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    Stereoselective process for the production of dioxolane nucleoside analogues
    3.
    发明授权
    Stereoselective process for the production of dioxolane nucleoside analogues 有权
    用于生产二氧戊环核苷类似物的立体选择性方法

    公开(公告)号：US07955835B2

    公开(公告)日：2011-06-07

    申请号：US10535235

    申请日：2003-11-18

    申请人： Alex Cimpoia ,  James Joseph LaLonde

    发明人： Alex Cimpoia ,  James Joseph LaLonde

    IPC分类号： C12P41/00

    CPC分类号： C12P17/16 ,  C07D317/32 ,  C12P17/04 ,  C12P17/188 ,  C12P41/005

    摘要： The present invention relates to a process for producing compounds of formula (I) and (VII); said process comprising the steps of: a) subjecting a compound of formula (II) to an enzymatic diastereomeric resolution in the presence of a suitable amount of enzyme chosen from Pig Liver Esterase or Porcine Pancreatic Lipase b) recovering said compounds of formula (I) and (VII). The invention also provides a process for producing compounds of formula (III) and (X); said process comprising the steps of: a) subjecting a compound of formula (IV) to an enzymatic diastereomeric resolution in the presence of a suitable amount of enzyme chosen from Candida Antarctica “A” lipase, Candida Antarctica “B” lipase, Candida Lypolitica Lipase or Rhizomucor Miehei Lipase b) recovering said compound of formula (III) and (X).

    摘要翻译： 本发明涉及制备式（I）和（VII）化合物的方法; 所述方法包括以下步骤：a）在合适量的选自猪肝酯酶或猪胰腺脂肪酶的酶的存在下，使式（II）化合物进行酶促非对映异构体拆分b）回收所述式（I）化合物， 和（Ⅶ）。 本发明还提供了制备式（III）和（X）化合物的方法; 所述方法包括以下步骤：a）在适当量的选自南极假丝酵母“A”脂肪酶，南极假丝酵母“B”脂酶，假单胞菌脂肪酶假丝酵母属脂肪酶的酶的存在下使式（IV）化合物进行酶促非对映异构体拆分 或根瘤菌Miehei脂肪酶b）回收所述式（III）和（X）化合物。

    Stereoselective synthesis of nucleoside analogues
    4.
    发明授权
    Stereoselective synthesis of nucleoside analogues 有权
    核苷类似物的立体选择性合成

    公开(公告)号：US06743910B2

    公开(公告)日：2004-06-01

    申请号：US10370470

    申请日：2003-02-24

    申请人： Alex Cimpoia ,  Yi Fong Wang

    发明人： Alex Cimpoia ,  Yi Fong Wang

    IPC分类号： C07H1900

    CPC分类号： C07D473/00 ,  C07D317/32 ,  C07D405/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/32 ,  C07D473/34

    摘要： The invention is a process for stereoselectively producing a dioxolane nucleoside analogue from an anomeric mixture of &bgr; and &agr; anomers represented by the following formula A or formula B: wherein R is selected from the group consisting of C1-6 alkyl and C6-15 aryl and Bz is benzoyl. The process comprises hydrolyzing said mixture with an enzyme selected from the group consisting of Protease N, Alcalase, Savinase, ChiroCLEC-BL, PS-30, and ChiroCLEC-PC to stereoselectively hydrolyze predominantly one anomer to form a product wherein R1 is replaced with H. The process also includes the step of separating the product from unhydrolyzed starting material. Additionally, the functional group at the C4 position is stereoselectively replaced with a purinyl or pyrimidinyl or derivative thereof.

    摘要翻译： 本发明是由下式A或式B表示的β和α端基异构体的端基异构混合物立体选择性地制备二氧戊环核苷类似物的方法：其中R选自C 1-6烷基和C 6-15芳基， Bz是苯甲酰基。 该方法包括用选自蛋白酶N，Alcalase，Savinase，ChiroCLEC-BL，PS-30和ChiroCLEC-PC的酶水解所述混合物以立体选择性地水解主要一种端基异构体以形成其中R1被H 该方法还包括将产物与未水解的原料分离的步骤。 此外，C4位置的官能团被嘌呤基或嘧啶基或其衍生物立体选择性地取代。

    Stereoselective process for the production of dioxolane nucleoside analogues
    5.
    发明申请
    Stereoselective process for the production of dioxolane nucleoside analogues 有权
    用于生产二氧戊环核苷类似物的立体选择性方法

