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    PROCESS FOR ASYMMETRIC INTRAMOLECULAR (3+2) CYCLO-ADDITION OF HYDRAZONES
    5.
    发明公开
    PROCESS FOR ASYMMETRIC INTRAMOLECULAR (3+2) CYCLO-ADDITION OF HYDRAZONES 有权
    VERFAHREN ZUR ASYMMETRISCHEN INTRAMOLEKULAREN 3 + 2-CYCLOADDITION VON HYDRAZONEN

    公开(公告)号：EP1489072A1

    公开(公告)日：2004-12-22

    申请号：EP03710300.9

    申请日：2003-03-11

    Applicant: Japan Science and Technology Agency

    Inventor： KOBAYASHI, Shu ,  YAMASHITA, Yasuhiro ,  ISHITANI, Haruro

    IPC: C07D231/56

    CPC classification number: C07D231/56

    Abstract: 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 Y 1 and Y 2 are each identical or different and denote a hydrogen atom or a halogen atom, and at least one of Y 1 and Y 2 denotes a halogen atom).

    Abstract translation: 腙的分子内Ä3+ 2u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（I）表示的锆烷氧化物混合得到的不对称催化剂体系存在下反应， ：具有下式（II）表示的联萘酚衍生物的Zr（OR）4（其中R为可具有取代基的烃基）：其中Y 1和Y 2各自相同或相同， 不同，表示氢原子或卤素原子，Y 1和Y 2中的至少一个表示卤素原子）。

    PROCESS FOR PRODUCING NITROGENOUS 5-MEMBERED CYCLIC COMPOUND
    8.
    发明公开
    PROCESS FOR PRODUCING NITROGENOUS 5-MEMBERED CYCLIC COMPOUND 有权
    制造方法氮肥5元环连接

    公开(公告)号：EP1731509A1

    公开(公告)日：2006-12-13

    申请号：EP05710758.3

    申请日：2005-02-21

    Applicant: Japan Science and Technology Agency

    Inventor： KOBAYASHI, Shu ,  YAMASHITA, Yasuhiro

    IPC: C07D231/12 ,  C07B53/00 ,  C07D231/18 ,  C07D231/20 ,  C07D401/06

    CPC classification number: C07B53/00 ,  C07D231/04 ,  C07D231/06 ,  C07D401/06

    Abstract: 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.

    Abstract translation: 的N-酰腙的分子内和分子间环化的用于高立体选择性的普通条件下和在高收率获得吡唑啉骨架或骨架pyrazolidines的方法。 的N-酰腙由下式（I）表示：（worin R1和R2相同或不同，并且各自darstellt氢或烃基，且Ar darstellt到任选substituiertem芳香族烃基）被转化成N- acylpyrazoline衍生物与 高立体选择性在路易斯酸催化剂或不对称的路易斯酸催化剂的存在下进行。

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