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    Alkylation of alcohols, amines, thiols and their derivatives by cyclic sulfate intermediates
    1.
    发明授权
    Alkylation of alcohols, amines, thiols and their derivatives by cyclic sulfate intermediates 失效
    通过环状硫酸盐中间体将醇，胺，硫醇及其衍生物烷基化

    公开(公告)号：US06277982B1

    公开(公告)日：2001-08-21

    申请号：US09378665

    申请日：1999-08-20

    申请人： Allister S. Fraser ,  Muthiah Manoharan ,  Phillip Dan Cook ,  Michael E. Jung ,  Andrew M. Kawasaki

    发明人： Allister S. Fraser ,  Muthiah Manoharan ,  Phillip Dan Cook ,  Michael E. Jung ,  Andrew M. Kawasaki

    IPC分类号： C07H2104

    CPC分类号： C07H19/06 ,  C07H21/00

    摘要： Methods for the alkylation of alcohols, amines and thiols by the use of cyclic sulfates are disclosed. The alkylated sulfates formed are versatile intermediates which may be further elaborated by methods of the invention. In particular, methods for the alkylation of the 2′, 3′ or 5′-hydroxy position of nucleosides and nucleoside analogs with cyclic sulfates to form the 2′, 3′ or 5′-O-alkyl sulfate modified compounds are disclosed. Displacement of the 2′,3′ or 5′-O-sulfate with a nucleophile provides 2′, 3′ or 5′-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.

    摘要翻译： 公开了通过使用环状硫酸盐烷基化醇，胺和硫醇的方法。 形成的烷基化硫酸盐是通用的中间体，其可以通过本发明的方法进一步阐述。 特别地，公开了用环状硫酸盐将核苷和核苷类似物的2'，3'或5'-羟基位置烷基化以形成2'，3'或5'-烷基硫酸酯改性化合物的方法。 具有亲核试剂的2'，3'或5'-硫酸硫酸酯的置换提供了可用于合成具有改善的杂交亲和力和核酸酶抗性的寡聚化合物的2'，3'或5'- O修饰的核苷和核苷类似物。

    Processes and reagents for sulfurization of oligonucleotides
    4.
    发明授权
    Processes and reagents for sulfurization of oligonucleotides 有权
    寡核苷酸硫化的方法和试剂

    公开(公告)号：US08058448B2

    公开(公告)日：2011-11-15

    申请号：US12351605

    申请日：2009-01-09

    申请人： Muthiah Manoharan ,  Michael E. Jung ,  Kallanthottathil G. Rajeev ,  Rajendra K. Pandey ,  Gang Wang

    发明人： Muthiah Manoharan ,  Michael E. Jung ,  Kallanthottathil G. Rajeev ,  Rajendra K. Pandey ,  Gang Wang

    IPC分类号： C07D285/01 ,  C07H21/00

    CPC分类号： C07H21/00 ,  C07H21/04 ,  Y02P20/55

    摘要： The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloramine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.

    摘要翻译： 本发明涉及寡核苷酸合成和纯化的方法和试剂。 本发明的一个方面涉及可用于在寡核苷酸合成中活化亚磷酰胺的化合物。 本发明的另一方面涉及使用本发明的活化剂通过亚磷酰胺方法制备寡核苷酸的方法。 本发明的另一方面涉及硫转移剂。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及通过用本发明的硫转移试剂处理亚磷酸酯制备硫代磷酸酯的方法。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及清除在带有乙腈基保护基团的磷酸酯基团去保护过程中产生的丙烯腈的化合物。 在优选的实施方案中，丙烯腈清除剂是聚合物结合的硫醇。 本发明的另一方面涉及用于将亚磷酸盐氧化成磷酸盐的试剂。 在优选的实施方案中，氧化剂是亚氯酸钠，氯胺或吡啶-N-氧化物。 本发明的另一方面涉及通过退火第一单链寡核苷酸和第二单链寡核苷酸来纯化寡核苷酸以形成双链寡核苷酸的方法; 并对双链寡核苷酸进行色谱纯化。 在优选的实施方案中，色谱纯化是高效液相色谱法。

