中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

4 records (took 0.012 seconds)

    Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides
    1.
    发明授权
    Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides 有权
    制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法

    公开(公告)号：US08592583B2

    公开(公告)日：2013-11-26

    申请号：US13505357

    申请日：2010-10-27

    Applicant: Matteo D'Anello ,  Marco Re

    Inventor： Matteo D'Anello ,  Marco Re

    IPC: C07D401/00

    CPC classification number: C07D403/04 ,  C07D207/34

    Abstract: The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. The synthesis is starting from the coupling of an acetal with a beta-ketoester; the resultant compound is acetylated and then reacted with a dialkyl acetal of N,N-dimethylformamide to give an intermediate which is cyclized to 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxylic ester; the carboxylic ester is then hydrolyzed and the resultant carboxylic acid is finally condensed with an appropriate form of ammonia to give the desired carboxamide. The compounds prepared according to the process of the invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

    Abstract translation: 本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。 该方法允许以高产率和纯度获得所需的产物。 合成起始于缩醛与β-酮酯的偶联; 将所得化合物乙酰化，然后与N，N-二甲基甲酰胺的二烷基缩醛反应，得到中间体，将其中环化为5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-基） 羧酸酯; 然后将羧酸酯水解，所得羧酸最终与适当形式的氨浓缩，得到所需的甲酰胺。 根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。 该化合物可用于治疗各种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

    PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES 有权
    制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-羧酸的方法

    公开(公告)号：US20120220771A1

    公开(公告)日：2012-08-30

    申请号：US13505357

    申请日：2010-10-27

    Applicant: Matteo D'Anello ,  Marco Re

    Inventor： Matteo D'Anello ,  Marco Re

    IPC: C07D403/04 ,  C07D207/34

    CPC classification number: C07D403/04 ,  C07D207/34

    Abstract: The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. The synthesis is starting from the coupling of an acetal with a beta-ketoester; the resultant compound is acetylated and then reacted with a dialkyl acetal of N,N-dimethylformamide to give an intermediate which is cyclized to 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxylic ester; the carboxylic ester is then hydrolyzed and the resultant carboxylic acid is finally condensed with an appropriate form of ammonia to give the desired carboxamide. The compounds prepared according to the process of the invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

    Abstract translation: 本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。 该方法允许以高产率和纯度获得所需的产物。 合成起始于缩醛与β-酮酯的偶联; 将所得化合物乙酰化，然后与N，N-二甲基甲酰胺的二烷基缩醛反应，得到中间体，将其中环化为5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-基） 羧酸酯; 然后将羧酸酯水解，所得羧酸最终与适当形式的氨浓缩，得到所需的甲酰胺。 根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。 该化合物可用于治疗各种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

Patent Agency Ranking