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13 条记录 (耗时 0.026 秒)

    Method for the production of 1-amino-3-phenyluracil derivatives
    1.
    发明授权
    Method for the production of 1-amino-3-phenyluracil derivatives 失效

    公开(公告)号：US07034156B2

    公开(公告)日：2006-04-25

    申请号：US10476941

    申请日：2002-04-25

    申请人： Jörn Stölting ,  Dorothee Hoischen ,  Roland Andree ,  Karl-Heinz Linker ,  Holger Weintritt ,  Heinz-Jürgen Wroblowsky

    发明人： Jörn Stölting ,  Dorothee Hoischen ,  Roland Andree ,  Karl-Heinz Linker ,  Holger Weintritt ,  Heinz-Jürgen Wroblowsky

    IPC分类号： C07D239/54

    CPC分类号： C07D239/22 ,  C07D239/54

    摘要： The present invention relates to a novel process for preparing known 1-amino-3-phenyluracil derivatives, to novel 1-amino-6-hydroxy-3-phenyldihydro-2,4(1H,3H)pyrimidinedione derivatives of the formula (II) in which R1 is hydrogen, cyano, nitro or halogen, R2 is cyano, nitro, halogen or optionally substituted alkyl or alkoxy, R3 is hydrogen, hydroxyl, mercapto, amino, hydroxyamino, hydrazino, halogen, or one of the radicals —R6, -Q-R6, —NH—R6, —NH—O—R6, —NH—SO2—R6, —N(SO2—R6)2, —CQ1-R6, —CQ1-Q2-R6, —CQ1-NH—R6, -Q2-CQ1-R6, —NH—CQ1-R6, —N(SO2—R6)(CQ1-R6), -Q2-CQ1-Q2-R6, —NH—CQ1-Q2-R6 or -Q2-CQ1-NH—R6, where Q is O, S, SO or SO2, Q1 and Q2 are each independently oxygen or sulphur and R6 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl, R4 is hydrogen, halogen or optionally substituted alkyl, and R5 is fluorine- and/or chlorine-substituted alkyl, as intermediates for the 1-amino-3-phenyluracil derivatives, and to a process for preparing the intermediates.

    Process for preparing [bis-(trifluoromethyl)-phenyl]-acetic acids and alkyl esters thereof and dialkyl [bis-(trifluoromethyl)-phenyl]-malonates
    3.
    发明授权
    Process for preparing [bis-(trifluoromethyl)-phenyl]-acetic acids and alkyl esters thereof and dialkyl [bis-(trifluoromethyl)-phenyl]-malonates 失效
    制备[双（三氟甲基） - 苯基] - 乙酸及其烷基酯和[双（三氟甲基） - 苯基] - 丙二酸二烷基酯的方法

    公开(公告)号：US06395921B1

    公开(公告)日：2002-05-28

    申请号：US09635164

    申请日：2000-08-09

    申请人： Albrecht Marhold ,  Jörn Stölting

    发明人： Albrecht Marhold ,  Jörn Stölting

    IPC分类号： C07C6976

    CPC分类号： C07C69/65 ,  C07C51/38 ,  C07C67/32 ,  C07C67/343 ,  C07C57/58

    摘要： [Bis-(trifluoromethyl)-phenyl]-acetic acids are obtained in an advantageous manner by reacting an appropriate bromo- or iodo-bis-(trifluoromethyl)-benzene with a di-C1-C4-alkyl malonate in the presence of a deprotonating agent and a copper salt and hydrolysing and decarboxylating the reaction product in basic medium. It is possible to obtain a mixture of alkyl [bis-(trifluoromethyl)-phenyl]-acetate and alkyl [bis-(tri-fluoromethyl)-phenyl]-malonate by admixing the reaction mixture which is present before hydrolysis and complete decarboxylation with water and acid and heating. From the mixture, it is possible to obtain alkyl [bis-(trifluoromethyl)-phenyl]-acetate by distillation under reduced pressure and dialkyl [bis-(trifluoromethyl)-phenyl]-malonate by work-up by column chromatography, fractional distillation or film distillation. [Bis-(trifluoromethyl)-phenyl]-malonic esters are novel compounds.

