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    COMPOSITION CONTAINING CHLOROMETHYL PHOSPHATE DERIVATIVE WITH IMPROVED STABILITY AND METHOD FOR PRODUCING THE SAME
    3.
    发明公开
    COMPOSITION CONTAINING CHLOROMETHYL PHOSPHATE DERIVATIVE WITH IMPROVED STABILITY AND METHOD FOR PRODUCING THE SAME 审中-公开
    与改善稳定性和处理CHLORMETYHLPHOSPHAT衍生物组合物及其

    公开(公告)号：EP2133355A1

    公开(公告)日：2009-12-16

    申请号：EP08721325.2

    申请日：2008-03-05

    申请人： Eisai R&D Management Co., Ltd.

    发明人： SATO, Keizo ,  ABE, Shinya ,  YOSHIZAWA, Kazuhiro ,  WAKASUGI, Kazunori ,  NEGI, Shigeto ,  MIYAZAWA, Mamoru

    IPC分类号： C07F9/09

    CPC分类号： C07F9/025 ,  C07F9/091

    摘要： The present invention provides a process or the like which is employed for producing chloromethyl phosphate derivatives that are useful for producing water-soluble prodrugs, and which are excellent from the points of view of workability, operativity and energy saving. According to the present invention, there is provided a process for producing a composition containing a compound represented by the following formula (I) and a tertiary amine,

    (wherein R1 and R2 are identical or different from each other, and represent a C1-C6 alkyl group, a C2-C6 alkenyl group or a C6-C14 aryl C1-C6 alkyl group which may have a substituent, and R1 and R2 may together form a ring), the proces comprising the step of adding the tertiary amine having a boiling point at 1 atmosphere of 150°C or higher to the compound represented by formula (I).

    摘要翻译： 本发明提供了一个过程或其被用于生产氯甲基磷酸酯衍生物做等所有可用于制备水溶性前药有用的，哪些是从考虑到加工性，操作性及节省能源的点优异。 。根据本发明，提供了一种用于生产含有由以下通式（I）表示的化合物和叔胺，（worin R1和R2是相同的或彼此不同的组合物，并代表C1-C6 烷基，可以具有取代基，并且R1和R2可以一起形成环的C2-C6链烯基或C6-C14芳基C1-C6烷基）时，PROCES包括加入具有沸点的叔胺的步骤 点在1个大气压的150℃或更高，以由式（I）表示的化合物。

    PROCESS FOR PRODUCTION OF HETEROCYCLE-SUBSTITUTED PYRIDINE DERIVATIVE
    9.
    发明公开
    PROCESS FOR PRODUCTION OF HETEROCYCLE-SUBSTITUTED PYRIDINE DERIVATIVE 审中-公开
    HERSTELLUNGSVERFAHRENFÜRHETEROCYCLUS-SUBSTITUIERTES PYRIDINDERIVAT

    公开(公告)号：EP2226320A1

    公开(公告)日：2010-09-08

    申请号：EP08863620.4

    申请日：2008-12-25

    申请人： Eisai R&D Management Co., Ltd.

    发明人： NIIJIMA, Jun ,  YOSHIZAWA, Kazuhiro ,  KOSAKA, Yuki ,  ABE, Shinya

    IPC分类号： C07D413/04 ,  A61P31/10 ,  C07D413/14 ,  C07F5/02 ,  A61K31/4439

    CPC分类号： C07D498/04 ,  C07D213/46 ,  C07D213/643 ,  C07D413/04 ,  C07D413/14 ,  Y02P20/55

    摘要： It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I):

    the method including reacting a compound represented by the following formula (III):

    and a compound represented by the following formula (II):

    in a solvent and in the presence of a palladium catalyst and a base,
    wherein R 1 represents a hydrogen atom, etc.; R 2 represents a hydrogen atom, a C 1-6 alkyl group, an amino group that may be protected with a protective group, etc.; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C 1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.; R represents a hydrogen atom or a C 1-6 alkyl group, etc.; R 3 represents a hydrogen atom or a halogen atom, etc.; and R 4 represents a hydrogen atom or a halogen atom;
    provided that when Z represents a single bond, or when R 3 represents a hydrogen atom, then R 1 , R 2 , and R 4 cannot all be a hydrogen atom at the same time.

    摘要翻译： 本发明的目的是提供一种制备杂环取代的吡啶衍生物的有效方法。 本发明提供下述式（I）表示的化合物的制造方法：使下述式（III）表示的化合物与下述式（II）所示的化合物反应的方法：在溶剂和 在钯催化剂和碱的存在下，其中R 1表示氢原子等; R 2表示氢原子，C 1-6烷基，可被保护基保护的氨基等; X和Y中的一个表示氮原子，另一个表示氮原子或氧原子; Q表示离去组; 环A表示可具有一个或两个卤素原子或C 1-6烷基的5-或6-元杂芳基环或苯环; Z表示单键，亚甲基，亚乙基，氧原子等; R表示氢原子或C 1-6烷基等; R 3表示氢原子或卤素原子等; R 4表示氢原子或卤素原子; 条件是当Z表示单键时，或当R 3表示氢原子时，则R 1，R 2和R 4不能同时为氢原子。