or R and R 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. 00000
    • 式(I)的化合物,其中B 1是核苷碱基的基团,R 1是氢或羟基保护基,R 2是氢,羟基或2'核苷修饰原子或 基团,R 3为未取代或取代的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 R 4和R 5各自独立地为未取代或取代的C 1至C 10烷基,C 2至C 10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 和R 5是氢,或者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是式(III)的基团: Nuc-O-,其中Nuc是除去其中5'羟基之后的天然或合成核苷或寡核苷酸的残基,其中5'羟基通过其5'亚甲基连接到指定的氧原子上。 00000