    摘要翻译： 通过使合适的溴 - 或碘 - 双 - （三氟甲基） - 苯与二-C1- C4烷基丙二酸酯在去质子化反应的存在下，通过有利的方式获得[双（三氟甲基） - 苯基] - 乙酸 试剂和铜盐，并在碱性介质中水解和脱羧反应产物。 可以通过将水解之前存在的反应混合物与水完全脱羧反应获得[双（（三氟甲基） - 苯基] - 乙酸烷基酯和[双 - （三氟甲基） - 苯基] - 丙二酸烷基酯的混合物 酸和加热。 从混合物中，可以通过在柱下色谱法，分馏或后处理中减压蒸馏和[双（三氟甲基） - 苯基] - 丙二酸二烷基酯来获得[双（三氟甲基） - 苯基] [双（三氟甲基） - 苯基] - 丙二酸酯是新化合物。

    Process for the preparation of 3,5-bis(trifluoro-methyl)-benzoyl chlorides and novel 3,5-bis(tri-halogenomethyl)-and 3,5-dimethylbenzoyl halides
    6.
    发明授权
    Process for the preparation of 3,5-bis(trifluoro-methyl)-benzoyl chlorides and novel 3,5-bis(tri-halogenomethyl)-and 3,5-dimethylbenzoyl halides 失效
    制备3,5-二（三氟 - 甲基） - 苯甲酰氯和新的3,5-双（三卤代甲基） - 和3,5-二甲基苯甲酰基卤化物的方法

    公开(公告)号：US06420601B2

    公开(公告)日：2002-07-16

    申请号：US09769797

    申请日：2001-01-25

    申请人： Albrecht Marhold ,  Jörn Stölting

    发明人： Albrecht Marhold ,  Jörn Stölting

    IPC分类号： C07C5158

    CPC分类号： C07C51/60 ,  C07C51/62 ,  C07C63/70 ,  C07C63/72

    摘要： 3,5-Bis(trifluoromethyl)benzoyl chlorides optionally substituted with fluorine or chlorine are advantageously prepared by converting 3,5-dimethylbenzoic acids optionally substituted with fluorine or chlorine into the corresponding acid chlorides; completely free-radically chlorinating said chlorides in the side chains, giving 3,5-bis(trichloromethyl)benzoyl chlorides optionally substituted by fluorine or chlorine; fluorinating the latter with anhydrous hydrogen fluoride and/or antimony pentafluoride, giving 3,5-bis(trifluoromethyl)benzoyl fluorides optionally substituted with fluorine or chlorine; and then reacting the 3,5-bis(trifluoromethyl)benzoyl fluorides with silicon tetrachloride in the presence of a further Lewis acid. Some of the 3,5-bis(trihalogenomethyl) and 3,5-dimethylbenzoyl halides which arise as intermediates are novel compounds.

    摘要翻译： 任选被氟或氯取代的3,5-双（三氟甲基）苯甲酰氯有利地通过将任选被氟或氯取代的3,5-二甲基苯甲酸转化成相应的酰氯来制备; 完全自由基地氯化侧链中的氯化物，得到任选被氟或氯取代的3,5-双（三氯甲基）苯甲酰氯; 用无水氟化氢和/或五氟化锑氟化后者，得到任选被氟或氯取代的3,5-双（三氟甲基）苯甲酰氟; 然后在另外的路易斯酸的存在下使3,5-双（三氟甲基）苯甲酰氟与四氯化硅反应。 作为中间体产生的一些3,5-二（三卤代甲基）和3,5-二甲基苯甲酰基卤化物是新的化合物。

    Process for the preparation of thioalkylamine derivatives
    7.
    发明授权
    Process for the preparation of thioalkylamine derivatives 有权
    制备硫代烷基胺衍生物的方法

    公开(公告)号：US07235668B2

    公开(公告)日：2007-06-26

    申请号：US10515441

    申请日：2003-05-12

    申请人： Jörn Stölting

    发明人： Jörn Stölting

    IPC分类号： C07C319/14 ,  C07C323/25 ,  C07D277/74

    CPC分类号： C07D277/36 ,  C07C303/24 ,  C07C319/14 ,  C07C305/06 ,  C07C323/25

    摘要： The present invention relates to a novel process for the preparation of compounds of the formula (I) by reacting in a first step amino alcohols of the formula (II) with oleum to give sulphuric acid esters of the general formula (III) and by reacting these sulphuric acid esters in a second step with mercaptans or salts thereof of the general formula (IV) RSM   (IV) wherein in each formula, where applicable, R1, R2, R3, R4, R5, R6, R, n and M have the meanings given in the disclosure, in the presence of a diluent and in the presence of a base.

    摘要翻译： 本发明涉及通过在式（II）的第一步氨基醇与发烟硫酸反应得到通式（III）的硫酸酯，并通过使 这些硫酸酯在第二步中与通式（IV）的硫醇或其盐进行比较<？in-line-formula description =“In-line Formulas”end =“lead”→> RSM（IV） line-formula description =“In-line Formulas”end =“tail”？>其中在每个公式中，如果适用，R 1，R 2，R 2， 3，R 4，R 5，R 6，R 6，n和M具有本公开内容中给出的含义，在 存在稀释剂并存在碱。