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    PREPARATION OF THIAZOLES
    2.
    发明申请
    PREPARATION OF THIAZOLES 失效
    制备THIAZOLES

    公开(公告)号：US20080076920A1

    公开(公告)日：2008-03-27

    申请号：US11947891

    申请日：2007-11-30

    申请人： Thomas Pitterna ,  Henry Szczepanski ,  Peter Maienfisch ,  Ottmar Huter ,  Thomas Rapold ,  Marcel Senn ,  Thomas Gobel ,  Anthony O'Sullivan

    发明人： Thomas Pitterna ,  Henry Szczepanski ,  Peter Maienfisch ,  Ottmar Huter ,  Thomas Rapold ,  Marcel Senn ,  Thomas Gobel ,  Anthony O'Sullivan

    IPC分类号： C07D417/02 ,  C07D277/36 ,  C07D417/14

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

    摘要： The present disclosure is directed to a process for the preparation of a compound having the formula: wherein R is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted C3-C6cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; and X is a selected leaving group that is not halogen, and may specifically be methylsulfonate, trifluoromethylsulfonate, and p-toluenesulfonate. These compounds are valuable intermediates useful in the synthesis of compounds having pesticidal activity. Generally, the process includes reacting a water-removing reagent, with a compound having the formula Water-removing agents that may be used include thionyl chloride (SOCl2), thionyl bromide (SOBr2), phosphorus oxychloride (POCl3), phosphorus oxybromide (POBr3), phosphorus pentachloride or a sulfonic acid chloride or bromide.

    摘要翻译： 本公开涉及制备具有下式的化合物的方法：其中R是未取代或取代的C 1 -C 12烷基，未取代或取代的C 1 -C 12烷基， 未取代或取代的C 2 -C 4炔基，未取代或取代的C 1 -C 4烷基， 3个C 6环烷基，未取代或取代的芳基，未取代或取代的杂芳基或-SR 1 N; R 1是未取代或取代的C 1 -C 12烷基，未取代或取代的C 2 -C 3 未取代或取代的C 2 -C 4炔基，未取代或取代的环烷基，未取代或取代的芳基或未取代或取代的杂芳基; X是不是卤素的选择的离去基团，可以具体为甲基磺酸酯，三氟甲基磺酸酯和对甲苯磺酸酯。 这些化合物是有用的合成具有杀虫活性的化合物的中间体。 通常，该方法包括使除水试剂与具有式的化合物反应可以使用的除水剂包括亚硫酰氯（SOCl 2/2），亚硫酰溴（SO 2 R 2） （POCl 3 3），三溴氧化磷（POBr 3 N），五氯化磷或磺酰氯或溴化物。

    PREPARATION OF THIAZOLES
    3.
    发明申请
    PREPARATION OF THIAZOLES 失效
    制备THIAZOLES

    公开(公告)号：US20070055063A1

    公开(公告)日：2007-03-08

    申请号：US11552255

    申请日：2006-10-24

    申请人： Thomas Pitterna ,  Henry Szczepanski ,  Peter Maienfisch ,  Ottmar Huter ,  Thomas Rapold ,  Marcel Senn ,  Thomas Gobel ,  Anthony O'Sullivan

    发明人： Thomas Pitterna ,  Henry Szczepanski ,  Peter Maienfisch ,  Ottmar Huter ,  Thomas Rapold ,  Marcel Senn ,  Thomas Gobel ,  Anthony O'Sullivan

    IPC分类号： C07D417/02

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

    摘要： A process for the preparation of a compound of the formula and, where applicable, its E/Z-isomers, mixtures of E/Z-isomers and/or tautomers and acid addition products thereof, in each case in free form or in salt form, wherein: R is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted C3-C6cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; and X is a leaving group; The process comprises reacting a compound of the formula: with a halogenating agent or a sulfonylating agent. Alternatively, when X is a selected halogen, the process can comprise reacting a compound of the formula with a compound having a formula selected from the group consisting of halogen-C(═O)—O—C1-C8alkyl; halogen-C(═O)—O-aryl; and halogen-C(═O)—O-benzyl.

