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1. 发明授权

US06800742B2 Method for producing &bgr;-D-ribofuranose derivatives or optical isomers thereof 失效
标题翻译：制备β-D-呋喃核糖衍生物或其旋光异构体的方法
公开(公告)号：US06800742B2
公开(公告)日：2004-10-05
申请号：US10100909
申请日：2002-03-20
申请人： Yoshihito Koguchi , Takayoshi Torii , Kunisuke Izawa
发明人： Yoshihito Koguchi , Takayoshi Torii , Kunisuke Izawa
IPC分类号： C07H1500
CPC分类号： C07H15/18 , C07H15/04 , C07H19/16
摘要： The present invention provides a method for efficiently producing &bgr;-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series products. The method comprises a step of producing 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate or an optical isomer thereof by allowing &bgr;-D-ribofuranose-1,2,3,5-tetraacetate or an optical isomer thereof to react with a benzyl alcohol in the presence of acid catalysts and a step of hydrolyzing the resulting 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate in the presence of a base to produce 1-O-benzyl-&bgr;-D-ribofuranose or an optical isomer thereof.
摘要翻译：本发明提供了有效生产β-D-呋喃核糖衍生物或其光学异构体的方法，其可用作药物核酸系列产品的合成中间体。该方法包括通过使β-D-呋喃核糖-1,2,3,5-四乙酸酯或其制备方法制备1-O-苄基-β-D-呋喃核糖-2,3,5-三乙酸酯或其旋光异构体的步骤其光学异构体在酸催化剂存在下与苄醇反应，并在碱的存在下水解所得的1-O-苄基-β-D-呋喃核糖-2,3,5-三乙酸酯以产生1 -O-苄基-β-D-呋喃核糖或其旋光异构体。

2. 发明授权

US5688948A Process for isomerizing acyclic nucleosides and process for separating purine nucleosides 失效
标题翻译：非循环核苷异构化方法和嘌呤核苷分离方法
公开(公告)号：US5688948A
公开(公告)日：1997-11-18
申请号：US454567
申请日：1995-05-30
申请人： Kunisuke Izawa , Yoshihito Koguchi , Hiroshi Shiragami , Yumiko Uchida , Satoshi Takamatsu
发明人： Kunisuke Izawa , Yoshihito Koguchi , Hiroshi Shiragami , Yumiko Uchida , Satoshi Takamatsu
IPC分类号： C07D473/00 , C07D473/18 , C07H19/16 , C07D473/06 , C07D473/16 , C07D473/30
CPC分类号： C07D473/00 , C07D473/18 , C07H19/16
摘要： Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar. Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.
摘要翻译：本文公开了一种用于从核糖核苷合成无环型核苷如阿昔洛韦和更昔洛韦的新颖且工业上有利的方法，该方法包括向核糖核苷如鸟苷和无环糖的酯衍生物的溶液中加入酸催化剂和酸酐，并加热混合物，由此在核糖核苷的核糖部分和无环糖的酯衍生物之间发生反缩糖反应。本文还公开了用于分离9-取代嘌呤核苷的工业上有利的方法，其是从核糖核苷合成无环核苷如阿昔洛韦，更昔洛韦等的重要中间体，该方法包括仅将9-异构体从通过冷却溶液或/和通过向其中加入结晶溶剂而含有9-取代的嘌呤核苷和7-取代的嘌呤核苷的溶液或悬浮液。

3. 发明授权

US5336770A Transglycosilation process for producing acyclic nucleosides 失效
标题翻译：用于生产无环核苷的转糖体化方法
公开(公告)号：US5336770A
公开(公告)日：1994-08-09
申请号：US917357
申请日：1992-07-23
申请人： Hiroshi Shiragami , Yoshihito Koguchi , Kunisuke Izawa
发明人： Hiroshi Shiragami , Yoshihito Koguchi , Kunisuke Izawa
IPC分类号： A61K31/52 , A61K31/522 , A61P31/12 , C07D239/26 , C07D239/42 , C07D473/00 , C07D473/18 , C07D473/30 , C07D473/34 , C07H19/16 , C07B43/04
CPC分类号： C07D473/00 , C07D473/18 , C07H19/16
摘要： Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar.
摘要翻译：本文公开了一种用于从核糖核苷合成无环型核苷如阿昔洛韦和更昔洛韦的新颖且工业上有利的方法，该方法包括向核糖核苷如鸟苷和无环糖的酯衍生物的溶液中加入酸催化剂和酸酐，并加热混合物，由此在核糖核苷的核糖部分和无环糖的酯衍生物之间发生反缩糖反应。

