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    Preparation of thiazoles
    3.
    发明授权
    Preparation of thiazoles 失效
    噻唑的制备

    公开(公告)号：US06548676B1

    公开(公告)日：2003-04-15

    申请号：US09331433

    申请日：1999-06-18

    申请人： Thomas Pitterna ,  Henry Szczepanski ,  Peter Maienfisch ,  Ottmar Franz Hüter ,  Thomas Rapold ,  Marcel Senn ,  Thomas Göbel ,  Anthony Cornelius O'Sullivan

    发明人： Thomas Pitterna ,  Henry Szczepanski ,  Peter Maienfisch ,  Ottmar Franz Hüter ,  Thomas Rapold ,  Marcel Senn ,  Thomas Göbel ,  Anthony Cornelius O'Sullivan

    IPC分类号： C07D27732

    CPC分类号： C07D277/32 ,  C07D277/16 ,  C07D277/36 ,  C07D277/70 ,  C07D277/74

    摘要： Described is a process for the preparation of a compound of formula (I) wherein R is unsubstituted or substituted C1-C12alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, aryl or heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, C2-C4alkenyl, C2-C4alkynyl, cycloalkyl, aryl or heteroaryl; and X is a leaving group; which comprises: a) reacting a compound of formula (II) wherein R is as defined for formula (I), with a water-removing reagent; or b) for the preparation of a compound of formula (I) wherein X is halogen or a sulfonate, reacting a compound of the formula (III) wherein R is as defined for formula (I), with a halogenating or a sulfonylating agent; or c) for the preparation of a compound of formula (I) wherein X is halogen, reacting a compound of formula (IV) wherein R is as defined for formula (I); and wherein R2 and R3 are for example H, C1-C6alkyl, C3-C6cycloalkyl, phenyl or benzyl; with a compound of the formula halogen-C(═O)—O—C1-C8alkyl, halogen-C(═O)—O-aryl or halogen-C(═O)—O-benzyl. Intermediates for the preparation of the synthesis of compounds (II) to (IV) and method of the preparation thereof.

    摘要翻译： 描述了制备式（I）化合物的方法，其中R是未取代的或取代的C 1 -C 12烷基，C 2 -C 4烯基，C 2 -C 4炔基，C 3 -C 6环烷基，芳基或杂芳基或-SR 1; R1是未取代的或取代的C1-C12烷基，C2-C4链烯基，C2-C4炔基，环烷基，芳基或杂芳基; X为离去群; 其包括：a）使其中R如式（I）所定义的式（II）化合物与除水试剂反应; 或者b）用于制备其中X为卤素或磺酸盐的式（I）化合物，其中R为式（I）所定义的式（III）化合物与卤化剂或磺酰化剂反应; 或c）用于制备其中X为卤素的式（I）化合物，其中R为式（I）所定义的式（IV）化合物; 并且其中R 2和R 3是例如H，C 1 -C 6烷基，C 3 -C 6环烷基，苯基或苄基; 与卤素-C（= O）-O-C 1 -C 8烷基，卤素-C（= O）-O-芳基或卤素-C（= O）-O-苄基的化合物反应。 用于制备化合物（II）至（IV）的合成的中间体及其制备方法。

    Process for the preparation of thiazole derivatives
    5.
    发明授权
    Process for the preparation of thiazole derivatives 失效
    噻唑衍生物的制备方法

    公开(公告)号：US06677457B2

    公开(公告)日：2004-01-13

    申请号：US10047807

    申请日：2002-01-15

    申请人： Thomas Pitterna ,  Henry Szczepanski ,  Peter Maienfisch ,  Ottmar Franz Hüter ,  Thomas Rapold ,  Marcel Senn ,  Thomas Göbel ,  Anthony Cornelius O'Sullivan ,  Gottfried Seifert

    发明人： Thomas Pitterna ,  Henry Szczepanski ,  Peter Maienfisch ,  Ottmar Franz Hüter ,  Thomas Rapold ,  Marcel Senn ,  Thomas Göbel ,  Anthony Cornelius O'Sullivan ,  Gottfried Seifert

