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    Activators for oligonucleotide synthesis
    2.
    发明授权
    Activators for oligonucleotide synthesis 有权

    公开(公告)号：US06642373B2

    公开(公告)日：2003-11-04

    申请号：US10318628

    申请日：2002-12-12

    Applicant: Muthia Manoharan ,  Vasulinga T. Ravikumar

    Inventor： Muthia Manoharan ,  Vasulinga T. Ravikumar

    IPC: C07H2100

    CPC classification number: C07H21/00 ,  Y02P20/55

    Abstract: The present invention relates to improved methods for the preparation of nucleoside phosphoramidites and oligonucleotides. In one aspect, the methods of the invention are used to prepare phosphitylating reagents using pyridinium salts as activators. In a further aspect, the methods of the invention are used to prepare internucleoside linkages using activators which include at least one pyridinium salt and at least one substituted imidazole. In a further aspect, methods are provided preparation of internucleoside linkages between nucleosides having 2′-substituents using imidazolium or benzimidazolium salts as an activator. In a further aspect, methods are provided preparation of internucleoside linkages between nucleosides having bioreversible protecting group that confers enhanced chemical and biophysical properties, without exocyclic amine protection, using imidazolium or benzimidazolium salts as an activator.

    Process for the synthesis of oligomeric compounds
    4.
    发明授权
    Process for the synthesis of oligomeric compounds 失效
    低聚化合物的合成方法

    公开(公告)号：US6051699A

    公开(公告)日：2000-04-18

    申请号：US68275

    申请日：1998-05-06

    Applicant: Vasulinga T. Ravikumar

    Inventor： Vasulinga T. Ravikumar

    IPC: C12N15/09 ,  C07F9/24 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C07H1/00 ,  C07F9/02

    CPC classification number: C07H21/00 ,  C07F9/2412

    Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, and phosphorodithioate covalent linkages. Also provided are synthetic intermediates useful in the processes.

    Abstract translation: PCT No.PCT / US96 / 18618 Sec。 371日期：1998年5月6日 102（e）1998年5月6日PCT PCT 1996年11月15日PCT公布。 公开号WO97 / 19092 日期1997年5月29日提供合成方法，其中制备具有磷酸二酯，硫代磷酸酯和二硫代磷酸酯共价键的低聚化合物。 还提供了在该方法中有用的合成中间体。

    Methods for synthesis of oligonucleotides
    6.
    发明授权
    Methods for synthesis of oligonucleotides 失效
    合成寡核苷酸的方法

    公开(公告)号：US07273933B1

    公开(公告)日：2007-09-25

    申请号：US09032972

    申请日：1998-02-26

    Applicant: Achim H. Krotz ,  Vasulinga T. Ravikumar

    Inventor： Achim H. Krotz ,  Vasulinga T. Ravikumar

    IPC: C07H21/00 ,  C07H21/04

    CPC classification number: C07H21/00

    Abstract: Improved methods for synthesis of oligonucleotides and other phosphorus-linked oligomers are disclosed. The methods include the use of aromatic solvents, alkyl aromatic solvents, halogenated aromatic solvents, halogenated alkyl aromatic solvents, or aromatic ether solvents to achieve deprotection of protected hydroxyl groups.

    Abstract translation: 公开了用于合成寡核苷酸和其它磷链寡聚物的改进方法。 所述方法包括使用芳香族溶剂，烷基芳香族溶剂，卤代芳香族溶剂，卤代烷基芳香族溶剂或芳香族醚类溶剂，使保护的羟基脱保护。

    Activators for oligonucleotide synthesis
    8.
    发明授权
    Activators for oligonucleotide synthesis 失效
    寡核苷酸合成活化剂

    公开(公告)号：US06846922B1

    公开(公告)日：2005-01-25

    申请号：US09708224

    申请日：2000-11-08

    Applicant: Muthia Manoharan ,  Vasulinga T. Ravikumar

    Inventor： Muthia Manoharan ,  Vasulinga T. Ravikumar

    IPC: C07F9/655 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04

    CPC classification number: C07H21/00 ,  Y02P20/55

    Abstract: The present invention relates to improved methods for the preparation of nucleoside phosphoramidites and oligonucleotides. In one aspect, the methods of the invention are used to prepare phosphitylating reagents using pyridinium salts as activators. In a further aspect, the methods of the invention are used to prepare internucleoside linkages using activators which include at least one pyridinium salt and at least one substituted imidazole. In a further aspect, methods are provided preparation of internucleoside linkages between nucleosides having 2′-substituents using imidazolium or benzimidazolium salts as an activator. In a further aspect, methods are provided preparation of internucleoside linkages between nucleosides having bioreversible protecting group that confers enhanced chemical and biophysical properties, without exocyclic amine protection, using imidazolium or benzimidazolium salts as an activator.

    Abstract translation: 本发明涉及制备核苷亚磷酰胺和寡核苷酸的改进方法。 一方面，本发明的方法用于制备使用吡啶鎓盐作为活化剂的磷酸化试剂。 在另一方面，本发明的方法用于使用包括至少一种吡啶鎓盐和至少一种取代的咪唑的活化剂来制备核苷间键。 在另一方面，提供了使用咪唑鎓或苯并咪唑鎓盐作为活化剂的具有2'-取代基的核苷之间的核苷间键合的制备方法。 在另一方面，提供了使用咪唑鎓或苯并咪唑鎓盐作为活化剂的具有生物可逆保护基团的核苷之间的核苷间键合的制备，其赋予增强的化学和生物物理性质，而不考虑环外胺保护。

    Process for the preparation of oligonucleotide compounds
    9.
    发明授权
    Process for the preparation of oligonucleotide compounds 有权
    寡核苷酸化合物的制备方法

    公开(公告)号：US06649750B1

    公开(公告)日：2003-11-18

    申请号：US09477878

    申请日：2000-01-05

    Applicant: Daniel C. Capaldi ,  Vasulinga T. Ravikumar ,  Douglas L. Cole

    Inventor： Daniel C. Capaldi ,  Vasulinga T. Ravikumar ,  Douglas L. Cole

    IPC: C07H2100

    CPC classification number: C07H21/00 ,  C07B2200/11

    Abstract: Synthetic processes are provided wherein high purity oligomers are prepared using support bound phosphoramidite protocols starting with a nucleoside or larger synthon linked to a support media through a nucleosidic heterocyclic base moiety. Intermediates undergoing depurination at the support linkage site are removed during the wash cycle. Also provided are compositions useful in such processes.

    Abstract translation: 提供了合成方法，其中使用支持结合的亚磷酰胺方案制备高纯度低聚物，起始于通过核苷酸杂环碱基部分与支持介质连接的核苷或更大的合成子。 在洗涤循环期间，在载体连接位点处经历去血的中间体被去除。 还提供了可用于这些方法的组合物。

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