发明名称 |
Directed synthesis of oligophosphoramidate stereoisomers |
摘要 |
The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.
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申请公布号 |
US8569515(B2) |
申请公布日期 |
2013.10.29 |
申请号 |
US201113099630 |
申请日期 |
2011.05.03 |
申请人 |
HEINDL DIETER;KESSLER DIRK;ROESLER ANGELIKA;SEIDEL CHRISTOPH;THUER WILMA;ROCHE DIAGNOSTICS OPERATIONS, INC. |
发明人 |
HEINDL DIETER;KESSLER DIRK;ROESLER ANGELIKA;SEIDEL CHRISTOPH;THUER WILMA |
分类号 |
C07F9/24 |
主分类号 |
C07F9/24 |
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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