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    A-(3,5-DIMETHOXY BENZYLIDENE)-A'-HYDROCARBYL METHYLENE CYCLIC KETONE AND PREPARATION METHOD THEREOF
    8.
    发明公开
    A-(3,5-DIMETHOXY BENZYLIDENE)-A'-HYDROCARBYL METHYLENE CYCLIC KETONE AND PREPARATION METHOD THEREOF 审中-公开
    HERSTELLUNGSVERFAHRENFÜRCYCLISCHES ALPHA-（3,5-二甲氧基苯基）-ALPHA'-烃基甲基酮

    公开(公告)号：EP2927208A1

    公开(公告)日：2015-10-07

    申请号：EP13858613.6

    申请日：2013-11-28

    申请人： Pharmaxyn Laboratories Ltd.

    发明人： AO, Guizhen ,  NIE, Jihua ,  LI, Huanqiu ,  MO, Lingxuan ,  CHEN, Lei ,  SONG, Heng ,  CHEN, Shaohua

    IPC分类号： C07C45/74 ,  C07C49/753 ,  C07C221/00 ,  C07C225/22 ,  C07C315/04 ,  C07C317/24 ,  A61K31/136 ,  A61K31/122 ,  A61P35/00

    CPC分类号： C07C49/753 ,  C07C45/45 ,  C07C225/22 ,  C07C317/24 ,  C07C2601/14

    摘要： The present invention discloses a α-(3,5-dimethoxybenzylidene)-α'-hydrocarbyl methylene cyclic ketone with the following structure:

    or

    wherein R is aryl or alkyl, its preparation method is: the cyclic ketone blended with morpholine are subjected to azeotropic dehydration to give enamine, the enamine is condensed with 3,5-dimethoxybenzaldehyde and then condensed with alkyl or aryl formaldehyde under acidic or basic conditions to give the product, the present invention further discloses an antitumor agent comprising α-(3,5-dimethoxybenzylidene)-α'-hydrocarbyl methylene cyclic ketone or medically acceptable salts and pharmaceutically acceptable carriers thereof. Through the above, the present invention providesα-(3,5-dimethoxybenzylidene)-α'-hydrocarbyl methylene cyclic ketone and preparation method thereof, the said compound is a high activity antitumor agent obtained by piecing and modifying the structures of natural anti-tumor active ingredient resveratrol and curcumin, which has a good inhibitory effect on epidermal growth factor receptor.

    摘要翻译： 本发明公开了具有以下结构的±（3,5-二甲氧基亚苄基） - ±' - 烃基亚甲基环酮，或其中R为芳基或烷基，其制备方法为：将与吗啉混合的环酮进行共沸 脱水得到烯胺，烯胺与3,5-二甲氧基苯甲醛缩合，然后在酸性或碱性条件下与烷基或芳基甲醛缩合得到产物，本发明进一步公开了一种抗肿瘤剂，其包含± - （3,5-二甲氧基亚苄基 ） - ± - - 烃基亚甲基环酮或其医药上可接受的盐和药学上可接受的载体。 通过上述，本发明提供了± - （3,5-二甲氧基亚苄基） - ±' - 烃基亚甲基环酮及其制备方法，所述化合物是通过接头和改性天然抗氧化剂结构获得的高活性抗肿瘤剂， 肿瘤活性成分白藜芦醇和姜黄素，对表皮生长因子受体具有良好的抑制作用。