    公开(公告)号：US20060134763A1

    公开(公告)日：2006-06-22

    申请号：US10535235

    申请日：2003-11-18

    申请人： Alex Cimpoia ,  James Lalonde

    发明人： Alex Cimpoia ,  James Lalonde

    IPC分类号： C12P17/16 ,  C07D473/02 ,  C07D405/04

    CPC分类号： C12P17/16 ,  C07D317/32 ,  C12P17/04 ,  C12P17/188 ,  C12P41/005

    摘要： The present invention relates to a process for producing a compound of formula (I); said process comprising the steps of: a) subjecting a compound of formula (II) to an enzymatic diastereomeric resolution in the presence of a suitable amount of enzyme chosen from Pig Liver Esterase or Porcine Pancreatic Lipase b) recovering said compound of formula (I). The invention also provides a process for producing a compound of formula (III); said process comprising the steps of: a) subjecting a compounds of formula (IV) to an enzymatic diastereomeric resolution in the presence of a suitable amount of enzyme chosen from Candida Antarctica “A” lipase, Candida Antarctica “B”lipase, Candida Lypolitica Lipase or Rhizomucor Miehei Lipase b) recovering said compound of formula (III).

    摘要翻译： 本发明涉及式（I）化合物的制备方法。 所述方法包括以下步骤：a）在合适量的选自猪肝酯酶或猪胰腺脂肪酶的酶的存在下，使式（II）化合物进行酶促非对映异构体拆分b）回收所述式（I）化合物， 。 本发明还提供了制备式（III）化合物的方法; 所述方法包括以下步骤：a）在适当量的选自南极假丝酵母“A”脂肪酶，南极假丝酵母“B”脂肪酶，假单胞菌脂肪酶假丝酵母属脂肪酶的酶的存在下使式（IV）化合物进行酶促非对映异构体拆分 或根瘤菌Miehei脂肪酶b）回收所述式（III）化合物。

    Process for producing dioxolane nucleoside analogues
    6.
    发明申请
    Process for producing dioxolane nucleoside analogues 审中-公开
    生产二氧戊环核苷类似物的方法

    公开(公告)号：US20050085638A1

    公开(公告)日：2005-04-21

    申请号：US10502440

    申请日：2003-01-23

    申请人： Gregory Bydlinski ,  Qing Yu ,  Alex Cimpoia

    发明人： Gregory Bydlinski ,  Qing Yu ,  Alex Cimpoia

    IPC分类号： C07D473/16 ,  C07D317/34 ,  C07D405/04 ,  C07D473/00 ,  C07D473/12 ,  C07D473/14 ,  C07D473/32 ,  C07D473/40 ,  C07D47/02

    CPC分类号： C07D317/34 ,  C07D405/04 ,  C07D473/00 ,  C07D473/16 ,  C07D473/32

    摘要： The present invention relates to a process conducted in a single reaction vessel for producing a dioxolane nucleoside analogue of formula I or a pharmaceutically acceptable salt thereof; the process comprising the steps of adding a Lewis acid, a silylating agent and a non-silylated purine or pyrimidine base or an analogue thereof to a dioxolane of formula II. The invention also provides a process for producing a dioxolane compound of formula III; by reacting a dioxolane compound of formula IV in a suitable solvent in the presence of DIB and I2, using a suitable source of energy.

    摘要翻译： 本发明涉及在用于制备式I的二氧戊环核苷类似物或其药学上可接受的盐的单个反应容器中进行的方法; 该方法包括将路易斯酸，甲硅烷基化剂和非甲硅烷基化嘌呤或嘧啶碱或其类似物加入式II的二氧戊环的步骤。 本发明还提供了制备式III的二氧杂环戊烷化合物的方法; 在合适的溶剂中，在DIB和I 2 N 2存在下，使用合适的能量来使式Ⅳ的二氧戊环化合物反应。

    Process for producing dioxolane nucleoside analogues
    7.
    发明授权
    Process for producing dioxolane nucleoside analogues 有权
    生产二氧戊环核苷类似物的方法

    公开(公告)号：US07442813B2

    公开(公告)日：2008-10-28

    申请号：US11713724

    申请日：2007-03-05

    申请人： Gregory Bydlinski ,  Qing Yu ,  Alex Cimpoia

    发明人： Gregory Bydlinski ,  Qing Yu ,  Alex Cimpoia

    IPC分类号： C07D317/20

    CPC分类号： C07D317/34 ,  C07D405/04 ,  C07D473/00 ,  C07D473/16 ,  C07D473/32

    摘要： The present invention relates to a process conducted in a single reaction vessel for producing a dioxolane nucleoside analogue of formula I or a pharmaceutically acceptable salt thereof; the process comprising the steps of adding a Lewis acid, a silylating agent and a non-silylated purine or pyrimidine base or an analogue thereof to a dioxolane of formula II. The invention also provides a process for producing a dioxolane compound of formula III; by reacting a dioxolane compound of formula IV in a suitable solvent in the presence of DIB and I2, using a suitable source of energy.