    IPC分类号： C07D27716

    CPC分类号： C07D277/32 ,  C07D277/16 ,  C07D277/36 ,  C07D417/06

    摘要： The invention relates to a process for the preparation of a compound of the formula wherein Q, Y, Z, R1, R2, R3, R4 and R5 are as defined in the specification, which comprises a) reacting a compound of the formula  with a halogenating agent to form a compound of the formula or b) converting a compound of formula (II) by means of a halogenating agent into a compound of the formula optionally c) converting the compound of formula (IV) into a compound of formula (III); d) converting a compound of formula (III) by means of a compound of the formula into a compound of the formula or e) converting a compound (IV) by means of a compound (V) into a compound (VI); and f) converting a compound (VI) by means of a chlorinating agent into a compound (I); a compound (IV); to a process for the preparation of a compound (III) and to a process for the preparation of a compound (IV).

    摘要翻译： 本发明涉及制备糠醛的化合物的方法，其中Q，Y，Z，R 1，R 2，R 3，R 4和R 5如本说明书中所定义，其包括：a）将卤化剂的化合物与 将式（II）化合物通过卤化剂转化成式（Ⅲ）的化合物，将式（Ⅳ）化合物转化为式（Ⅳ）化合物; d）将化合物 通过化学式（Ⅳ）将化合物（Ⅳ）转化为化合物（Ⅵ）;将式（Ⅳ）化合物与式 和（f）通过氯化剂将化合物（VI）转化为化合物（I）;化合物（IV）; 涉及制备化合物（III）的方法和制备化合物（IV）的方法。

    Thiazole compounds
    6.
    发明授权
    Thiazole compounds 失效
    噻唑化合物

    公开(公告)号：US06211381B1

    公开(公告)日：2001-04-03

    申请号：US09077569

    申请日：1998-06-01

    申请人： Henry Szczepanski ,  Thomas Göbel ,  Ottmar Franz Hüter ,  Anthony Cornelius O'Sullivan ,  Marcel Senn ,  Thomas Rapold ,  Peter Maienfisch ,  Thomas Pitterna

    发明人： Henry Szczepanski ,  Thomas Göbel ,  Ottmar Franz Hüter ,  Anthony Cornelius O'Sullivan ,  Marcel Senn ,  Thomas Rapold ,  Peter Maienfisch ,  Thomas Pitterna

    IPC分类号： C07D27732

    CPC分类号： C07D277/32 ,  C07D277/36 ,  C07D417/06

    摘要： The invention relates to a process for preparing a compound of formula (I), in which X is CH or N, Y is NO2 or CN, Z is CHR3, O, NR3 or S, R1 and R2 are either each, independently of the other, hydrogen or unsubstituted or R4-substituted alkyl or together a two- or three-membered alkylene bridge or a two- or three-membered alkylene bridge in which one member is replaced by a hetero member selected from the group, consisting of NR5, O and S, R3 is H or unsubstituted or R4-substituted alkyl, R4 is an unsubstituted or substituted aryl or heteroaryl group, and R5 is H or alkyl, which comprises a) reacting a compound of formula (II) with a chlorinating agent or b1) initially reacting a compound of formula (IV) with a compound of formula (V) and b2) further reacting the compound of formula (II) obtainable thereby, with or without intermediate isolation, with a chlorinating agent, to intermediates used in this process, to the use of these intermediates and to a process for the preparation of these intermediates.

    摘要翻译： 本发明涉及制备式（I）化合物的方法，其中X是CH或N，Y是NO 2或CN，Z是CHR 3，O，NR 3或S，R 1和R 2各自独立地是 另一个，氢或未取代的或R4取代的烷基或二元或三元亚烷基桥或二元或三元亚烷基桥，其中一个成员被选自NR5， O和S，R 3是H或未取代的或R 4取代的烷基，R 4是未取代或取代的芳基或杂芳基，R 5是H或烷基，其包括a）使式（II）化合物与氯化剂或 b1）最初使式（Ⅳ）化合物与式（Ⅴ）化合物反应，和b2）使可得到的式（Ⅱ）化合物进一步与中间体分离与氯化剂反应，得到本发明的中间体 过程，使用这些中间体和制备过程 这些中间体。