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    METHOD FOR PREPARING PHENYLALANINE DERIVATIVES HAVING QUINAZOLINE-DIONE SKELETON AND INTERMEDIATES FOR USE IN THE PREPARATION OF DERIVATIVES
    73.
    发明申请
    METHOD FOR PREPARING PHENYLALANINE DERIVATIVES HAVING QUINAZOLINE-DIONE SKELETON AND INTERMEDIATES FOR USE IN THE PREPARATION OF DERIVATIVES 有权
    制备具有喹唑啉酮骨架的苯乙烯胺衍生物的方法和用于制备衍生物的中间体

    公开(公告)号：US20090318688A1

    公开(公告)日：2009-12-24

    申请号：US12470846

    申请日：2009-05-22

    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： C07D265/26 ,  C07D239/72 ,  C07C229/00 ,  C07C269/00

    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。

    MANUFACTURE PROCESS OF ORGANIC COMPOUNDS
    74.
    发明申请
    MANUFACTURE PROCESS OF ORGANIC COMPOUNDS 有权
    有机化合物的制造工艺

    公开(公告)号：US20090253811A1

    公开(公告)日：2009-10-08

    申请号：US11721817

    申请日：2005-12-14

    申请人： Bernhard Riss ,  Ulrich Meier

    发明人： Bernhard Riss ,  Ulrich Meier

    IPC分类号： A61K47/12 ,  C07C233/64 ,  C07D265/26 ,  A61P43/00

    CPC分类号： C07C235/60 ,  C07D265/26

    摘要： The present invention relates to a method of preparing N-substituted salicylamides or derivatives thereof, and their salts, hydrates and solvates. In particular, the present invention relates to a method of preparing N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC) and its corresponding disodium monohydrate.

    摘要翻译： 本发明涉及制备N-取代的水杨酰胺或其衍生物及其盐，水合物和溶剂合物的方法。 特别地，本发明涉及制备N-（5-氯水杨酰基）-8-氨基己酸（5-CNAC）及其相应的一水合二钠的方法。

    Process for preparing benzoxazin-4-one polymer conjugates
    77.
    发明申请
    Process for preparing benzoxazin-4-one polymer conjugates 有权
    制备苯并恶嗪-4-酮聚合物共轭物的方法

    公开(公告)号：US20020028934A1

    公开(公告)日：2002-03-07

    申请号：US09891475

    申请日：2001-06-26

    发明人： Renae Dianna Fossum ,  Todd Laurence Underiner

    IPC分类号： C07D265/26 ,  G01N033/53

    CPC分类号： C08F8/30

    摘要： The present invention relates to a process for forming polymer conjugates which are useful as enzyme inhibitors. The process of the present invention comprises the steps of: a) reacting a polymer or copolymer alcohol to form a chloroformate; b) combining a substituted or unsubstituted anthranilic acid comprising an enzyme interaction attenuating unit; and a base catalyst wherein said base catalyst is a supported base catalyst, to form a substrate reactive admixture; and c) adding to said chloroformate formed in step (a) said substrate reactive admixture formed in step (b) to form a benzoxazin-4-one conjugate.

    摘要翻译： 本发明涉及可用作酶抑制剂的聚合物缀合物的形成方法。 本发明的方法包括以下步骤：a）使聚合物或共聚物醇反应形成氯甲酸酯; b）将包含酶相互作用衰减单元的取代或未取代的邻氨基苯甲酸组合; 和碱催化剂，其中所述碱催化剂是负载型催化剂，以形成底物反应性外加剂; 和c）将步骤（a）中形成的所述氯甲酸酯加入步骤（b）中形成的所述底物反应性混合物以形成苯并恶嗪-4-酮缀合物。

    Process for producing isatoic anhydrides
    78.
    发明授权
    Process for producing isatoic anhydrides 失效

    公开(公告)号：US5981749A

    公开(公告)日：1999-11-09

    申请号：US90858

    申请日：1998-06-05

    申请人： Shinji Nishii ,  Masashi Komatsu ,  Hiroshi Ueda

    发明人： Shinji Nishii ,  Masashi Komatsu ,  Hiroshi Ueda

    IPC分类号： C07D265/26 ,  C07D265/14

    CPC分类号： C07D265/26

    摘要： A process for producing isatoic anhydrides of the formula (II): ##STR1## which comprises reacting an anthranilic acid of formula (I): ##STR2## or a salt thereof with phosgene using a mixed solvent of water and an organic solvent miscible with water and inert to the reaction;conducting the reaction in the coexistence of an alkylpyridinium salt in an aqueous solvent; orusing a mixed solvent of water and a specific amount of an organic solvent substantially immiscible with water and inert to the reaction.