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    Process for asymmetric intramolecular [3+2] cyclo-addition of hydrazones
    5.
    发明授权
    Process for asymmetric intramolecular [3+2] cyclo-addition of hydrazones 有权
    腙的不对称分子内[3 + 2]环加成方法

    公开(公告)号：US07351831B2

    公开(公告)日：2008-04-01

    申请号：US10507309

    申请日：2003-03-11

    申请人： Shu Kobayashi ,  Yasuhiro Yamashita ,  Haruro Ishitani

    发明人： Shu Kobayashi ,  Yasuhiro Yamashita ,  Haruro Ishitani

    IPC分类号： C07D471/04

    CPC分类号： C07D231/56

    摘要： An intramolecular [3+2] cycloaddition reaction of a hydrazone is carried out under a mild condition with a high stereoselectivity and yield by reacting a hydrazone derivative in the presence of an asymmetric catalyst system obtained by mixing a zirconium alkoxide represented by the following formula (I): Zr(OR)4   (I) (wherein R is a hydrocarbon group which may have a substituent) with a binaphthol derivative represented by the following formula (II): (wherein Y1 and Y2 are each identical or different and denote a hydrogen atom or a halogen atom, and at least one of Y1 and Y2 denotes a halogen atom).

    摘要翻译： 腙的分子内[3 + 2]环加成反应在具有高立体选择性的温和条件下进行，并且通过使腙衍生物在由下式表示的锆烷氧化物 I）：<？in-line-formula description =“In-line Formulas”end =“lead”？> Zr（OR）4（I）<？in-line-formula description =“ （其中R是可以具有取代基的烃基）与下式（II）表示的联萘酚衍生物：（其中Y 1和X 2） Y 2各自相同或不同，表示氢原子或卤素原子，Y 1和Y 2中的至少一个表示一个 卤素原子）。

    Process for asymmetric intramolecular [3+2] cyclo-addition of hydrazones
    6.
    发明申请
    Process for asymmetric intramolecular [3+2] cyclo-addition of hydrazones 有权
    腙的不对称分子内[3 + 2]环加成方法

    公开(公告)号：US20050165237A1

    公开(公告)日：2005-07-28

    申请号：US10507309

    申请日：2003-03-11

    申请人： Shu Kobayashi ,  Yasuhiro Yamashita ,  Haruro Ishitani

    发明人： Shu Kobayashi ,  Yasuhiro Yamashita ,  Haruro Ishitani

    IPC分类号： C07D231/56 ,  C07F7/28 ,  C07D471/02

    CPC分类号： C07D231/56

    摘要： An intramolecular [3+2] cycloaddition reaction of a hydrazone is carried out under a mild condition with a high stereoselectivity and yield by reacting a hydrazone derivative in the presence of an asymmetric catalyst system obtained by mixing a zirconium alkoxide represented by the following formula (I): Zr(OR)4   (I) (wherein R is a hydrocarbon group which may have a substituent) with a binaphthol derivative represented by the following formula (II): (wherein Y1 and Y2 are each identical or different and denote a hydrogen atom or a halogen atom, and at least one of Y1 and Y2 denotes a halogen atom).

    摘要翻译： 腙的分子内[3 + 2]环加成反应在具有高立体选择性的温和条件下进行，并且通过使腙衍生物在由下式表示的锆烷氧化物 I）：<？in-line-formula description =“In-line Formulas”end =“lead”？> Zr（OR）4（I）<？in-line-formula description =“ （其中R是可以具有取代基的烃基）与下式（II）表示的联萘酚衍生物：（其中Y 1和X 2） Y 2各自相同或不同，表示氢原子或卤素原子，Y 1和Y 2中的至少一个表示一个 卤素原子）。

    Process for producing nitrogenous 5-membered cyclic compound
    8.
    发明申请
    Process for producing nitrogenous 5-membered cyclic compound 有权
    生产含氮五元环化合物的方法

    公开(公告)号：US20070191614A1

    公开(公告)日：2007-08-16

    申请号：US10592139

    申请日：2005-02-21

    申请人： Shu Kobayashi ,  Yasuhiro Yamashita

    发明人： Shu Kobayashi ,  Yasuhiro Yamashita

    IPC分类号： C07D231/06

    CPC分类号： C07B53/00 ,  C07D231/04 ,  C07D231/06 ,  C07D401/06

    摘要： A method of the intramolecular and intermolecular cyclization of an N-acylhydrazone for obtaining a pyrazoline skeleton or pyrazolidine skeleton under ordinary conditions with high stereoselectivity and in high yield. An N-acylhydrazone represented by the following formula (I): (wherein R1 and R2 are the same or different and each represents hydrogen or a hydrocarbon group and Ar represents an optionally substituted aromatic hydrocarbon group) is converted to an N-acylpyrazoline derivative with high stereoselectivity in the presence of a Lewis acid catalyst or asymmetric Lewis acid catalyst.

    摘要翻译： 用于获得吡唑啉骨架或吡唑烷骨架的N-酰腙的分子内和分子间环化的方法，在具有高立体选择性和高收率的常规条件下。 由下式（I）表示的N-酰腙：（其中R 1和R 2相同或不同，各自表示氢或烃基，Ar表示任选取代的芳族烃基）转化成N-酰基吡唑啉衍生物， 在路易斯酸催化剂或不对称路易斯酸催化剂存在下具有高立体选择性。

    Process for producing nitrogenous 5-membered cyclic compound
    10.
    发明授权
    Process for producing nitrogenous 5-membered cyclic compound 有权
    生产含氮五元环化合物的方法

    公开(公告)号：US07705161B2

    公开(公告)日：2010-04-27

    申请号：US10592139

    申请日：2005-02-21

    申请人： Shu Kobayashi ,  Yasuhiro Yamashita

    发明人： Shu Kobayashi ,  Yasuhiro Yamashita

    IPC分类号： C07D231/06

    CPC分类号： C07B53/00 ,  C07D231/04 ,  C07D231/06 ,  C07D401/06

    摘要： A method of the intramolecular and intermolecular cyclization of an N-acylhydrazone for obtaining a pyrazoline skeleton or pyrazolidine skeleton under ordinary conditions with high stereoselectivity and in high yield. An N-acylhydrazone represented by the following formula (I): (wherein R1 and R2 are the same or different and each represents hydrogen or a hydrocarbon group and Ar represents an optionally substituted aromatic hydrocarbon group) is converted to an N-acylpyrazoline derivative with high stereoselectivity in the presence of a Lewis acid catalyst or asymmetric Lewis acid catalyst.

    摘要翻译： 用于获得吡唑啉骨架或吡唑烷骨架的N-酰腙的分子内和分子间环化的方法，在具有高立体选择性和高收率的常规条件下。 由下式（I）表示的N-酰腙：（其中R 1和R 2相同或不同，各自表示氢或烃基，Ar表示任选取代的芳族烃基）转化成N-酰基吡唑啉衍生物， 在路易斯酸催化剂或不对称路易斯酸催化剂存在下具有高立体选择性。