发明名称 |
MODIFIED PHOSPHOROUS INTERMEDIATES FOR PROVIDING FUNCTIONAL GROUPS ON THE 5' END OF OLIGONUCLEOTIDES |
摘要 |
MODIFIED PHOSPHOROUS INTERMEDIATES FOR PROVIDING FUNCTIONAL GROUPS ON THE 5' END OF OLIGONUCLEOTIDES Phosphoramidites of the formula where R is a base-labile protecting group, R1 and R2 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' 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. 2P50285.1
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申请公布号 |
CA2073846(A1) |
申请公布日期 |
1993.01.16 |
申请号 |
CA19922073846 |
申请日期 |
1992.07.14 |
申请人 |
LA JOLLA PHARMACEUTICAL COMPANY |
发明人 |
JONES, DAVID S.;HACHMANN, JOHN P.;CONRAD, MICHAEL J.;COUTTS, STEPHEN;LIVINGSTON, DOUGLAS A. |
分类号 |
C07C43/178;C07C69/78;C07C323/12;C07D317/20;C07F7/18;C07F9/24;C07F9/553;C07F9/655;C07H21/00;(IPC1-7):C07H21/04;C08G69/10;C07K14/00;C07C323/16 |
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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