    Processes and reagents for desilylation of oligonucleotides
    6.
    发明授权
    Processes and reagents for desilylation of oligonucleotides 有权
    寡核苷酸脱乙酰化的方法和试剂

    公开(公告)号：US08063198B2

    公开(公告)日：2011-11-22

    申请号：US12050633

    申请日：2008-03-18

    申请人： Muthiah Manoharan ,  Michael E. Jung ,  Kallanthottathil G. Rajeev ,  Rajendra K. Pandey ,  Gang Wang

    发明人： Muthiah Manoharan ,  Michael E. Jung ,  Kallanthottathil G. Rajeev ,  Rajendra K. Pandey ,  Gang Wang

    IPC分类号： C07H21/00 ,  C07C17/07

    CPC分类号： C07H21/00 ,  C07H21/04 ,  Y02P20/55

    摘要： The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloroamine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.

    摘要翻译： 本发明涉及用于寡核苷酸合成和纯化的方法和试剂。 本发明的一个方面涉及可用于在寡核苷酸合成中活化亚磷酰胺的化合物。 本发明的另一方面涉及使用本发明的活化剂通过亚磷酰胺方法制备寡核苷酸的方法。 本发明的另一方面涉及硫转移剂。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及通过用本发明的硫转移试剂处理亚磷酸酯制备硫代磷酸酯的方法。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及清除在带有乙腈基保护基团的磷酸酯基团去保护过程中产生的丙烯腈的化合物。 在优选的实施方案中，丙烯腈清除剂是聚合物结合的硫醇。 本发明的另一方面涉及用于将亚磷酸盐氧化成磷酸盐的试剂。 在优选的实施方案中，氧化剂是亚氯酸钠，氯胺或吡啶-N-氧化物。 本发明的另一方面涉及通过退火第一单链寡核苷酸和第二单链寡核苷酸来纯化寡核苷酸以形成双链寡核苷酸的方法; 并对双链寡核苷酸进行色谱纯化。 在优选的实施方案中，色谱纯化是高效液相色谱法。

    Processes and Reagents for Desilylation of Oligonucleotides
    8.
    发明申请
    Processes and Reagents for Desilylation of Oligonucleotides 有权
    寡核苷酸脱甲酰化的方法和试剂

    公开(公告)号：US20090005549A1

    公开(公告)日：2009-01-01

    申请号：US12050633

    申请日：2008-03-18

    申请人： Muthiah Manoharan ,  Michael E. Jung ,  Kallanthottathil G. Rajeev ,  Rajendra K. Pandey ,  Gang Wang

    发明人： Muthiah Manoharan ,  Michael E. Jung ,  Kallanthottathil G. Rajeev ,  Rajendra K. Pandey ,  Gang Wang

    IPC分类号： C07H19/00

    CPC分类号： C07H21/00 ,  C07H21/04 ,  Y02P20/55

    摘要： The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloroamine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.

    摘要翻译： 本发明涉及寡核苷酸合成和纯化的方法和试剂。 本发明的一个方面涉及可用于在寡核苷酸合成中活化亚磷酰胺的化合物。 本发明的另一方面涉及使用本发明的活化剂通过亚磷酰胺方法制备寡核苷酸的方法。 本发明的另一方面涉及硫转移剂。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及通过用本发明的硫转移试剂处理亚磷酸酯制备硫代磷酸酯的方法。 在优选的实施方案中，硫转移剂是3-氨基-1,2,4-二噻唑烷-5-酮。 本发明的另一方面涉及清除在带有乙腈基保护基团的磷酸酯基团去保护过程中产生的丙烯腈的化合物。 在优选的实施方案中，丙烯腈清除剂是聚合物结合的硫醇。 本发明的另一方面涉及用于将亚磷酸盐氧化成磷酸盐的试剂。 在优选的实施方案中，氧化剂是亚氯酸钠，氯胺或吡啶-N-氧化物。 本发明的另一方面涉及通过退火第一单链寡核苷酸和第二单链寡核苷酸来纯化寡核苷酸以形成双链寡核苷酸的方法; 并对双链寡核苷酸进行色谱纯化。 在优选的实施方案中，色谱纯化是高效液相色谱法。