发明名称 |
2'-O-AMINOOXYMETHYL NUCLEOSIDE DERIVATIVES FOR USE IN THE SYNTHESIS AND MODIFICATION OF NUCLEOSIDES, NUCLEOTIDES AND OLIGONUCLEOTIDES |
摘要 |
Disclosed are O-protected compounds of the formula (I): wherein B is an optionally protected nucleobase, and R1-R3 are as described herein, a method of preparing such compounds, and a method of preparing oligonucleotides such as RNA starting from such compounds. The O-protected compounds have one or more advantages, for example, the 2'-O-protected compound is stable during the various reaction steps involved in oligonucleotide synthesis; the protecting group can be easily removed after the synthesis of the oligonucleotide, for example, by reaction with tetrabutylammonium fluoride; and/or the O-protected groups do not generate DNA/RNA alkylating side products, which have been reported during removal of 2'-O-(2-cyanoethyl)oxymethyl or 2'-O-[2-(4-tolylsulfonyl)ethoxymethyl groups under similar conditions. |
申请公布号 |
US2014051846(A1) |
申请公布日期 |
2014.02.20 |
申请号 |
US201214008805 |
申请日期 |
2012.03.29 |
申请人 |
BEAUCAGE SERGE L.;CIESLAK JACEK;THEUNITED OFAMERICA,ASREPRESENTEDBYTHE SECRE -TARY,DEPARTMENT OFHEALTHAND HUMAN SERVICE |
发明人 |
BEAUCAGE SERGE L.;CIESLAK JACEK |
分类号 |
C07H19/16;C07H1/00;C07H19/048 |
主分类号 |
C07H19/16 |
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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