    摘要翻译： 制备下式化合物及其E / Z-异构体的方法，E / Z-异构体和/或互变异构体的混合物及其酸加成产物，各自为游离形式或盐形式 ，其中：R是未取代或取代的C 1 -C 12烷基，未取代或取代的C 2 -C 4 烯基，未取代或取代的C 2 -C 4炔基，未取代或取代的C 3 -C 6环烷基 ，未取代或取代的芳基，未取代或取代的杂芳基或-SR 1 N; R 1是未取代或取代的C 1 -C 12烷基，未取代或取代的C 2 -C 3 未取代或取代的C 2 -C 4炔基，未取代或取代的环烷基，未取代或取代的芳基或未取代或取代的杂芳基; X为离去群; 该方法包括使下式化合物与卤化剂或磺酰化剂反应。 或者，当X是选择的卤素时，该方法可以包括使下式的化合物与具有选自以下的式的化合物反应：卤素-C（ - ） - O-C 1 -C 烷基; 卤素-C（ - ） - O-芳基; 和卤素-C（ - ） - O-苄基。

    "> Avermectins substituted in the 4
    4.
    发明申请
    Avermectins substituted in the 4"-position having pesticidal properties 有权
    在4“位置取代的阿维菌素具有杀虫特性

    公开(公告)号：US20060105970A1

    公开(公告)日：2006-05-18

    申请号：US11319686

    申请日：2005-12-28

    申请人： Thomas Pitterna ,  Anthony O'Sullivan ,  William Lutz

    发明人： Thomas Pitterna ,  Anthony O'Sullivan ,  William Lutz

    IPC分类号： A01N43/04 ,  C07H17/08

    CPC分类号： C07H19/01 ,  A01N43/90 ,  A01N47/12 ,  A01N47/14 ,  A01N47/28 ,  A01N47/30 ,  A01N47/32

    摘要： What is described are a compound of the formula in which R1 is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; R2 is H, unsubstituted or mono- to pentasubstituted C1-C12alkyl or unsubstituted or mono-to pentasubstituted C1-C12alkenyl; R3 is C2-C12alkyl, mono- to pentasubstituted C1-C12alkyl, unsubstituted or mono- to pentasubstituted C1-C6alkoxy-C1-C6alkyl, unsubstituted or mono- to pentasubstituted C3-C12cycloalkyl, C2-C12alkenyl, C2-C12alkynyl; or R2 and R3 together are an alkylene or alkenylene bridge; with the proviso that R1 is not sec-butyl or isopropyl if R2 is H and R3 is 2-hydroxyethyl, isopropyl, n-octyl or benzyl;or, if appropriate, in E/Z isomer, an E/Z isomer mixture and/or a tautomer thereof; a process for preparing and using these compounds and their tautomers; pesticides whose active compound is selected from these compounds and their tautomers; and a process for preparing these compounds and compositions, and the use of these compounds and compositions.

    摘要翻译： 描述的是下式的化合物，其中R 1是C 1 -C 12 -C 12烷基，C 3〜 C 1 -C 8环烷基或C 2 -C 12 - 烯基; R 2是H，未取代的或一至五取代的C 1 -C 12烷基或未被取代的或单取代或单取代的C 1 C 12 -C 12烯基; R 3是C 2 -C 12烷基，一至五取代C 1 -C 12烷基，C 1 -C 12烷基，C 1 -C 12烷基， 未取代的或一至五取代的C 1 -C 6烷氧基-C 1 -C 6烷基， 未取代的或一至五取代的C 3 -C 12环烷基，C 2 -C 12烷基， 烯基，C 2 -C 12炔基; 或R 2和R 3一起是亚烷基或亚烯基桥; 条件是R 1不是仲丁基或异丙基，如果R 2是H，R 3是2-羟乙基，异丙基，n 辛基或苄基;或如果合适，在E / Z异构体中，E / Z异构体混合物和/或其互变异构体; 一种制备和使用这些化合物及其互变异构体的方法; 活性化合物选自这些化合物及其互变异构体的农药; 以及制备这些化合物和组合物的方法，以及这些化合物和组合物的用途。