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1. 发明授权

US06172226B2 Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions 失效
标题翻译：用于在温和条件下合成和去保护肽核酸的合成子
公开(公告)号：US06172226B2
公开(公告)日：2001-01-09
申请号：US09116793
申请日：1998-07-16
申请人： James M. Coull , Michael Egholm , Richard P. Hodge , Mohamed Ismail , S. B. Rajur
发明人： James M. Coull , Michael Egholm , Richard P. Hodge , Mohamed Ismail , S. B. Rajur
IPC分类号： C07D23910
CPC分类号： C07D239/47 , C07D473/18 , C07D473/34 , C07D473/40 , C07K14/003 , Y02P20/55
摘要： A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.
摘要翻译：公开了一种制备具有能够在温和条件下去除的保护基的新型PNA合成子的方法。通过将具有杂环的外环氨基的氨基甲酸酯保护的新的N-取代的核碱基中间体与氨基酸N-（2-氨基乙基） - 甘氨酸的氨基保护的主链或氨基保护的主链酯偶联来制备PNA合成子。通过本发明的方法，所得的PNA合成子可以具有氨基甲酸酯保护的核碱基和氨基保护的主链的正交保护。 PNA合成子可用于合成肽核酸（PNA）和其他寡聚体如PNA-DNA嵌合体，并可用于自动合成仪中。还公开了新的组合物。此外，公开了具有不受保护的C6羰基的环外2-氨基的选择性氨基甲酸酯保护的鸟嘌呤PNA合成子。

2. 发明授权

US5756707A Method of making 2'-O-alkyl pyrimidine ribonucleosides 失效
标题翻译： 2'-O-烷基嘧啶核糖核苷的制备方法
公开(公告)号：US5756707A
公开(公告)日：1998-05-26
申请号：US355544
申请日：1994-12-13
申请人： Richard P. Hodge , Nanda D. Sinha
发明人： Richard P. Hodge , Nanda D. Sinha
IPC分类号： C07H19/06 , C07H19/10 , C07H21/00
CPC分类号： C07H19/06 , C07H19/10 , C07H21/00
摘要： Method for production of 2'-O-derivatized uridine and cytosine RNA synthons comprising derivatizing the 2'-hydroxyl group of a partially protected cytosine ribonucleoside to preferentially produce a partially protected 2'-O-derivatized nucleoside, which is then either (1) reacted at the 3'-hydroxyl group to produce a 2'-O-derivatized cytosine RNA synthon, or (2) reacted with a hydroxide source to produce a uridine nucleobase by deamination, thereby producing a partially protected 2'-O-derivatized uridine ribonucleoside which can be reacted at its 3'-hydroxyl group to produce a uridine RNA synthon.
摘要翻译：包括衍生化部分保护的胞嘧啶核糖核苷的2'-羟基以优先产生部分保护的2'-O-衍生的核苷的2'-O-衍生的尿苷和胞嘧啶RNA合成子的方法，其然后是（1）在3'-羟基反应生成2'-O-衍生化的胞嘧啶RNA合成子，或（2）与氢氧化物源反应，通过脱氨生成尿苷核碱基，从而产生部分保护的2'-O-衍生的尿苷核糖核苷可以在其3'-羟基反应产生尿苷RNA合成酶。

3. 发明授权

US6133444A Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions 失效
标题翻译：用于在温和条件下合成和去保护肽核酸的合成子
公开(公告)号：US6133444A
公开(公告)日：2000-10-17
申请号：US487666
申请日：1995-06-07
申请人： James M. Coull , Michael Egholm , Richard P. Hodge , Mohamed Ismail , Sharanappa B. Rajur
发明人： James M. Coull , Michael Egholm , Richard P. Hodge , Mohamed Ismail , Sharanappa B. Rajur
IPC分类号： C07D239/47 , C07D239/46 , C07D473/18 , C07D473/34 , C07D473/40 , C07K14/00
CPC分类号： C07D239/47 , C07D473/18 , C07D473/34 , C07D473/40 , C07K14/003 , Y02P20/55
摘要： A method is disclosed for preparing novel purine PNA synthons having protecting groups which may be removed under mild conditions. The purine PNA synthons generally are prepared by coupling purine derivatives having carbamate protection to a protected N-(2-aminoethyl)-glycine backbone. By a method of this invention, purine PNA synthons may have orthogonal protection of the carbamate protected purine and the protected backbone. The purine PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. In practicing methods of the invention, novel compositions of matter also are disclosed. For example, disclosed herein are an adenine PNA synthon having the following formula: ##STR1## and a guanine PNA synthon having the following formula: ##STR2##
摘要翻译：公开了一种制备具有可在温和条件下除去的保护基的新型嘌呤PNA合成子的方法。嘌呤PNA合成酶通常通过将具有氨基甲酸酯保护的嘌呤衍生物与保护的N-（2-氨基乙基） - 甘氨酸主链偶联来制备。通过本发明的方法，嘌呤PNA合成子可具有氨基甲酸酯保护的嘌呤和被保护的主链的正交保护。嘌呤PNA合成子可用于合成肽核酸（PNA）和其它寡聚体如PNA-DNA嵌合体，并可用于自动合成仪中。在本发明的实践方法中，还公开了新的物质组合物。例如，本文公开了具有下式的腺嘌呤PNA合成子和具有下式的鸟嘌呤PNA合成子：

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