PROCESS FOR PREPARATION OF PYRIMIDINYLACETONITRILE DERIVATIVES AND INTERMEDIATES FOR SYNTHESIS THEREOF
    28.
    发明公开
    PROCESS FOR PREPARATION OF PYRIMIDINYLACETONITRILE DERIVATIVES AND INTERMEDIATES FOR SYNTHESIS THEREOF 有权
    用于生产PYRIMIDINYLACETONITRILDERIVATEN和中间产品及其合成

    公开(公告)号:EP2474536A1

    公开(公告)日:2012-07-11

    申请号:EP10811488.5

    申请日:2010-08-23

    Inventor: KAWAZOE, Kentaro

    Abstract: Provided is a process by which pyrimidinylacetonitrile derivatives can be prepared easily and efficiently from industrially available raw materials. Also provided are intermediates for the synthesis of the derivatives. A process for the preparation of pyrimidinylacetonitrile derivatives represented by general formula (3) [wherein X is a halogen atom, and R is an alkoxymethyl group], characterized by reacting a 2,4-dihalogeno-6-nitrobenzene derivative represented by general formula (1) [wherein X and R are each as defined above] with 4,6-dimethoxy-2-cyanomethylpyrimidine represented by general formula (2) [wherein Me represents a methyl group] in the presence of a base; and intermediates for the synthesis of the pyrimidinylacetonitrile derivatives.

    Abstract translation: 提供了通过该pyrimidinylacetonitrile衍生物可以容易且有效地从工业上获得的原料来制备的方法。 这样提供了用于该衍生物的合成中间体。 一种衍生物的制备过程pyrimidinylacetonitrile由通式(3)表示[worin X为卤素原子,R是烷氧基甲基],通过使由通式表示的2,4-二卤代-6-硝基苯衍生物为特征的( 1)[式中,X和R分别如上定义]与通式4,6-二甲氧基-2-氰基甲基(2)[其中,Me darstellt甲基〕在碱的存在; 和用于pyrimidinylacetonitrile衍生物的合成中间体。

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