Production method of famciclovir and production and crystallization method of intermediate therefor
    1.
    发明授权
    Production method of famciclovir and production and crystallization method of intermediate therefor 失效
    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

    IPC分类号: C30B2500

    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。

    INOSINE DERIVATIVES AND PRODUCTION METHODS THEREFOR
    3.
    发明申请
    INOSINE DERIVATIVES AND PRODUCTION METHODS THEREFOR 失效
    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

    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。

    Inosine derivatives and production methods therefor
    4.
    发明授权
    Inosine derivatives and production methods therefor 失效
    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

    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。

    Inosine derivatives and production methods therefor
    6.
    发明授权
    Inosine derivatives and production methods therefor 有权
    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

    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。

    Method for producing &bgr;-D-ribofuranose derivatives or optical isomers thereof
    7.
    发明授权
    Method for producing &bgr;-D-ribofuranose derivatives or optical isomers thereof 失效
    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

    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。

    Production method of fluorinated purine nucleoside derivative, intermediate therefor and production method thereof
    8.
    发明申请
    Production method of fluorinated purine nucleoside derivative, intermediate therefor and production method thereof 审中-公开
    氟化嘌呤核苷衍生物的制备方法及其制备方法

    公开(公告)号:US20070179290A1

    公开(公告)日:2007-08-02

    申请号:US11341453

    申请日:2006-01-30

    IPC分类号: C07H19/16 C07D498/22

    CPC分类号: C07D513/22

    摘要: Purine nucleosides which are fluorinated at the 3′-position (preferably the α-position), may be economically and efficiently produced by fluorinating a novel purine nucleoside derivative (1) in which the hydroxyl group at the 5′-position is protected to obtain a novel purine nucleoside derivative (2) in a high yield. The derivative (2) is subjected to desulfurization, deprotection of R1 and, as necessary protection, deprotection, or modification of nucleic acid base moiety, to obtain the desired purine nucleoside (3). wherein each symbol is as defined in the specification.

    摘要翻译: 通过氟化新的嘌呤核苷衍生物(1)可以经济有效地产生在3'-位(优选α位置)氟化的嘌呤核苷,其中5位的羟基被保护以获得 一种新型嘌呤核苷衍生物(2),产率高。 将衍生物(2)进行脱硫,R 1脱保护,根据需要保护,脱保护或修饰核酸碱基部分,得到所需的嘌呤核苷(3)。 其中每个符号如说明书中所定义。

    Inosine derivatives and production methods therefor
    9.
    发明申请
    Inosine derivatives and production methods therefor 有权
    肌苷衍生物及其制备方法

    公开(公告)号:US20060094870A1

    公开(公告)日:2006-05-04

    申请号:US11304675

    申请日:2005-12-16

    IPC分类号: C07D473/02 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。

    Process for the production of purine nucleoside compounds
    10.
    发明申请
    Process for the production of purine nucleoside compounds 审中-公开
    生产嘌呤核苷化合物的方法

    公开(公告)号:US20050171126A1

    公开(公告)日:2005-08-04

    申请号:US11016741

    申请日:2004-12-21

    CPC分类号: C07H1/00 C07H19/16

    摘要: 2′,3′-didehydro-2′,3′-dideoxypurine nucleoside compounds and 2′,3′-dideoxypurine nucleoside compounds may be produced efficiently by treating a 3′-deoxy-3′-bromopurine nucleoside compound with a perfluoroalkanesulfonyl fluoride in the presence of a base to give a 2′,3′-didehydro-2′,3′-dideoxypurine nucleoside compound, which may be converted to a 2′,3′-dideoxypurine nucleoside compound, by catalytic hydrogenation.

    摘要翻译: 通过用全氟烷基磺酰氟处理3'-脱氧-3'-溴嘌呤核苷化合物可以有效地制备2',3'-二脱氢-2',3'-脱氨基嘌呤核苷化合物和2',3'-脱氧枯草苷核苷化合物 碱的存在得到可通过催化氢化转化为2',3'-脱氧枯草苷核苷化合物的2',3'-二脱氢-2',3'-脱氧枯草苷核苷化合物。