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1. 发明授权

US6117993A Synthons for oligonucleotide synthesis 失效
标题翻译：合成寡核苷酸合成
公开(公告)号：US6117993A
公开(公告)日：2000-09-12
申请号：US15472
申请日：1998-01-29
申请人： Radhakrishnan P. Iyer , Dong Yu , Mao-Jun Guo , Sudhir Agrawal
发明人： Radhakrishnan P. Iyer , Dong Yu , Mao-Jun Guo , Sudhir Agrawal
IPC分类号： C07H19/11 , C07H19/10 , C07H19/16 , C07H19/20 , C07H19/213 , C07H21/00 , C07H19/04
CPC分类号： C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00
摘要： The invention provides new reagents and processes for synthesizing oligonucleotides, including stereoselective oligonucleotide synthesis. In a first aspect, the invention provides novel monomer synthons for the synthesis of oligonucleotides. Monomer synthons according to this aspect of the invention are useful in the synthesis of oligonucleotides and can be used in place of the well known beta-cyanoethyl phosphoramidite monomer synthon in the phosphoramidite synthesis procedure. Certain monomer synthons according to this aspect of the invention are useful in this procedure for producing oligonucleotides having defined stereochemistry.In a second aspect, the invention provides processes for synthesizing monomer synthons according to the invention, including diastereomerically enriched or purified monomer synthons. In the processes according to this aspect of the invention, the chemical reactions are stereoretentive so that the products of each reaction retain the same stereoconfiguration as their precursor reagent.In a third aspect, the invention provides processes for synthesizing oligonucleotides using the well known phosphoramidite approach. In the processes according to this aspect of the invention, any of the monomer synthons according to the invention is used in place of the conventional beta-cyanoethyl phosphoramidite.
摘要翻译：本发明提供用于合成寡核苷酸的新试剂和方法，包括立体选择性寡核苷酸合成。在第一方面，本发明提供了用于合成寡核苷酸的新型单体合成子。根据本发明该方面的单体合成子可用于寡核苷酸的合成，并可用于代替在亚磷酰胺合成方法中众所周知的β-氰乙基亚磷酰胺单体合成子。根据本发明该方面的某些单体合成子可用于制备具有确定的立体化学的寡核苷酸的该方法中。在第二方面，本发明提供了合成根据本发明的单体合成子的方法，包括非对映体富集或纯化的单体合成子。在根据本发明的这个方面的方法中，化学反应是立体反应性的，使得每个反应的产物保持与其前体试剂相同的立体构型。在第三方面，本发明提供使用公知的亚磷酰胺方法合成寡核苷酸的方法。在根据本发明的这个方面的方法中，使用根据本发明的任何单体合成物代替常规的β-氰基乙基亚磷酰胺。

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