发明名称 |
OLIGORIBONUCLEOSIDE AND OLIGODEOXYRIBONUCLEOSIDE BORANOPHOSPHATES |
摘要 |
<p>A process of making oligoribonucleoside and deoxyribonucleoside boranophosphates and salts thereof is disclosed. The process comprises the steps of condensing a ribonucleotide or deoxyribonucleotide with a nucleoside phosphitylating agent, wherein the phosphitylating agent includes a 5' -OH group protected by an acid-labile protecting group and a moiety bonded to the phosphorus atom therein that is a stronger proton acceptor than the 5'-OH group of the ribonucleotide or deoxyribonucleotide to form a reaction intermediate, then oxidizing the reaction intermediate so formed with a compound comprising a Lewis base and a boron-containing substituent, wherein the Lewis base is a weaker electron donor than the phosphite phosphorus of the reaction intermediate, to form a ribonucleotide or deoxyribonucleotide boranophosphate. These steps are repeated on the nucleotide boranophosphate to form an oligonucleotide boranophosphate.</p> |
申请公布号 |
EP0594578(B1) |
申请公布日期 |
1996.10.09 |
申请号 |
EP19910902200 |
申请日期 |
1990.11.29 |
申请人 |
BORON BIOLOGICALS, INC.;DUKE UNIVERSITY;THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL |
发明人 |
SPIELVOGEL, BERNARD F.;SOOD, ANUP;HALL, IRIS H.;SHAW, BARBARA RAMSAY |
分类号 |
A61K31/69;A61K31/70;A61K31/7135;A61P3/06;A61P29/00;A61P35/00;C07H21/00;C07H21/04;C07H23/00;C12N15/113;C12Q1/68;(IPC1-7):C07H1/00;A61K31/00;A61K48/00 |
主分类号 |
A61K31/69 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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