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    • 8. 发明公开
    • PROCESS FOR PRODUCING ESTER COMPOUND
    • VERFAHREN ZUR HERSTELLUNG EINER ESTERVERBINDUNG
    • EP2716630A1
    • 2014-04-09
    • EP12792034.6
    • 2012-05-17
    • Sumitomo Chemical Company Limited
    • IKEMOTO, TetsuyaLUTETE, Leopold MpakaAIKAWA, Toshiaki
    • C07D209/52C07C205/29C07C217/44C07C271/16C07C271/18C07D317/16C07D317/28
    • C07C223/02C07C201/12C07C205/29C07C213/02C07C213/08C07C217/44C07C269/04C07C271/16C07C271/18C07C2601/08C07D209/52C07D317/16C07D317/28C07C205/44
    • Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process comprising steps A to G as mentioned below:

      [Step A] A step of reacting an aldehyde compound (2) with nitromethane to produce a nitroaldehyde compound (3);
      [Step B] A step of reacting the nitroaldehyde compound (3) with an alcohol to produce a nitroacetal compound (4);
      [Step C] A step of reducing the nitroacetal compound (4) to produce an aminoacetal compound (5);
      [Step D] A step of protecting an amino group in the aminoacetal compound (5) to produce a protected aminoacetal compound (6);
      [Step E] A step of treating the protected aminoacetal compound (6) with an acid and aubsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile compound (7);
      [Step F] A step of hydrolyzing the nitrile compound (7) to produce a protected amino acid compound (8); and
      [Step G] A steep of substituting a group R 5 in the protected amino acid compound (8) by a hydrogen atom and protecting a carboxyl group therein.
    • 化合物(1)或可用作制备药物,农药等的中间体的盐可以通过包括如下所述的步骤A至G的方法制备:[步骤A]使醛 化合物(2)与硝基甲烷反应生成硝基醛化合物(3); [步骤B]使硝基醛化合物(3)与醇反应以制备硝基缩醛化合物(4)的步骤; [步骤C]还原硝基缩醛化合物(4)以产生氨基缩醛化合物(5)的步骤; [步骤D]保护氨基缩醛化合物(5)中的氨基以产生受保护的氨基缩醛化合物(6)的步骤; [步骤E]用酸和随后用碱处理受保护的氨基缩醛化合物(6),然后使所得产物与氰化剂反应以产生腈化合物(7)的步骤。 [步骤F]水解腈化合物(7)以产生受保护的氨基酸化合物(8)的步骤; 和[步骤G]通过氢原子将保护的氨基酸化合物(8)中的基团R 5取代并保护其中的羧基的陡峭。