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公开(公告)号：US20080139802A1
公开(公告)日：2008-06-12
申请号：US11973748
申请日：2007-10-10
申请人： Steven D. Axt , Byoung-Kwon Chun , Qingwu Jin , Suguna Rachakonda , Bruce Ross , Keshab Sarma , Justin Vitale , Jiang Zhu
发明人： Steven D. Axt , Byoung-Kwon Chun , Qingwu Jin , Suguna Rachakonda , Bruce Ross , Keshab Sarma , Justin Vitale , Jiang Zhu
IPC分类号： C07H19/06 , C07H13/04 , C07D307/20
摘要： The present process provides an improved method for converting 2′-deoxy-2′-fluoro-2′-methyl-D-ribonolactones derivatives to 3-fluoro-3-methyl-2-chlorofuran compounds which are useful for the synthesis of nucleosides and improved processes for the synthesis of the D-ribonolactone compounds.
摘要翻译： 本发明提供了将2'-脱氧-2'-氟-2'-甲基-D-核糖内酯衍生物转化成可用于合成核苷的3-氟-3-甲基-2-氯呋喃化合物的改进方法， 用于合成D-核糖内酯化合物的改进方法。
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公开(公告)号：US5198598A
公开(公告)日：1993-03-30
申请号：US732551
申请日：1991-07-19
申请人： Karlheinz Hill , Steven D. Axt , Kenneth J. Weese
发明人： Karlheinz Hill , Steven D. Axt , Kenneth J. Weese
IPC分类号： B01J31/24 , C07B61/00 , C07C41/06 , C07C43/178
CPC分类号： C07C41/06
摘要： Alkadienyl ethers are prepared by the telomerization of conjugated dienes with polyols by continuous addition of the alkadiene to a reaction mixtue comprised of the polyol, secondary alcohol solvent, a portion of the alkadiene to be added, and low palladium catalyst concentration.
摘要翻译： 通过将链二烯连续加入到由多元醇，仲醇溶剂，一部分待加入的链烯二烯和低钯催化剂浓度组成的反应混合物中，通过将共轭二烯与多元醇进行调聚来制备二硬脂基醚。
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公开(公告)号：US20100056770A1
公开(公告)日：2010-03-04
申请号：US12444608
申请日：2007-10-05
申请人： Steven D. Axt , Keshab Sarma , Justin Vitale , Jiang Zhu , Bruce Ross , Suguna Rachakonda , Qingwu Jin , Byoung-kwon Chun
发明人： Steven D. Axt , Keshab Sarma , Justin Vitale , Jiang Zhu , Bruce Ross , Suguna Rachakonda , Qingwu Jin , Byoung-kwon Chun
IPC分类号： C07H19/067
摘要： The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydrox-ymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase.
摘要翻译： 本发明方法提供了制备4-氨基-1 - （（2R，3R，4R，5R）-3-氟-4-羟基-5-羟基 - 甲基-3-甲基 - 四氢 - 呋喃-2-基） 吡啶-2-基）-1H-嘧啶-2-酮，其是丙型肝炎病毒（HCV）NS5B聚合酶的有效抑制剂的式（IV）。
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4.发明授权Process for preparing a 2-(2-amino-1, 6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 有权制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法公开(公告)号：US06340756B1
公开(公告)日：2002-01-22
申请号：US09497319
申请日：2000-02-03
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07D47318
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： wherein Z1 is hydrogen or an amino-protecting group selected from the group consisting of acyl of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms; trityl, optionally substituted with methoxy; and N-(9-fluorenylmethoxycarbonyl); Y1 is halo, aralkyloxy or acyloxy, wherein acyl is as defined above; and Y2 is aralkyloxy. These intermediates are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译： 其中Z1是氢或选自式R-C（O） - 的酰基的氨基保护基，其中R是1-6个碳原子的烷基; 三苯甲基，任选被甲氧基取代; 和N-（9-芴基甲氧基羰基）; Y1是卤素，芳烷氧基或酰氧基，其中酰基如上所定义; 而Y2是芳烷氧基。 这些中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇（更昔洛韦）的单-L-缬氨酸酯的新方法 ）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。
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5.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 有权制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法公开(公告)号：US06218568B1
公开(公告)日：2001-04-17
申请号：US09497538
申请日：2000-02-03
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07C67743
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： Process for preparing intermediates of formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译： 制备式（III）的中间体的方法，其中Y1是酰氧基，其中酰基是式RC（O） - ，其中R是1-6个碳原子的烷基，Y2是芳烷氧基，Z是苯甲酰氧基或酰氧基，其中酰基 式（III）的中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基） - 的单-L-缬氨酸酯的新方法， 甲氧基-1,3-丙二醇（更昔洛韦）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。
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6.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol derivative 失效制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US6040446A
公开(公告)日：2000-03-21
申请号：US127380
申请日：1998-07-31
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07D473/00 , C07D473/18
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： Process and novel intermediates for preparing the L-mono-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process and intermediates provide for reduced impurities in the mono-valine ester end-product and lower overall production costs. The process involves the condensation of a silylated guanine compound with a substituted glycerol derivative and esterification of this product with an L-valine derivative. These mono-valine products are of value as antiviral agents with improved absorption.
摘要翻译： 用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇的L-缬氨酸酯的方法和新型中间体及其药学上可接受的盐。 本方法和中间体提供了单缬氨酸酯最终产物中减少的杂质，降低了总体生产成本。 该方法包括将甲硅烷基化鸟嘌呤化合物与取代的甘油衍生物缩合，并将该产物与L-缬氨酸衍生物酯化。 这些单缬氨酸产品具有改善吸收的抗病毒剂的价值。
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公开(公告)号：US08912321B2
公开(公告)日：2014-12-16
申请号：US12444608
申请日：2007-10-05
申请人： Steven D. Axt , Keshab Sarma , Justin Vitale , Jiang Zhu , Bruce Ross , Suguna Rachakonda , Quingwu Jin , Byoung-Kwon Chun
发明人： Steven D. Axt , Keshab Sarma , Justin Vitale , Jiang Zhu , Bruce Ross , Suguna Rachakonda , Quingwu Jin , Byoung-Kwon Chun
摘要： The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydrofuran-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase.
摘要翻译： 本方法提供了制备4-氨基-1 - （（2R，3R，4R，5R）-3-氟-4-羟基-5-羟甲基-3-甲基 - 四氢呋喃-2-基） （IV）的1H-嘧啶-2-酮，其是丙型肝炎病毒（HCV）NS5B聚合酶的有效抑制剂。
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8.发明授权Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 有权制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法公开(公告)号：US06215017B1
公开(公告)日：2001-04-10
申请号：US09497537
申请日：2000-02-03
申请人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
发明人： Charles A. Dvorak , Douglas L. Wren , Lawrence E. Fisher , Steven D. Axt , Eric R. Humphreys , Humberto B. Arzeno , Colin C. Beard , Sam Linh Nguyen , Yeun-Kwei Han , Christopher R. Roberts , Jan P. Lund , Paul R. Fatheree
IPC分类号： C07C67743
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： Intermediates of Formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译： 式（III）的中间体，其中Y1是酰氧基，其中酰基是式RC（O） - ，其中R是1-6个碳原子的烷基，Y2是芳烷氧基，Z是苯甲酰氧基或酰氧基，其中酰基如所定义 式（III）的中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1的单-L-缬氨酸酯的新方法 ，3-丙二醇（更昔洛韦）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。
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