发明名称 |
DISULFONE REAGENTS AND METHODS OF PREPARING AND USING SAME |
摘要 |
The present invention provides novel disulfone compounds and methods of preparing and using those compounds to further prepare biologically relevant <i>gem</i>-disulfone analogs of natural enzyme substrates. Methods of using a variety of disulfone compounds as reagents capable of forming symmetrical and non-symmetrical alpha , beta unsaturated <i>gem</i>-disulfones are also provided. There is also provided a disulfone reagent which reacts with both aromatic and aliphatic aldehydes in good to moderate yield to give exclusively the <i>trans</i> isomer. In accordance with further aspects of the present invention, a methodology for stereospecifically preparing potential <i>gem</i>-disulfone enzyme inhibitors is provided. A synthetic design which allows easy substitution of functional groups so that a number of substrate analogs can be synthesized readily is also provided. In addition, there is provided a new class of compounds which are potential glycosyl transferase inhibitors having characteristics which can inhibit the incorporation of sialic acid and/or fucose into glycoconjugates present at the surface of certain cancer cells. Additionally, a class of potent disulfone-linked catechol-based enzyme inhibitors, such as HIV-1 integrase inhibitors, is provided.
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申请公布号 |
WO0077013(A1) |
申请公布日期 |
2000.12.21 |
申请号 |
WO2000US16463 |
申请日期 |
2000.06.14 |
申请人 |
THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA |
发明人 |
GERVAY-HAGUE, JACQUELYN;HADD, MICHAEL, J. |
分类号 |
C07F9/40;C07F9/655;(IPC1-7):C07F9/40 |
主分类号 |
C07F9/40 |
代理机构 |
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