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    Process for isomerizing acyclic nucleosides and process for separating purine nucleosides
    1.
    发明授权
    Process for isomerizing acyclic nucleosides and process for separating purine nucleosides 失效
    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。

    Process for producing acyclic nucleosides and process for separating purine nucleosides
    3.
    发明授权
    Process for producing acyclic nucleosides and process for separating purine nucleosides 失效
    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。

    Method for producing &bgr;-D-ribofuranose derivatives or optical isomers thereof
    4.
    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

    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。

    Process for producing purine derivatives
    5.
    发明授权
    Process for producing purine derivatives 失效
    嘌呤衍生物的制备方法

    公开(公告)号：US06245910B1

    公开(公告)日：2001-06-12

    申请号：US09427989

    申请日：1999-10-27

    申请人： Kunisuke Izawa ,  Hiroshi Shiragami ,  Keizo Yamashita

    发明人： Kunisuke Izawa ,  Hiroshi Shiragami ,  Keizo Yamashita

    IPC分类号： C07D47330

    CPC分类号： C07D473/00

    摘要： Purine derivatives in which a desired substituent is introduced into the 9-position only are synthesized by first introducing an easily-removable substituent in the 7-position of a purine base of natural purine nucleosides obtained through fermentation or derivatives thereof, then hydrolyzing the ribose moiety to form purine derivatives having the substituent in the 7-position, subsequently introducing the desired substituent in the 9-position, and then removing the substituent in the 7-position.

    摘要翻译： 其中将所需的取代基引入9-位的嘌呤衍生物仅通过首先在通过发酵或其衍生物获得的天然嘌呤核苷的嘌呤碱基的7-位上引入容易移除的取代基来合成，然后水解核糖部分 以形成在7-位具有取代基的嘌呤衍生物，随后将所需取代基引入9-位，然后除去7-位上的取代基。

    Process for preparing 2',3'-Dideoxy-2',3'-dehydronucleosides
    9.
    发明授权
    Process for preparing 2',3'-Dideoxy-2',3'-dehydronucleosides 失效
    制备2'，3'-二脱氧-2'，3'-脱氢核苷的方法

    公开(公告)号：US5625057A

    公开(公告)日：1997-04-29

    申请号：US295478

    申请日：1994-08-25

    申请人： Hiroshi Shiragami ,  Yumiko Uchida ,  Kunisuke Izawa

    发明人： Hiroshi Shiragami ,  Yumiko Uchida ,  Kunisuke Izawa

    IPC分类号： C07D405/04 ,  C07D403/04 ,  C07H19/06 ,  C07H19/067 ,  C07H1/00 ,  C07H19/073

    CPC分类号： C07D403/04 ,  C07H19/06

    摘要： A process for preparing a 2', 3'-dideoxy-2',3'-didehydropyrimidine nucleoside comprising reacting the pyrimidine ribofuranoside with a trialkyl orthoester to yield the 2',3'-O-alkoxyethylidene derivative; which is reacted with hydrogen bromide in acetic acid or acetyl bromide to yield the 2-deoxy-2'-bromo-3'-acetyl-pyrimidine nucleoside; which is then reduced with zinc to yield the 2',3'-olefin of the pyrimidine nucleoside.

    摘要翻译： 制备2'，3'-二脱氧-2'，3'-二脱氢嘧啶核苷的方法，包括使嘧啶核糖呋喃糖苷与三烷基原酸酯反应得到2'，3'-O-烷氧基亚乙基衍生物; 其与溴化氢在乙酸或乙酰溴中反应，得到2-脱氧-2'-溴-3'-乙酰基 - 嘧啶核苷; 然后用锌还原，得到嘧啶核苷的2'，3'-烯烃。

    Method of purifying 2',3'-dideoxynucleosides
    10.
    发明授权
    Method of purifying 2',3'-dideoxynucleosides 失效
    2'，3'-双脱氧核苷的纯化方法

    公开(公告)号：US5451671A

    公开(公告)日：1995-09-19

    申请号：US76964

    申请日：1993-06-16

    申请人： Hiroshi Shiragami ,  Masayuki Arai ,  Kunisuke Izawa ,  Yutaka Honda ,  Yasuhiro Tanaka ,  Toshihide Yukawa ,  Satoji Takahashi

    发明人： Hiroshi Shiragami ,  Masayuki Arai ,  Kunisuke Izawa ,  Yutaka Honda ,  Yasuhiro Tanaka ,  Toshihide Yukawa ,  Satoji Takahashi

    IPC分类号： C07H1/06 ,  C07H19/04 ,  C07H19/173

    CPC分类号： C07H1/06 ,  C07H19/04

    摘要： A crude 2',3'-dideoxynucleoside compound is purified by extracting with an organic solvent, or crystallizing, the 2',3'-dideoxynucleoside compound from a basic aqueous solution having a pH of not less than 12 containing the same. In another embodiment of purification a basic aqueous solution having a pH of not less than 11 of a crude 2',3'-dideoxynucleoside derivative is brought into contact with a nonpolar porous resin, whereby the derivative is adsorbed on the resin, and then the thus adsorbed derivative is desorbed with an aqueous alcoholic solution.2',3'-Dideoxynucleoside compounds which have utility as anti-AIDS drugs or anti-virus drugs can be isolated and purified in high purity and in high yield from their crude products containing impurities.

    摘要翻译： 粗制的2'，3'-二脱氧核苷化合物通过用有机溶剂萃取，或从含有其的pH不低于12的碱性水溶液中结晶2'，3'-二脱氧核苷化合物而纯化。 在纯化的另一个实施方案中，使粗制的2'，3'-二脱氧核苷衍生物的pH不低于11的碱性水溶液与非极性多孔树脂接触，由此将衍生物吸附在树脂上，然后将 因此吸附的衍生物用含水醇溶液解吸。 具有作为抗艾滋病药物或抗病毒药物的作用的2'，3'-二脱氧核苷化合物可以从其含有杂质的粗产物中以高纯度和高产率分离和纯化。