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    PROCESS FOR PRODUCTION OF PHENYLALANINE DERIVATIVES HAVING QUINAZOLINEDIONE SKELETONS AND INTERMEDIATES FOR THE PRODUCTION
    32.
    发明公开
    PROCESS FOR PRODUCTION OF PHENYLALANINE DERIVATIVES HAVING QUINAZOLINEDIONE SKELETONS AND INTERMEDIATES FOR THE PRODUCTION 有权
    工艺生产具有CHINAZOLINDIONGERÜSTEN苯丙氨酸衍生物和中间产品的生产

    公开(公告)号：EP2103601A1

    公开(公告)日：2009-09-23

    申请号：EP07832344.1

    申请日：2007-11-22

    Applicant: Ajinomoto Co., Inc.

    Inventor： KATAOKA, Noriyasu ,  OKADO, Kotaro ,  YAMADA, Tatsuhiro ,  FUJITA, Koichi ,  SUZUKI, Tamotsu ,  OKUZUMI, Tatsuya ,  SUGIKI, Masayuki ,  TATARA, Akinori

    IPC: C07D239/96 ,  C07C233/51 ,  C07C237/40 ,  C07C265/12 ,  C07C271/22 ,  C07C271/28 ,  C07C275/42

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

    Abstract: 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.

    Abstract translation: 一种用于制备苯丙氨酸衍生物具有由下式表示的喹唑啉二酮环（1）或其药学上可接受的盐，其包括以下步骤（a），（b）和（c）中的方法：（A）反应成酰基 由下式（2）表示的苯丙氨酸衍生物：与羰基导入试剂和特定的邻氨基苯甲酸衍生物，以形成因此对应羧基不对称脲衍生物; （B）将所述羧基不对称脲衍生物为相应的喹唑啉二酮衍生物在羧基活化剂的存在下：如果需要清除（c）中，用N-烷基为键合到本氮原子上的氢原子 在使用N-烷基化剂，然后脱保护得到的产物，当取代基R3“是对应于R3基团被保护的喹唑啉二酮衍生物的喹唑啉二酮环。 。根据该方法，可以得到在工业上有利地高收率具有喹唑啉二酮骨架苯基丙氨酸衍生物。

    INHIBITORS FOR GLYT-1
    33.
    发明公开
    INHIBITORS FOR GLYT-1 有权
    GLYT-1抑制剂

    公开(公告)号：EP2069286A1

    公开(公告)日：2009-06-17

    申请号：EP07802709.1

    申请日：2007-08-20

    Applicant: F. Hoffmann-La Roche AG

    Inventor： JOLIDON, Synese ,  NARQUIZIAN, Robert ,  PINARD, Emmanuel

    IPC: C07C233/51 ,  C07C235/52 ,  C07C235/56 ,  C07C237/40 ,  C07C255/57 ,  C07D213/56 ,  C07D213/61 ,  C07D213/74 ,  C07D261/18 ,  C07D333/70 ,  A61K31/166 ,  A61K31/167 ,  A61K31/44 ,  A61K31/381 ,  A61K31/415

    CPC classification number: C07C237/12 ,  C07C255/57 ,  C07D213/81 ,  C07D213/82 ,  C07D317/52 ,  C07D333/20 ,  C07D333/70

    Abstract: The present invention relates to compounds of the general formula I wherein R1 is lower alkyl, aryl or heteroaryl, wherein aryl and heteroaryl are optionally substituted by halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, amino, di-lower alkyl amino or morpholinyl; R2 is lower alkyl, -(CH2)n-aryl, -(CH2)n-heteroaryl or -(CH2)n-cycloalkyl, wherein the aryl or heteroaryl groups are optionally substituted by one or more substituents, selected from the group consisting of halogen, lower alkyl, cyano, or lower alkoxy; R3 is hydrogen or lower alkyl; R4 is aryl or heteroaryl, wherein at least one ring is aromatic in nature, wherein aryl and heteroaryl are optionally substituted by one or more substituents, selected from the group consisting of halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl; X is a bond or -OCH2-; n is 0, 1 or 2; or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2, 4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]- benzeneacetamide. and to their use in the treatment of neurological and neuropsychiatric disorders.

