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    Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of the derivatives
    2.
    发明授权
    Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of the derivatives 有权
    制备具有喹唑啉二酮骨架的苯丙氨酸衍生物的方法和用于制备衍生物的中间体

    公开(公告)号：US08546610B2

    公开(公告)日：2013-10-01

    申请号：US13218946

    申请日：2011-08-26

    申请人： Noriyasu Kataoka ,  Kotaro Okado ,  Tatsuhiro Yamada ,  Koichi Fujita ,  Tamotsu Suzuki ,  Tatsuya Okuzumi ,  Masayuki Sugiki ,  Akinori Tatara

    发明人： Noriyasu Kataoka ,  Kotaro Okado ,  Tatsuhiro Yamada ,  Koichi Fujita ,  Tamotsu Suzuki ,  Tatsuya Okuzumi ,  Masayuki Sugiki ,  Akinori Tatara

    IPC分类号： C07C229/56

    CPC分类号： C07D239/96 ,  C07C233/47 ,  C07C233/87 ,  C07C237/40 ,  C07C237/42 ,  C07C265/12 ,  C07C271/22 ,  C07C271/28 ,  C07C275/42 ,  Y02P20/55

    摘要： A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3′ which is a group corresponding to R3 is protected. According to this method, there can be obtained a phenylalanine derivative having a quinazoline-dione skeleton in a industrially favorably high yield.

    摘要翻译： 一种制备具有由下式（1）表示的喹唑啉二酮环的苯丙氨酸衍生物或其药学上可接受的盐的方法，包括以下步骤（a），（b）和（c）：（a）使酰基 由下式（2）表示的苯丙氨酸衍生物：具有羰基导入试剂和特定的邻氨基苯甲酸衍生物，从而形成相应的羧基不对称脲衍生物; （b）在羧基活化剂存在下将羧基不对称脲衍生物转化为相应的喹唑啉二酮衍生物：（c）如果需要，用N-烷基取代与氮原子键合的氢原子存在 在使用N-烷基化试剂的喹唑啉二酮衍生物的喹唑啉二酮环中，然后当对应于R3的基团的取代基R3'被保护时，使得到的产物脱保护。 根据该方法，可以得到具有喹唑啉二酮骨架的苯丙氨酸衍生物，工业上有利地高产率。