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11. 发明专利

AT298759T 未知
公开(公告)号：AT298759T
公开(公告)日：2005-07-15
申请号：AT02731195
申请日：2002-03-29
申请人： GILEAD SCIENCES INC
发明人： SZNAIDMAN MARCOS
IPC分类号： C07H19/09 , C07H15/04 , C07H19/06
摘要： The present invention is directed to the process for the preparation of 2'-deoxy-2'-halo-beta-L-arabinofuranosyl nucleosides, and in particular, 2'-deoxy-2'-fluoro-beta-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and less expensive than L-ribose or L-xylose, in ten steps. All of the reagents and starting materials are inexpensive and no special equipment is required to carry out the reactions.

13. 发明公开

EP1720840A4 METHODS TO MANUFACTURE 1,3-DIOXOLANE NUCLEOSIDES 有权
标题翻译：制备1,3-二氧基核糖核苷的方法
公开(公告)号：EP1720840A4
公开(公告)日：2009-01-21
申请号：EP05722747
申请日：2005-02-03
申请人： UNIV EMORY
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

14. 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。

15. 发明专利

CA2554782A1 METHODS TO MANUFACTURE 1,3-DIOXOLANE NUCLEOSIDES 未知
公开(公告)号：CA2554782A1
公开(公告)日：2005-08-18
申请号：CA2554782
申请日：2005-02-03
申请人： UNIV EMORY
发明人： ALMOND MERRICK R , PAINTER GEORGE R , SZNAIDMAN MARCOS , CLEARY DARRYL G , PESYAN AMIR
IPC分类号： C07D239/47 , C07D239/54 , C07D405/04 , C07D473/16
摘要： This aplication provides a process for preparing enantiomerically pure .beta .- D-dioxolane nucleosides. In particular, a new synthesis of (-)-DAPD, suitabl e 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 protecte d .beta.-D or .beta.-L-1,3-dioxolane nucleoside.

16. 发明专利

ES2568467T3 Métodos para la fabricación de nucleósidos de 1,3-dioxolano 未知
公开(公告)号：ES2568467T3
公开(公告)日：2016-04-29
申请号：ES05722747
申请日：2005-02-03
申请人： UNIV EMORY
发明人： SZNAIDMAN MARCOS , PAINTER GEORGE R , ALMOND MERRICK R , CLEARY DARRYL G , PESYAN AMIR
IPC分类号： C07D317/34 , C07D239/47 , C07D239/54 , C07D405/04 , C07D473/16
摘要： Un proceso para preparar un nucleósido de ß-D- o ß-L-1,3-dioxolano sustancialmente puro que comprende: a) Obtener un etanol esterificado de 2,2-dialcoxi de la fórmula (Ia) o el compuesto de la fórmula (Ib): **Fórmula** Donde: cada R1 es independientemente un alquilo, un arilo, un heteroarilo, un heterocíclico, un alcarilo, un alquilheteroarilo o un alquilheterocíclico, o un aralquilo; y R2 es un grupo removible adecuado; b) Ciclizar el etanol esterificado de 2,2-dialcoxi de la fórmula (Ia) o del compuesto de la fórmula (Ib) con ácido glicólico para obtener una lactona de 1,3-dioxolano de la fórmula (II): **Fórmula** c) Resolver la lactona de 1,3-dioxolano de la fórmula (II) para obtener una D- o L-lactona sustancialmente pura; d) Reducir selectivamente con un agente reductor y activar la lactona D- o L- quiral sustancialmente pura para obtener una D- o L-1,3-dioxolana sustancialmente pura de la fórmula (III): **Fórmula** Donde L es un grupo que deja adecuado; e) Acoplar al D- o L-1,3-dioxolano sustancialmente puro de la fórmula (III) a una base purina o pirimidina activada y/o protegida de su derivado para obtener una mezcla α:ß de nucleósidos de D- o L-1,3-dioxolano sustancialmente puros protegidos de la fórmula (IV): donde B es una base purina o pirimidina o su derivado; f) Opcionalmente purificar a la mezcla α:ß de nucleósidos de D- o L-1,3-dioxolano sustancialmente puros y protegidos de la fórmula (IV) para obtener un nucleósido de ß-D- o ß-L-1,3-dioxolano sustancialmente puro y protegido; y g) Opcionalmente desproteger el nucleósido de P-D- o P-L-1,3-dioxolano sustancialmente puro y protegido para obtener un nucleósido de ß-D- o ß-L-1,3-dioxolano sustancialmente puro.

17. 发明专利

CA2340214C METHOD OF MANUFACTURE OF 1,3-OXATHIOLANE NUCLEOSIDES 未知
公开(公告)号：CA2340214C
公开(公告)日：2007-10-30
申请号：CA2340214
申请日：1999-08-12
申请人： TRIANGLE PHARMACEUTICALS INC , UNIV EMORY
发明人： ALMOND MERRICK , LIOTTA DENNIS C , CLEARY DARRYL , PAINTER GEORGE R , SORIA JOSE , SZNAIDMAN MARCOS
IPC分类号： C07D327/04 , A61K31/505 , A61K31/513 , C07D319/06 , C07D411/04 , C07D473/00
摘要： Processes for the preparation of 1,3-oxathiolane nucleosides are provided th at include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

18. 发明专利

CA2340214A1 METHOD OF MANUFACTURE OF 1,3-OXATHIOLANE NUCLEOSIDES 未知
公开(公告)号：CA2340214A1
公开(公告)日：2000-02-24
申请号：CA2340214
申请日：1999-08-12
申请人： TRIANGLE PHARMACEUTICALS INC , UNIV EMORY
发明人： LIOTTA DENNIS C , SZNAIDMAN MARCOS , SORIA JOSE , CLEARY DARRYL , ALMOND MERRICK , PAINTER GEORGE R
IPC分类号： A61K31/505 , C07D319/06 , C07D327/04 , C07D411/04 , C07D473/00
摘要： Processes for the preparation of 1,3-oxathiolane nucleosides are provided th at include efficient methods for the preparation of the 1,3-oxathiolane ring an d subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

19. 发明专利

CA2554782C METHODS TO MANUFACTURE 1,3-DIOXOLANE NUCLEOSIDES 未知
公开(公告)号：CA2554782C
公开(公告)日：2013-08-13
申请号：CA2554782
申请日：2005-02-03
申请人： UNIV EMORY
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
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.

20. 发明专利

BRPI0507363A 未知
公开(公告)号：BRPI0507363A
公开(公告)日：2007-07-03
申请号：BRPI0507363
申请日：2005-02-03
申请人： UNIV EMORY
发明人： SZNAIDMAN MARCOS , PAINTER GEORGE R , ALMOND MERRICK , CLEARY DARRYL G , PESYAN AMIR
IPC分类号： C07D239/47 , C07D239/54 , C07D405/04 , C07D473/16
摘要： This application provides a process for preparing enantiomerically pure &bgr;-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 &bgr;-D- or &bgr;-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 purifying the nucleoside to obtain a substantially pure protected &bgr;-D- or &bgr;-L-1,3-dioxolane nucleoside.

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