    Production method of optically active diphenylalanine compounds
    37.
    发明公开
    Production method of optically active diphenylalanine compounds 审中-公开
    Herstellungsverfahren von optisch aktiven Diphenylalaninverbindungen

    公开(公告)号：EP1724253A2

    公开(公告)日：2006-11-22

    申请号：EP06252438.4

    申请日：2006-05-09

    Applicant: Ajinomoto Co., Inc.

    Inventor： Hamada, Takayuki, Ajinomoto Co., Inc. ,  Yatagai, Masanobu, Ajinomoto Co., Inc.

    IPC: C07C227/16 ,  C07C227/32 ,  C07C229/36 ,  C07C233/51

    CPC classification number: C07C227/20 ,  C07C231/12 ,  C07C229/36 ,  C07C233/47 ,  C07C233/51

    Abstract: The present invention provides a production method including reacting a diphenylmethylene halide compound represented by the following formula (1) with a malonic acid diester compound represented by the following formula (2) in an organic solvent selected from N-methyl-2-pyrrolidone, N-ethyl-2-pyrrolidone and N,N-dimethylformamide, in the presence of a base selected from an alkali metal hydride and an alkali metal t-butoxide to give a diester compound represented by the following formula (3), and then subjecting the diester compound to hydrolysis and decarboxylation to give a diphenylalanine compound represented by the following formula (4).
    According to the present invention, diphenylalanine compound (4) can be obtained industrially advantageously in a high yield.

    wherein each symbol is as defined in the specification.

    Abstract translation: 本发明提供一种制造方法，其特征在于，使下述式（1）表示的二苯基亚甲基卤化物与下述式（2）所示的丙二酸二酯化合物在选自N-甲基-2-吡咯烷酮，N - 乙基-2-吡咯烷酮和N，N-二甲基甲酰胺，在选自碱金属氢化物和碱金属叔丁醇盐的碱的存在下，得到下式（3）表示的二酯化合物，然后 二酯化合物进行水解和脱羧，得到由下式（4）表示的二苯丙氨酸化合物。 根据本发明，可以在工业上有利地以高产率获得二苯丙氨酸化合物（4）。 其中每个符号如说明书中所定义。

    PROCESS FOR PRODUCING AMINO ACID DERIVATIVES
    38.
    发明公开
    PROCESS FOR PRODUCING AMINO ACID DERIVATIVES 审中-公开
    用于生产氨基酸衍生物

    公开(公告)号：EP1613586A1

    公开(公告)日：2006-01-11

    申请号：EP04725378.6

    申请日：2004-04-02

    Applicant: SOLVAY

    Inventor： CALLENS, Roland ,  LARCHEVEQUE, Marc ,  POUSSET, Cyrille

    IPC: C07C231/12 ,  C07D207/08 ,  C07C233/51

    CPC classification number: C25B3/00 ,  C07D207/12 ,  C12P13/04 ,  C12P41/007

    Abstract: Process for producing amino acid derivatives, in which (a) an organic amine, the amino functionality of which is protected, or an α-amino acid, the amino functionality of which is protected, is subjected to an electrochemical reaction so as to form an amine which is activated in the α-position; (b) the activated amine is subjected to a reaction with a carbanionic reagent containing at least 3 carbon atoms and comprising an unsaturated group so as to form an unsaturated amine comprising an unsaturated group, the atom of the unsaturated group closest to the nitrogen being separated from the nitrogen by at least 2 carbon atoms; (c) the unsaturated amine is subjected to oxidation of the unsaturated group so as to form an amino acid derivative.

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