发明名称 |
SYNTHESIS OF beta-L-2-DEOXY NUCLEOSIDES |
摘要 |
An improved process for the preparation of 2'-modified nucleosides and 2'-deoxy-nucleosides, such as, beta-L-2'-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2'-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2' anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2'-anhydro-1-furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2'-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2'-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and/or antineoplastic agents. |
申请公布号 |
WO2005003374(A2) |
申请公布日期 |
2005.01.13 |
申请号 |
WO2004US21281 |
申请日期 |
2004.06.30 |
申请人 |
IDENIX (CAYMAN) LIMITED;STORER, RICHARD;MOUSSA, ADEL;WANG, JING, YANG;CHAUDHURI, NARAYAN;MATHIEU, STEVEN;STEWART, ALISTAIR |
发明人 |
STORER, RICHARD;MOUSSA, ADEL;WANG, JING, YANG;CHAUDHURI, NARAYAN;MATHIEU, STEVEN;STEWART, ALISTAIR |
分类号 |
A61K31/7072;A61K31/7076;C07H13/08;C07H19/00;C07H19/048;C07H19/073;C07H19/22;C12Q |
主分类号 |
A61K31/7072 |
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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