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1. 发明公开

KR1020100022470A 올리고뉴클레오타이드의 합성 无效
标题翻译：合成寡核苷酸
公开(公告)号：KR1020100022470A
公开(公告)日：2010-03-02
申请号：KR1020097025932
申请日：2007-11-21
申请人： 기린두스 아게
发明人： 랑게마인놀프 , 홀펠트안드레아스 , 쇤베르거안드레아스 , 키르흐호프크리슈티나 , 그뢰셀올라프
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： A method for preparing an oligonucleotide comprising the steps of a) providing a hydroxyl containing compound having the formula (1), wherein B is a heterocyclic base and the radicals R, Rand Rare as defined in the description; b) reacting said compound with a phosphitylating agent in the presence of an activator having the formula (I) (activator I)), wherein R = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl; R, R= either H or form a 5 to 6-membered ring together; X, X= independently either N or CH; Y = H or Si(R), with R= alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl; B = deprotonated acid; to prepare a phosphitylated compound; c) reacting said phosphitylated compound without isolation with a second compound having the formula (1), wherein R, R, R, B are independently selected, but have the same definition as above in the presence of an activator II selected from the group of imidazole imidazolium salts and mixtures thereof.
摘要翻译：一种制备寡核苷酸的方法，包括以下步骤：a）提供具有式（1）的含羟基化合物，其中B是杂环碱基和如说明书中所定义的基团R，Rand Rare; b）在具有式（I）的活化剂（活化剂I））的存在下使所述化合物与磷酸化剂反应，其中R =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基; R，R = H或一起形成5至6元环; X，X =独立地是N或CH; Y = H或Si（R），其中R =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基; B =去质子酸以制备磷酸化化合物; c）使所述磷化合物化合物与不具有式（1）的第二化合物反应，其中R 1，R 2，R 3，B各自独立地选自但具有与上述相同的定义，在活化剂II的存在下，咪唑咪唑鎓盐及其混合物。

2. 发明公开

KR1020070090019A 4차 헤테로시클릭 활성화제를 사용한 포스피틸화 화합물의합성 无效
标题翻译：使用四元杂环激活剂合成磷酸化合物
公开(公告)号：KR1020070090019A
公开(公告)日：2007-09-04
申请号：KR1020077016163
申请日：2005-12-15
申请人： 기린두스 아게
发明人： 랑에마이놀프 , 쇤베르거안드레아스 , 키르크호프크리스티나 , 그뢰셀올라프 , 오멜첸코나쟈 , 홀펠트안드레아스 , 링크프리츠
IPC分类号： C07D233/58 , C07D233/54 , C07F7/02
CPC分类号： C07H21/04 , B01J31/0271 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/02
摘要： A method for preparing a phosphitylated compound comprising the step of:-reacting a hydroxy! containing compound with a phosphitylating agent in the presence of an activator having the formula (I) wherein R = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl R1, R 2 = either H or form a 5 to 6-membered ring together. X1, X2 = independently either N or CH Y = H or Si(R 4)3, with R4 = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl B = deprotonated acid. The hydroxyl containing compound is preferably a sugar moiety or a nucleoside or an oligomer derived therefrom.
摘要翻译：一种制备磷酸化化合物的方法，包括以下步骤： - 将羟基 - 在具有式（I）的活化剂存在下，含有磷酸化剂的化合物，其中R =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基R 1，R 2 = H或一起形成5至6元环。 X 1，X 2独立地为N或CHY = H或Si（R 4）3，其中R 4 =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基B =去质子化酸。含羟基化合物优选为糖部分或核苷或由其衍生的低聚物。

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