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    Cyclopropanation
    2.
    发明授权
    Cyclopropanation 有权

    公开(公告)号：US09663420B2

    公开(公告)日：2017-05-30

    申请号：US15034760

    申请日：2014-11-06

    申请人： ETH Zurich

    发明人： Juan Manuel Sarria Toro ,  Peter Chen ,  Tim Den Hartog

    IPC分类号： C07C2/86

    CPC分类号： C07C2/86 ,  C07C2531/22 ,  C07C2531/24 ,  C07C2601/02 ,  C07C2602/02 ,  C07C2602/24 ,  C07C2603/62 ,  C07C2603/66 ,  C07C13/605 ,  C07C13/45 ,  C07C13/04

    摘要： A method of preparing a cyclopropane ring-bearing compound of the formula I in which R1 and R2 are independently selected from C1-C10 alkyl, optionally substituted, or R1 and R2, together with the bonds linking them to the cyclopropane ring, form a monocyclic or bicyclic ring system, which may comprise at least one hetero-atom, comprising the reaction of a compound of formula II R1—CH═CH—R2  II in which R1 and R2 have the significances hereinabove defined, with a compound of formula III X—CH2—Y  III in which X is a nucleofuge selected from halides and pseudohalides and Y is an electrofuge selected from boranes and borates, in the presence of a metal catalyst complex selected from those useful for catalytic cyclopropanation and those useful for catalyzing Heck coupling. The method provides a particularly easy and non-hazardous method of cyclopropanation.

    CYCLOPROPANATION
    6.
    发明申请
    CYCLOPROPANATION 有权
    循环

    公开(公告)号：US20160280617A1

    公开(公告)日：2016-09-29

    申请号：US15034760

    申请日：2014-11-06

    申请人： ETH Zurich

    发明人： Juan Manuel SARRIA TORO ,  Peter CHEN ,  Tim DEN HARTOG

    IPC分类号： C07C2/86

    CPC分类号： C07C2/86 ,  C07C2531/22 ,  C07C2531/24 ,  C07C2601/02 ,  C07C2602/02 ,  C07C2602/24 ,  C07C2603/62 ,  C07C2603/66 ,  C07C13/605 ,  C07C13/45 ,  C07C13/04

    摘要： A method of preparing a cyclopropane ring-bearing compound of the formula I in which R1 and R2 are independently selected from C1-C10 alkyl, optionally substituted, or R1 and R2, together with the bonds linking them to the cyclopropane ring, form a monocyclic or bicyclic ring system, which may comprise at least one hetero-atom, comprising the reaction of a compound of formula II R1—CH═CH—R2  II in which R1 and R2 have the significances hereinabove defined, with a compound of formula III X—CH2—Y  III in which X is a nucleofuge selected from halides and pseudohalides and Y is an electrofuge selected from boranes and borates, in the presence of a metal catalyst complex selected from those useful for catalytic cyclopropanation and those useful for catalyzing Heck coupling. The method provides a particularly easy and non-hazardous method of cyclopropanation.

    摘要翻译： 其中X是选自卤化物和拟卤化物的核苷，Y是选自硼烷和硼酸盐的电极，在选自用于催化环丙烷化的那些金属催化剂络合物和可用于催化Heck偶联的催化剂络合物存在下。 该方法提供了一种特别容易且无危险的环丙烷化方法。

    Process for the preparation of pyrazole carboxylic acid amides
    8.
    发明授权
    Process for the preparation of pyrazole carboxylic acid amides 有权
    制备吡唑羧酸酰胺的方法

    公开(公告)号：US08895757B2

    公开(公告)日：2014-11-25

    申请号：US13981913

    申请日：2012-01-25

    申请人： Miroslav Terinek ,  Dominik Faber ,  Stefan Koenig

    发明人： Miroslav Terinek ,  Dominik Faber ,  Stefan Koenig

    IPC分类号： C07D231/14 ,  C07C251/56 ,  C07C329/04 ,  C07C231/14 ,  C07C329/02 ,  C07C251/64

    CPC分类号： C07C231/14 ,  C07C251/56 ,  C07C251/64 ,  C07C329/02 ,  C07C329/04 ,  C07C2603/66 ,  C07D231/14

    摘要： The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide by acylating the oxime oxygen of the compound of formula (VIII), in the presence of a solvent and an acylating agent of formula (XI) R1C(X)—CI (XI); wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; and a) if R1 is chloro and the compound of formula (XI) was added to the compound of formula (VIII); reacting the so obtained product of formula (XIIa) wherein X is oxygen or sulfur; with the compound of formula (IX) b) if R1 is chloro and the compound of formula (VIII) was added to the compound of formula (XI); or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; reacting the so obtained product of formula (XII) wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; with the compound of formula (IX).