    摘要翻译： 本发明涉及在用于制备式I的二氧戊环核苷类似物或其药学上可接受的盐的单个反应容器中进行的方法; 该方法包括将路易斯酸，甲硅烷基化剂和非甲硅烷基化嘌呤或嘧啶碱或其类似物加入式II的二氧戊环的步骤。 本发明还提供了制备式III的二氧杂环戊烷化合物的方法; 在合适的溶剂中，在DIB和I 2 N 2存在下，使用合适的能量来使式Ⅳ的二氧戊环化合物反应。

    Process for producing dioxolane nucleoside analogues
    8.
    发明申请
    Process for producing dioxolane nucleoside analogues 有权
    生产二氧戊环核苷类似物的方法

    公开(公告)号：US20070197784A1

    公开(公告)日：2007-08-23

    申请号：US11713724

    申请日：2007-03-05

    申请人： Gregory Bydlinski ,  Qing Yu ,  Alex Cimpoia

    发明人： Gregory Bydlinski ,  Qing Yu ,  Alex Cimpoia

    IPC分类号： C07D473/10 ,  C07D405/02

    CPC分类号： C07D317/34 ,  C07D405/04 ,  C07D473/00 ,  C07D473/16 ,  C07D473/32

    摘要： The present invention relates to a process conducted in a single reaction vessel for producing a dioxolane nucleoside analogue of formula I or a pharmaceutically acceptable salt thereof; the process comprising the steps of adding a Lewis acid, a silylating agent and a non-silylated purine or pyrimidine base or an analogue thereof to a dioxolane of formula II. The invention also provides a process for producing a dioxolane compound of formula III; by reacting a dioxolane compound of formula IV in a suitable solvent in the presence of DIB and I2, using a suitable source of energy.

    摘要翻译： 本发明涉及在用于制备式I的二氧戊环核苷类似物或其药学上可接受的盐的单个反应容器中进行的方法; 该方法包括将路易斯酸，甲硅烷基化剂和非甲硅烷基化嘌呤或嘧啶碱或其类似物加入式II的二氧戊环的步骤。 本发明还提供了制备式III的二氧杂环戊烷化合物的方法; 在合适的溶剂中，在DIB和I 2 N 2存在下，使用合适的能量来使式Ⅳ的二氧戊环化合物反应。

    Stereoselective synthesis of nucleoside analogues
    9.
    发明授权
    Stereoselective synthesis of nucleoside analogues 有权
    核苷类似物的立体选择性合成

    公开(公告)号：US06541625B2

    公开(公告)日：2003-04-01

    申请号：US09779853

    申请日：2001-02-09

    申请人： Alex Cimpoia ,  Yi Fong Wang

    发明人： Alex Cimpoia ,  Yi Fong Wang

    IPC分类号： C07H1900

    CPC分类号： C07D473/00 ,  C07D317/32 ,  C07D405/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/32 ,  C07D473/34

    摘要： The invention is a process for stereoselectively producing a dioxolane nucleoside analogue from an anomeric mixture of &bgr; and &agr; anomers represented by the following formula A or formula B: wherein R is selected from the group consisting of C1-6 alkyl and C6-15 aryl and Bz is benzoyl. The process comprises hydrolyzing said mixture with an enzyme selected from the group consisting of Protease N, Alcalase, Savinase, ChiroCLEC-BL, PS-30, and ChiroCLEC-PC to stereoselectively hydrolyze predominantly one anomer to form a product wherein R1 is replaced with H. The process also includes the step of separating the product from unhydrolyzed starting material. Additionally, the functional group at the C4 position is stereoselectively replaced with a purinyl or pyrimidinyl or derivative thereof.

    摘要翻译： 本发明是由下式A或式B表示的β和α端基异构体的端基异构混合物立体选择性地制备二氧戊环核苷类似物的方法：其中R选自C 1-6烷基和C 6-15芳基， Bz是苯甲酰基。 该方法包括用选自蛋白酶N，Alcalase，Savinase，ChiroCLEC-BL，PS-30和ChiroCLEC-PC的酶水解所述混合物以立体选择性地水解主要一种端基异构体以形成其中R1被H 该方法还包括将产物与未水解的原料分离的步骤。 此外，C4位置的官能团被嘌呤基或嘧啶基或其衍生物立体选择性地取代。