4. 发明授权

US5792868A Process for producing acyclic nucleosides and process for separating purine nucleosides 失效
标题翻译：用于生产无环核苷的方法和用于分离嘌呤核苷的方法
公开(公告)号：US5792868A
公开(公告)日：1998-08-11
申请号：US214756
申请日：1994-03-18
申请人： Kunisuke Izawa , Yoshihito Koguchi , Hiroshi Shiragami
发明人： Kunisuke Izawa , Yoshihito Koguchi , Hiroshi Shiragami
IPC分类号： C07D473/00 , C07D473/18 , C07H19/16 , C07D473/16 , C07D473/30 , C07D473/34
CPC分类号： C07D473/00 , C07D473/18 , C07H19/16
摘要： Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar. Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.
摘要翻译：本文公开了一种用于从核糖核苷合成无环型核苷如阿昔洛韦和更昔洛韦的新颖且工业上有利的方法，该方法包括向核糖核苷如鸟苷和无环糖的酯衍生物的溶液中加入酸催化剂和酸酐，并加热混合物，由此在核糖核苷的核糖部分和无环糖的酯衍生物之间发生反缩糖反应。本文还公开了用于分离9-取代嘌呤核苷的工业上有利的方法，其是从核糖核苷合成无环核苷如阿昔洛韦，更昔洛韦等的重要中间体，该方法包括仅将9-异构体从通过冷却溶液或/和通过向其中加入结晶溶剂而含有9-取代的嘌呤核苷和7-取代的嘌呤核苷的溶液或悬浮液。

5. 发明授权

US06761767B2 Production method of famciclovir and production and crystallization method of intermediate therefor 失效
标题翻译：泛昔洛韦的生产方法及其中间体的生产和结晶方法
公开(公告)号：US06761767B2
公开(公告)日：2004-07-13
申请号：US10231249
申请日：2002-08-30
申请人： Toyoto Hijiya , Takayoshi Torii , Kunisuke Izawa
发明人： Toyoto Hijiya , Takayoshi Torii , Kunisuke Izawa
IPC分类号： C30B2500
CPC分类号： C07D473/00 , C07D473/32 , C07D473/40
摘要： An N-9-position alkylated form is selectively precipitated by subjecting a mixture containing the N-9-position alkylated form and an N-7-position alkylated form of 2-amino-6-halopurine to a crystallization step using a mixed solvent of an organic solvent and water. Then, this N-9-position alkylated form is reduced to give famciclovir. By this method of the present invention, famciclovir known as an antiviral agent, and an intermediate compound therefor can be efficiently produced.
摘要翻译：通过使含有N-9位烷基化形式和N-7-位烷基化形式的2-氨基-6-卤代嘌呤的混合物进行结晶步骤，使用以下的混合溶剂将N-9位烷基化形式选择性沉淀：有机溶剂和水。然后，将该N-9-位烷基化形式还原，得到泛昔洛韦。通过本发明的方法，可以有效地制备称为抗病毒剂的泛昔洛韦及其中间体化合物。

6. 发明授权

US06639094B2 Process for producing &agr;-aminoketone derivatives 失效
公开(公告)号：US06639094B2
公开(公告)日：2003-10-28
申请号：US09949614
申请日：1999-09-12
申请人： Tomoyuki Onishi , Takashi Nakano , Naoko Hirose , Takayoshi Torii , Masakazu Nakazawa , Kunisuke Izawa
发明人： Tomoyuki Onishi , Takashi Nakano , Naoko Hirose , Takayoshi Torii , Masakazu Nakazawa , Kunisuke Izawa
IPC分类号： C07C26100
CPC分类号： C07C269/06 , C07C221/00 , C07C227/02 , C07C249/02 , C07C225/06 , C07C225/16 , C07C229/34 , C07C251/04 , C07C251/24 , C07C271/18 , C07C271/22
摘要： A process for producing &agr;-amino-dihalogenated methyl ketone derivatives by reacting an N-protected &agr;-amino acid ester with a dihalomethyl lithium is provided. This process is suitable for the production on an industrial scale and by this process, &agr;-amino-dihalogenated methyl ketone derivatives and &bgr;-amino-&agr;-hydroxycarboxylic acid derivatives can be obtained efficiently and economically advantageously.