    摘要翻译： 本发明涉及制备3-二氟甲基-1-甲基-1H-吡唑-4-羧酸（9-二氯亚甲基-1,2,3,4-四氢-1,4-亚甲基 - 萘-5 （XI）R1C（X）-CⅠ（XI）的溶剂和酰化剂的存在下酰化式（Ⅷ）化合物的肟氧; 其中X是氧或硫; 如果X是氧或硫，则R1是氯; 或者如果X是氧，则R1是C1-C6烷氧基，CH3-C（= CH2）-O-，苯氧基或三氯甲氧基; 和a）如果R1是氯，并且将式（XI）化合物加入到式（VIII）化合物中; 使所得的式（XIIa）化合物与X为氧或硫反应; 与式（Ⅸ）化合物b）如果R 1是氯，并将式（Ⅷ）化合物加到式（Ⅺ）化合物中; 或者如果X是氧，则R1是C1-C6烷氧基，CH3-C（= CH2）-O-，苯氧基或三氯甲氧基; 使所得的式（XII）化合物（其中X是氧或硫）反应; 如果X是氧或硫，则R1是氯; 或者如果X是氧，则R1是C1-C6烷氧基，CH3-C（= CH2）-O-，苯氧基或三氯甲氧基; 与式（IX）的化合物反应。

    METHOD OF REGIOSELECTIVE SYNTHESIS OF SUBSTITUTED BENZOATES
    9.
    发明申请
    METHOD OF REGIOSELECTIVE SYNTHESIS OF SUBSTITUTED BENZOATES 有权
    取代苯甲酸酯的取代合成方法

    公开(公告)号：US20140288324A1

    公开(公告)日：2014-09-25

    申请号：US14234079

    申请日：2012-06-21

    申请人： George A. Kraus

    发明人： George A. Kraus

    IPC分类号： C07C67/317 ,  C07C51/377

    CPC分类号： C07C67/317 ,  C07C51/367 ,  C07C51/377 ,  C07C67/313 ,  C07C67/343 ,  C07C2603/66 ,  C07C2603/86 ,  C07C69/80 ,  C07C69/76 ,  C07C63/04 ,  C07C63/331 ,  C07C65/24 ,  C07C65/21 ,  C07C63/49 ,  C07C69/612

    摘要： A method of synthesis of para-substituted benzoate esters and acids is provided, wherein the para-substituted regioisomer is obtained substantially free of the meta-substituted impurity, the method comprising contacting a coumalate ester or acid and an unactivated alkene at elevated temperature in the presence of a metal oxidation catalyst and an oxidant. The metal oxidation catalyst can be palladium, such as palladium on carbon, and the oxidant can be the oxygen gas in ambient air. The reaction can be carried out without solvent or in high boiling hydrocarbon solvents such as mesitylene. When the unactivated alkene is a monosubstituted alkene, yields of at least about 50 or 60% of para-substituted ester and acid products, respectively, are obtained, substantially free of the regioisomeric meta-substituted impurity.

    摘要翻译： 提供了一种合成对位取代的苯甲酸酯和酸的方法，其中基本上不含间位取代的杂质获得对位取代的区域异构体，该方法包括在高温下使香豆酸酯或酸与未活化的烯烃接触 存在金属氧化催化剂和氧化剂。 金属氧化催化剂可以是钯，例如钯碳，氧化剂可以是环境空气中的氧气。 该反应可以在没有溶剂的情况下进行，也可以在高沸点烃溶剂例如均三甲苯中进行。 当未活化的烯烃是单取代的烯烃时，分别获得至少约50或60％的对位取代的酯和酸产物的产率，基本上不含区域异构间位取代的杂质。

    Compounds and processes that generate cyclopropenes and substituted cyclopropenes on demand
    10.
    发明授权
    Compounds and processes that generate cyclopropenes and substituted cyclopropenes on demand 有权
    根据需要产生环丙烯和取代环丙烯的化合物和方法

    公开(公告)号：US08656638B2

    公开(公告)日：2014-02-25

    申请号：US13065521

    申请日：2011-03-23

    申请人： Cheryl D. Stevenson ,  John Perrin Davis

    发明人： Cheryl D. Stevenson ,  John Perrin Davis

    IPC分类号： A01N3/00 ,  A01N43/20 ,  C07D305/14 ,  C07C1/207

    CPC分类号： C07D305/14 ,  A01N3/00 ,  A01N27/00 ,  C07C1/2078 ,  C07C49/573 ,  C07C69/753 ,  C07C69/757 ,  C07C2603/66

    摘要： Compounds and methods that release 1-methylcyclopropene, 1-trifluoromethylcyclopropene, and other substituted cyclopropenes are disclosed. The compounds are of the class of chemical analogue of 2-oxa-bicyclo[2.1.0]penta-3-one useful as vessels for molecular plant ethylene receptor inhibitors. The compounds and methods overcome present limitations for storage, transportation, and application of the cyclopropene containing compounds by using light, including sunlight, and/or heat as the primary release trigger. Additional products released include innocuous gases and value added aryl-group compounds.

    摘要翻译： 公开了释放1-甲基环丙烯，1-三氟甲基环丙烯和其它取代的环丙烯的化合物和方法。 该化合物是用作分子植物乙烯受体抑制剂的血管的2-氧杂 - 双环[2.1.0]五-3-酮的化学类似物。 化合物和方法通过使用包括阳光的光和/或作为主要释放触发剂的光来克服存在，运输和施用含环丙烯化合物的现有限制。 发布的其他产品包括无害气体和增值芳基化合物。