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    VERFAHREN ZUR HERSTELLUNG VON 2-(4-N, N-DIALKYLAMINO-2-HYDROXYBENZOYL)BENZOES UREESTERN
    3.
    发明授权
    VERFAHREN ZUR HERSTELLUNG VON 2-(4-N, N-DIALKYLAMINO-2-HYDROXYBENZOYL)BENZOES UREESTERN 有权
    用于生产2-（4-N，N-二烷基氨基-2-羟基苯甲酰）苯甲酸UREESTERN

    公开(公告)号：EP1506159B1

    公开(公告)日：2007-09-19

    申请号：EP03720564.8

    申请日：2003-05-12

    申请人： BASF Aktiengesellschaft

    发明人： HEIDENFELDER, Thomas ,  BECK, Karl

    IPC分类号： C07C227/38 ,  C07C229/52

    CPC分类号： C07C227/38 ,  C07C229/52

    摘要： The invention relates to a method for producing 2-(4-N,N-dialkylamino-2-hydroxybenzoyl)benzoates of formula (I), in which the substituents R to R , independently of one another, are defined as cited in the description. Said substances are produced as follows: I. 3-N,N-dialkylaminophenol of formula (II) is reacted with phthalic anhydride of formula (III) to obtain 2-(4-N,N-dialkylamino-2-hydroxybenzoyl) benzoic acid of formula (IV) and II. said 2-(4-N,N-dialkylamino-2-hydroxybenzoyl) benzoic acid of formula (IV) that has been formed in stage I. is esterified by means of a C1-C12 alcohol or a cyclic C3-C10 alcohol in the presence of an acidic catalyst to obtain 2-(4-N,N-dialkylamino-2-hydroxybenzoyl)benzoate of formula (I). The method is characterised in that the ester of formula (I) that has been formed is purified in an additional stage III by treatment with an adsorbent and/or by distillation.

    PROCESS FOR THE PREPARATION OF ARYLETHANOLAMINE DERIVATIVES HAVING AN ANTI-OBESITY AND ANTI-DIABETIC PROPERTIES
    6.
    发明公开
    PROCESS FOR THE PREPARATION OF ARYLETHANOLAMINE DERIVATIVES HAVING AN ANTI-OBESITY AND ANTI-DIABETIC PROPERTIES 有权
    方法糖尿病的肥胖治疗和ARYLETHANOLAMINDERIVATE的

    公开(公告)号：EP1235788A1

    公开(公告)日：2002-09-04

    申请号：EP00985495.1

    申请日：2000-12-08

    申请人： GLAXO GROUP LIMITED

    发明人： LAWRENCE, Ronnie, MaxwellGlaxo Wellcome plc ,  MILLAR, AlanSmithkline Beecham Corporation

    IPC分类号： C07C237/06 ,  C07C229/52 ,  C07D213/80 ,  A61K31/44 ,  A61K31/24 ,  A61P3/04 ,  A61P3/10

    CPC分类号： C07D213/40 ,  C07C229/52 ,  C07C237/06 ,  C07C237/22 ,  C07D213/38

    摘要： A process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: wherein R1 is an aryl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C¿1-6?alkoxy, C1-6alkyl, hydroxymethyl, trifluoromethyl, -NR?6R6¿, and -NHSO¿2R?6, where each R6 is independently hydrogen or C¿1-4?alkyl; R?2¿ is hydrogen or C¿1-6?alkyl; R?3¿ is CO¿2R?7 where R7 is hydrogen or C¿1-6?alkyl; R?4 and R5¿ are independently hydrogen, C¿1-6?alkyl, or -CO2C1-6alkyl; and Y is N or CH comprising the step of preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof: wherein R?1¿ is an aryl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C¿1-6?alkoxy, C1-6alkyl, hydroxymethyl, trifluoromethyl, -NR?6R6¿, and -NHSO¿2R?6, where each R6 is independently hydrogen or C¿1-4?alkyl; R?2¿ is hydrogen or C¿1-6?alkyl; R?3¿ is CO¿2R?7 where R7 is C¿1-6?alkyl; R?4 and R5¿ are independently hydrogen, C¿1-6?alkyl, -CO2C1-6alkyl; and Y is N or CH.