7. 发明申请

US20110028706A1 INOSINE DERIVATIVES AND PRODUCTION METHODS THEREFOR 失效
标题翻译：非甾体衍生物及其生产方法
公开(公告)号：US20110028706A1
公开(公告)日：2011-02-03
申请号：US12847399
申请日：2010-07-30
申请人： Takayoshi TORII , Kunisuke Izawa , Doo Ok Jang , Dae Hyan Cho
发明人： Takayoshi TORII , Kunisuke Izawa , Doo Ok Jang , Dae Hyan Cho
IPC分类号： C07H19/16
CPC分类号： C07D473/30 , C07H19/167
摘要： The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
摘要翻译：本发明提供由以下通式（1）表示的肌苷衍生物的制造方法，其特征在于，包括使通式（3）的肌苷衍生物进行二硫代羰基化，进行所得化合物的自由基还原的工序。根据本发明，可以生产用于工业规模的抗艾滋病药物的化合物。其中R 1可以相同或不同，并且各自可以在通式（1）和（3）中具有取代基的苄基，二苯甲基或三苯甲基。

8. 发明授权

US08288526B2 Inosine derivatives and production methods therefor 失效
标题翻译：肌苷衍生物及其制备方法
公开(公告)号：US08288526B2
公开(公告)日：2012-10-16
申请号：US12847399
申请日：2010-07-30
申请人： Takayoshi Torii , Kunisuke Izawa , Doo Ok Jang , Dae Hyan Cho
发明人： Takayoshi Torii , Kunisuke Izawa , Doo Ok Jang , Dae Hyan Cho
IPC分类号： C07H19/173 , C07H19/167 , C07H19/16
CPC分类号： C07D473/30 , C07H19/167
摘要： The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
摘要翻译：本发明提供由以下通式（1）表示的肌苷衍生物的制造方法，其特征在于，包括使通式（3）的肌苷衍生物进行二硫代羰基化，进行所得化合物的自由基还原的工序。根据本发明，可以生产用于工业规模的抗艾滋病药物的化合物。其中R 1可以相同或不同，并且各自可以在通式（1）和（3）中具有取代基的苄基，二苯甲基或三苯甲基。

9. 发明授权

US08252920B2 Inosine derivatives and production methods therefor 有权
公开(公告)号：US08252920B2
公开(公告)日：2012-08-28
申请号：US12847399
申请日：2010-07-30
申请人： Takayoshi Torii , Kunisuke Izawa , Doo Ok Jang , Dae Hyan Cho
发明人： Takayoshi Torii , Kunisuke Izawa , Doo Ok Jang , Dae Hyan Cho
IPC分类号： C07H19/173 , C07H19/167 , C07H19/16
摘要： The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).

10. 发明授权

US07816513B2 Inosine derivatives and production methods therefor 有权
标题翻译：肌苷衍生物及其制备方法
公开(公告)号：US07816513B2
公开(公告)日：2010-10-19
申请号：US11304675
申请日：2005-12-16
申请人： Takayoshi Torii , Kunisuke Izawa , Doo Ok Jang , Dae Hyan Cho
发明人： Takayoshi Torii , Kunisuke Izawa , Doo Ok Jang , Dae Hyan Cho
IPC分类号： C07H19/173 , C07H19/167 , C07H19/16
CPC分类号： C07D473/30 , C07H19/167
摘要： The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
摘要翻译：本发明提供由以下通式（1）表示的肌苷衍生物的制造方法，其特征在于，包括使通式（3）的肌苷衍生物进行二硫代羰基化，进行所得化合物的自由基还原的工序。根据本发明，可以生产用于工业规模的抗艾滋病药物的化合物。其中R 1可以相同或不同，并且各自可以在通式（1）和（3）中具有取代基的苄基，二苯甲基或三苯甲基。

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