发明名称 |
METHODS TO MANUFACTURE 1,3-DIOXOLANE NUCLEOSIDES |
摘要 |
<p>This aplication provides a process for preparing enantiomerically pure beta-D-dioxolane nucleosides. In particular, a new synthesis of (-)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure beta-D or beta-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D-or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifiying the nucleoside to obtain a substantially pure protected beta-D or beta-L-1,3-dioxolane nucleoside.</p> |
申请公布号 |
WO2005074654(A3) |
申请公布日期 |
2005.09.22 |
申请号 |
WO2005US03620 |
申请日期 |
2005.02.03 |
申请人 |
EMORY UNIVERSITY;SZNAIDMAN, MARCOS;PAINTER, GEORGE, R.;ALMOND, MERRICK, R.;CLEARY, DARRYL, G.;PESYAN, AMIR |
发明人 |
SZNAIDMAN, MARCOS;PAINTER, GEORGE, R.;ALMOND, MERRICK, R.;CLEARY, DARRYL, G.;PESYAN, AMIR |
分类号 |
C07D239/47;C07D239/54;C07D405/04;C07D473/16;(IPC1-7):C07D239/47 |
主分类号 |
C07D239/47 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|