公开(公告)号：US06384209B1

公开(公告)日：2002-05-07

申请号：US08979864

申请日：1997-11-26

Applicant: Jin-Yan Tang ,  Zhaoda Zhang

Inventor： Jin-Yan Tang ,  Zhaoda Zhang

IPC: C07H2100

CPC classification number: C07C329/14

Abstract: The invention relates to the chemical synthesis of oligonucleotides and to chemical entities useful in such synthesis. More particularly, the invention relates to sulfurization of the internucleoside linkages of oligonucleotides. The invention provides new sulfur transfer reagents and processes for their use in sulfurizing oligonucleotides. The sulfur transfer reagents according to the invention are inexpensive to make, stable in storage and highly efficient in sulfurization.

Abstract translation: 本发明涉及寡核苷酸的化学合成以及可用于这种合成的化学实体。 更具体地，本发明涉及寡核苷酸的核苷间键的硫化。 本发明提供新的硫转移试剂及其用于硫化寡核苷酸的方法。 根据本发明的硫转移试剂制备成本低，贮存稳定，硫化效率高。

公开(公告)号：US06310198B1

公开(公告)日：2001-10-30

申请号：US09545273

申请日：2000-04-07

Applicant: Jin-Yan Tang ,  Nandkumar Bongle ,  Jose Gonzalez ,  Warren E. Schwartz

Inventor： Jin-Yan Tang ,  Nandkumar Bongle ,  Jose Gonzalez ,  Warren E. Schwartz

IPC: C07H2100

CPC classification number: C07H21/00

Abstract: The present invention comprises an improved method of synthesizing oligonucleotides. The method comprises employing dinucleotides (or “dimer blocks”) as the basic synthetic unit building block. The method results in extremely high purity oligonucleotides in which the N−1 content is very low, generally less than 1-2% of the full length, N, oligonucleotide. We have found that synthesis using dinucleotide phosphorothioates results in oligonucleotides having very little phosphodiester content. Furthermore, we have found that the amount of dimer required in each coupling step can be less than about 6 and is preferably about 2 equivalents. Synthesis of oligonucleotides according to the dimer block approach described herein can also be conducted without the capping step that has heretofore been deemed necessary after each coupling.

Abstract translation: 本发明包括一种合成寡核苷酸的改进方法。 该方法包括使用二核苷酸（或“二聚体嵌段”）作为基本合成单元结构单元。 该方法产生非常高纯度的寡核苷酸，其中N-1含量非常低，通常小于全长N，寡核苷酸的1-2％。 我们已经发现，使用二核苷酸硫代磷酸酯的合成导致寡核苷酸具有非常少的磷酸二酯含量。 此外，我们已经发现，每个偶联步骤中所需的二聚体的量可以小于约6，优选约为2当量。 根据本文所述的二聚体嵌段方法的寡核苷酸的合成也可以在没有在每次偶联之后被认为是必要的封端步骤的情况下进行。

公开(公告)号：US5739314A

公开(公告)日：1998-04-14

申请号：US846124

申请日：1997-04-25

Applicant: Saroj Roy ,  Jin-Yan Tang

Inventor： Saroj Roy ,  Jin-Yan Tang

IPC: C07H19/06 ,  C07H1/00 ,  C07H1/02 ,  C07H11/067

CPC classification number: C07H19/06

Abstract: The present invention provides an improved method of synthesizing 2'-O--R substituted pyrimidine mononucleosides. The method comprises reacting an anhydropyrimidine with magnesium alkoxide in the corresponding alcohol at elevated temperatures to directly produce the 2'-O--R substituted pyrimidine nucleoside product. The method advantageously eliminates several steps from prior art methods, thereby reducing the time and cost of synthesis and increasing the yield of final product.

Abstract translation: 本发明提供合成2'-O-R取代的嘧啶单核苷的改进方法。 该方法包括在升高的温度下使相应的醇中的氢化嘧啶与烷氧基镁反应直接产生2'-O-R取代的嘧啶核苷产物。 该方法有利地消除了与现有技术方法的几个步骤，从而减少了合成的时间和成本，并提高了最终产品的产率。

公开(公告)号：US5403709A

公开(公告)日：1995-04-04

申请号：US958133

申请日：1992-10-06

Applicant: Sudhir Agrawal ,  Jin-Yan Tang

Inventor： Sudhir Agrawal ,  Jin-Yan Tang

IPC: C12N15/09 ,  C12Q1/68 ,  C12P19/34 ,  C01N33/48

CPC classification number: C12Q1/6855 ,  C12Q1/6869 ,  Y10T436/143333

Abstract: The invention relates to synthetic oligonucleotides and more particularly to the determination of nucleotide sequences of synthetic oligonucleotides having non-phosphodiester internucleotide linkages. The invention provides a method for sequencing such modified synthetic oligonucleotides.

Abstract translation: 本发明涉及合成的寡核苷酸，更具体地涉及确定具有非磷酸二酯核苷酸间键的合成寡核苷酸的核苷酸序列。 本发明提供了对这种修饰的合成寡核苷酸进行测序的方法。