发明名称 |
Modified phosphorous intermediates for providing functional groups on the 5' end of oligonucleotides |
摘要 |
<p>Phosphoramidites of the formula <CHEM> where R is a base-labile protecting group, R<1> and R<2> are individually alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, or aryl of 6 to 20 carbon atoms or are joined together to form with the nitrogen atom a cyclic structure of 4-7 carbon atoms and 0 to 1 annular chalcogen atoms of atomic number 8 to 16, G is a hydrocarbylene group of 1 to 20 carbon atoms and Z is a hydroxy-protected vicinal diol group bound to G by one of the vicinal diol carbon atoms or a disulfide group and bound to G by one of the sulfur atoms of the disulfide group, with the proviso that G is of at least 4 carbon atoms when Z is said disulfide group are used in conventional automated oligonucleotide synthesis to introduce a functional aldehyde or thiol group on the 5 min end of the oligonucleotide to thereby provide a reactive site on the oligonucleotide that may be used to conjugate the oligonucleotide to molecules that contain a free amino group or an electrophilic center reactive with a thiol group.</p> |
申请公布号 |
EP0523978(B1) |
申请公布日期 |
1999.05.12 |
申请号 |
EP19920306477 |
申请日期 |
1992.07.15 |
申请人 |
LA JOLLA PHARMACEUTICAL |
发明人 |
JONES, DAVID S.;HACHMANN, JOHN P.;CONRAD, MICHAEL J.;COUTTS, STEPHEN;LIVINGSTON, DOUGLAS ALAN |
分类号 |
C07C43/178;C07C69/78;C07C323/12;C07D317/20;C07F7/18;C07F9/24;C07F9/553;C07F9/655;C07H21/00;(IPC1-7):C07F9/655;C07F9/146;C07C323/11;C07C69/96;C07D317/36;C07F9/141;C07F9/09;G01N33/543 |
主分类号 |
C07C43/178 |
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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