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一种apratoxin类海洋天然产物Dtena修饰片段的合成方法

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摘要

本发明涉及一种apratoxin类海洋天然产物Dtena修饰片段的合成方法，属于化学合成领域。本发明通过烯醇硼醚和醛的adol反应制备beta-羟基酮，通过其羟基的Troc保护反应和硅醚脱保护反应制备O-Troc醇，通过该醇与N-Fmoc？脯氨酸的偶联反应制备含脯氨酸结构单元的邻O-Bz基酮，通过该酮的O-Bz脱保护反应和新生成的邻羟基酮的氧化反应合成apratoxin类海洋天然产物的Dtena修饰片段（见附图）。本发明具有反应步骤少、总收率高、产物选择性好、适合工业化生产等特点。

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公开/公告号CN105481746A

专利类型发明专利
公开/公告日2016-04-13

原文格式PDF
申请/专利权人哈尔滨工业大学(威海);
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申请/专利号CN201510804489.2
发明设计人李惠静;王龙飞;吴彦超;
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申请日2015-11-20
分类号C07D207/16;
代理机构
代理人
地址 264209 山东省威海市高区文化西路2号
入库时间 2023-12-18 15:16:23

法律信息

法律状态公告日

法律状态信息

法律状态
2019-01-18

发明专利申请公布后的驳回 IPC(主分类):C07D207/16 申请公布日:20160413 申请日:20151120

发明专利申请公布后的驳回
2016-05-11

实质审查的生效 IPC(主分类):C07D207/16 申请日:20151120

实质审查的生效
2016-04-13

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1. 一种apratoxin类海洋天然产物Dtena修饰片段的合成方法 [P] . 中国专利： CN105481746A . 2016-04-13
2. 一种海洋天然产物apratoxin E的moCys片段的合成方法 [P] . 中国专利： CN105294519A . 2016-02-03
3. A compound comprising a modified oligonucleotide with a nucleobase sequence consisting of 20 linked nucleosides according to EP-B1-2563920 claim 1 (SEQ ID NO: 80), wherein the modified oligonucleotide comprises: a gap segment consisting of ten linked deoxynucleosides; a 5 'wing segment consisting of five linked nucleosides; and a 3 'wing segment consisting of five linked nucleosides; wherein the gap segment is positioned between the 5 'wing segment and the 3' wing segment, wherein each nucleoside of each wing segment comprises a 2'-O-methoxyethyl sugar; wherein each cytosine of the modified oligonucleotide is a 5-methyl cytosine, and wherein each internucleoside linkage of the modified oligonucleotide is a phosphorothioate linkage; and in particular inotersen; and derivatives thereof, such as salts thereof, including sodium salts, as protected by EP-B1-2563920. [P] . NL300963I9 . 2019-01-16

机译： 6.一种化合物，其包含具有根据20的EP-B1-2563920（SEQ ID NO：80）的具有由20个连接的核苷组成的核碱基序列的修饰的寡核苷酸，其中所述修饰的寡核苷酸包含：由十个连接的脱氧核苷组成的缺口片段;和由五个连接的核苷组成的5'翼区段; 3'翼段由五个连接的核苷组成;其中所述间隙片段位于5'侧翼片段和3'侧翼片段之间，其中每个侧翼片段的每个核苷包含2'-O-甲氧基乙基糖;其中修饰的寡核苷酸的每个胞嘧啶是5-甲基胞嘧啶，并且其中修饰的寡核苷酸的每个核苷间键是硫代磷酸酯键;特别是inotersen;及其衍生物，例如由EP-B1-2563920保护的其盐，包括钠盐。
4. A compound comprising a modified oligonucleotide with a nucleobase sequence consisting of 20 linked nucleosides according to EP-B1-2563920 claim 1 (SEQ ID NO: 80), wherein the modified oligonucleotide comprises: a gap segment consisting of ten linked deoxynucleosides; a 5 'wing segment consisting of five linked nucleosides; and a 3 'wing segment consisting of five linked nucleosides; wherein the gap segment is positioned between the 5 'wing segment and the 3' wing segment, wherein each nucleoside of each wing segment comprises a 2'-O-methoxyethyl sugar; wherein each cytosine of the modified oligonucleotide is a 5-methyl cytosine, and wherein each internucleoside linkage of the modified oligonucleotide is a phosphorothioate linkage; and in particular inotersen; and derivatives thereof, such as salts thereof, including sodium salts, as protected by EP-B1-2563920. [P] . NL300963I1 . 2019-01-08

机译： 6.一种化合物，其包含具有根据20的EP-B1-2563920（SEQ ID NO：80）的具有由20个连接的核苷组成的核碱基序列的修饰的寡核苷酸，其中所述修饰的寡核苷酸包含：由十个连接的脱氧核苷组成的缺口片段;和由五个连接的核苷组成的5'翼区段; 3'翼段由五个连接的核苷组成;其中所述间隙片段位于5'侧翼片段和3'侧翼片段之间，其中每个侧翼片段的每个核苷包含2'-O-甲氧基乙基糖;其中修饰的寡核苷酸的每个胞嘧啶是5-甲基胞嘧啶，并且其中修饰的寡核苷酸的每个核苷间键是硫代磷酸酯键;特别是inotersen;及其衍生物，例如由EP-B1-2563920保护的其盐，包括钠盐。
5. methods for screening for a therapeutic agent, for suppressing the polynucleotide sequence, for treating a non-steroidal cancer, for screening for binding of an agent specifically to a polynucleotide, and for determining whether a patient is at risk for developing or having a non-steroidal cancer, pharmaceutical composition, uses of a therapeutic agent, an antisense molecule or a cell that expresses and / or contains the antisense molecule, at least one of the immunogenic membrane proteins, fragments, derivatives or homologues thereof or from a cell containing and / or expressing at least one of the immunogenic membrane proteins or fragments, derivatives or homologues thereof and an agent or antibody, agent, and kit for identifying a patient at risk of developing or have non-steroidal cancer [P] . BRPI0414446A . 2006-11-14

机译：筛选治疗剂，抑制多核苷酸序列，治疗非甾体类癌症，筛选试剂特异性结合多核苷酸的方法以及确定患者是否处于发展或患有非糖尿病风险的方法类固醇癌，药物组合物，表达和/或含有反义分子的治疗剂，反义分子或细胞，免疫原性膜蛋白，其片段，衍生物或同源物中至少一种或来自含有和/或含有细胞的细胞的用途或表达至少一种免疫原性膜蛋白或其片段，衍生物或同系物以及一种试剂或抗体，试剂和试剂盒，用于鉴定有发生或患有非甾体癌风险的患者