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1. 发明申请

WO2005074654A2 METHODS TO MANUFACTURE 1,3-DIOXOLANE NUCLEOSIDES 审中-公开
标题翻译：制备1,3-二氧戊环核苷的方法
公开(公告)号：WO2005074654A2
公开(公告)日：2005-08-18
申请号：PCT/US2005003620
申请日：2005-02-03
申请人： UNIV EMORY , 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
IPC分类号： C07D239/47 , C07D239/54 , C07D405/04 , C07D473/16
CPC分类号： C07D473/16 , C07D317/34 , C07D405/04
摘要： 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.
摘要翻译：该应用提供了制备对映体纯的β-D-二氧戊环核苷的方法。具体来说，描述了适用于大规模开发的（ - ） - DAPD的新合成。在一个实施方案中，本发明提供了制备基本上纯的β-D或β-L-1,3-二氧戊环核苷的方法，其包括a）制备或获得酯化的2,2-二烷氧基乙醇; b）用乙醇酸环化酯化的2,2-二烷氧基乙醇以获得1,3-二氧戊环内酯; c）分解1,3-二氧戊环内酯以获得基本上纯的D-或L-内酯; d）选择性还原和活化D-或L-手性内酯以获得基本上纯的D-或L-1,3-二氧戊环; e）将D-或L-1,3-二氧戊环偶联到活化和/或保护的嘌呤或嘧啶碱基上; 和f）任选纯化核苷以获得基本上纯的受保护的β-D或β-L-1,3-二氧戊环核苷。

3. 发明申请

WO2005074654A3 METHODS TO MANUFACTURE 1,3-DIOXOLANE NUCLEOSIDES 审中-公开
公开(公告)号：WO2005074654A3
公开(公告)日：2005-08-18
申请号：PCT/US2005/003620
申请日：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
IPC分类号： C07D239/47
摘要： This aplication provides a process for preparing enantiomerically pure β-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 β-D or β-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 β-D or β-L-1,3-dioxolane nucleoside.

4. 发明申请

WO2004050613A2 2-SUBSTITUTED-3-PROPENAMIDE DERIVATIVES AND METHODS OF USING THE SAME 审中-公开
标题翻译： 2-取代-3-丙烯酰胺衍生物及其使用方法
公开(公告)号：WO2004050613A2
公开(公告)日：2004-06-17
申请号：PCT/US2003/038233
申请日：2003-12-02
申请人： TRIANGLE PHARMACEUTICALS, INC. , 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
IPC分类号： C07D
CPC分类号： C07D207/325 , C07C235/38 , C07C237/22 , C07D203/18 , C07D205/04 , C07D207/20 , C07D207/24 , C07D207/33 , C07D211/18 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/26 , C07D213/40 , C07D213/75 , C07D213/82 , C07D231/40 , C07D233/06 , C07D233/64 , C07D239/06 , C07D239/26 , C07D239/42 , C07D239/48 , C07D239/52 , C07D241/20 , C07D251/22 , C07D253/07 , C07D261/14 , C07D263/12 , C07D277/04 , C07D277/22 , C07D277/46 , C07D277/58 , C07D285/135 , C07D295/185 , C07D295/205 , C07D307/10 , C07D307/14 , C07D307/20 , C07D307/38 , C07D307/52 , C07D307/56 , C07D307/79 , C07D309/04 , C07D309/20 , C07D317/46 , C07D317/52 , C07D317/62 , C07D317/64 , C07D319/18 , C07D333/12 , C07D333/20 , C07D333/36 , C07D333/44 , C07D401/12 , C07D405/12 , C07D417/12 , C07D491/10
摘要： This invention provides 2-substituted-propenamide derivatives and their compositions for the treament of hepatitis B virus and/or hepatitis D virus.
摘要翻译：本发明提供2-取代的丙烯酰胺衍生物及其用于治疗乙型肝炎病毒和/或丙型肝炎病毒的组合物。

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