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公开(公告)号：US06894158B2
公开(公告)日：2005-05-17
申请号：US10373336
申请日：2003-02-24
IPC分类号： C12N15/09 , C07B61/00 , C07H19/073 , C07H19/10 , C07H19/173 , C07H19/20 , C07H21/00
摘要： Provided are methods of producing phosphitylated compounds, including 3′-O-phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of: (1) acid-base complexes derived from an amine base of Formula I wherein R, R1, and R2 are independently C1-C10 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, C7-C10 aralkyl, C1-C10 heteroalkyl, or C1-C10 heteroaryl, wherein any two adjacent R, R1, and R2 may be connected to form a heterocyclic ring; (2) acid-base complexes derived from a diazabicyclo amine base; and (3) combinations of two or more thereof.
摘要翻译： 提供了生产磷酸化化合物（包括3'-O-亚磷酰胺）的方法，包括在磷酸化活化剂存在下使含羟基的化合物与磷酸化剂反应的步骤，所述磷化活化剂选自：（1）酸碱 衍生自式I的胺碱的络合物，其中R 1，R 2和R 2独立地为C 1 -C 10烷基， C 1 -C 6烷基，C 3 -C 10环烷基，C 6 -C 10芳基，C
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公开(公告)号：US20060178509A1
公开(公告)日：2006-08-10
申请号：US11053733
申请日：2005-02-08
申请人： Kalakota Reddy
发明人： Kalakota Reddy
IPC分类号： C07H21/04
摘要： The present invention provides an improved phosphoramidite activator comprising a solution of 5-benzylmercaptotetrazole in acetonitrile and N-alkyimidazole. Further provided are improved methods of oligonucleotide synthesis wherein a phosphoramidite activator comprising a solution of 5-benzylmercaptotetrazole in acetonitrile and N-alkyimidazole is used to prepare internucleoside linkages.
摘要翻译： 本发明提供了一种改进的亚磷酰胺活化剂，其包括5-苄基巯基四唑在乙腈和N-烷基咪唑中的溶液。 还提供了寡核苷酸合成的改进方法，其中使用包含5-苄基巯基四唑在乙腈和N-烷基咪唑中的溶液的亚磷酰胺活化剂来制备核苷间键。
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公开(公告)号：US20050124804A1
公开(公告)日：2005-06-09
申请号：US10990138
申请日：2004-11-16
IPC分类号： C12N15/09 , C07B61/00 , C07H19/073 , C07H19/10 , C07H19/173 , C07H19/20 , C07H21/04
摘要： Provided are methods of producing phosphitylated compounds, including 3′-O-phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of: (1) acid-base complexes derived from an amine base of Formula II wherein R3, R4, R5, R6, and R7 are independently hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, C7-C10 aralkyl, C1-C10 heteroalkyl, or C1-C10 heteroaryl, and at least one of R3, R4, R5, R6, and R7 is not hydrogen; (2) zwitterionic amine complexes; and (3) combinations of two or more thereof, to produce a phosphitylated compound. Further provided are methods for purifying phosphitylated compounds comprising the steps of providing a phosphitylated compound in a solution solvent, contacting said phosphitylated compound with a precipitation solvent, and precipitating said phosphitylated compound
摘要翻译： 提供了生产磷酸化化合物（包括3'-O-亚磷酰胺）的方法，包括在含磷酸化活化剂存在下使含羟基的化合物与磷酸化剂反应的步骤，所述磷化活化剂选自：（1）酸碱 衍生自式II的胺碱的络合物，其中R 3，R 4，R 5，R 6， R 7独立地是氢，C 1 -C 10烷基，C 3 -C 10烷基，C 1 -C 10烷基，C 3 -C 10烷基， 环烷基，C 6 -C 10芳基，C 7 -C 10芳烷基，C 1 -C 10烷基， 或者C 1 -C 10杂芳基，以及至少一个R 1，R 2，R 2， R 4，R 4，R 5，R 6和R 7不是氢; （2）两性离子胺络合物; 和（3）两种或更多种的组合，以产生磷酸化化合物。 还提供了纯化磷酸化化合物的方法，包括以下步骤：在溶液中提供磷酸化化合物，使所述磷酸化化合物与沉淀溶剂接触，并将所述磷酸化化合物
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