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    Production methods of imidazole compound and salt thereof and intermediates therefor
    1.
    发明授权
    Production methods of imidazole compound and salt thereof and intermediates therefor 失效
    咪唑化合物及其盐及其中间体的制备方法

    公开(公告)号：US06649768B1

    公开(公告)日：2003-11-18

    申请号：US10309961

    申请日：2002-12-04

    申请人： Tetsuya Shintaku ,  Nobushige Itaya

    发明人： Tetsuya Shintaku ,  Nobushige Itaya

    IPC分类号： C07D40104

    CPC分类号： C07D401/04

    摘要： A production method including a step for converting a halogen compound of the formula (6) or a salt thereof to a glyoxal compound of the formula (2) or a salt thereof in dimethyl sulfoxide, and a step for reacting the glyoxal compound of the formula (2) or a salt thereof obtained in the previous step with ammonia and an aldehyde compound of the formula (3) or a salt thereof can conveniently produce an imidazole compound of the formula (1) or a salt thereof. The imidazole compound is a synthetic intermediate for a compound useful as pharmaceutical agents and agricultural chemicals. The production method is suitable for industrial scale production. is wherein each symbol is as defined in the specification.

    摘要翻译： 一种制备方法，其包括将式（6）的卤素化合物或其盐转化为二甲基亚砜中的式（2）的乙二醛化合物或其盐的步骤和使式（Ⅳ）的乙二醛化合物反应的步骤 （3）的醛化合物或其盐可以方便地制备式（1）的咪唑化合物或其盐。 咪唑化合物是用作药剂和农药的化合物的合成中间体。 该制造方法适用于工业规模生产，其中每个符号如说明书中所定义。

    Production method of hydrazine derivative
    2.
    发明授权
    Production method of hydrazine derivative 有权
    肼衍生物的制备方法

    公开(公告)号：US06376678B1

    公开(公告)日：2002-04-23

    申请号：US09521058

    申请日：2000-03-08

    申请人： Kiyoshi Sugi ,  Kozo Matsui ,  Tetsuya Shintaku ,  Nobushige Itaya

    发明人： Kiyoshi Sugi ,  Kozo Matsui ,  Tetsuya Shintaku ,  Nobushige Itaya

    IPC分类号： C07D21170

    CPC分类号： C07D213/06 ,  C07D213/42

    摘要： A production method of hydrazine derivative having a group of the formula (II) which comprises subjecting a hydrazone derivative having a group of the formula (I) to catalytic reduction and deactivating the reduction catalyst contained in the reaction mixture thereof. According to the production method of the present invention, which is industrially superior, hydrazine derivative (II) stable even in a solution state can be produced

    摘要翻译： 具有式（II）基团的肼衍生物的制备方法，其包括将具有式（I）的基团的腙衍生物进行催化还原和使其反应混合物中所含的还原催化剂失活。 根据工业上优越的本发明的制造方法，可以制造即使在溶液状态下稳定的肼衍生物（II）

    2-phenylpyridine derivative and production method thereof
    3.
    发明授权
    2-phenylpyridine derivative and production method thereof 有权
    2-苯基吡啶衍生物及其制备方法

    公开(公告)号：US06242608B1

    公开(公告)日：2001-06-05

    申请号：US09602031

    申请日：2000-06-23

    申请人： Kozo Matsui ,  Kiyoshi Sugi ,  Yoshihide Umemoto ,  Tetsuya Shintaku ,  Nobushige Itaya

    发明人： Kozo Matsui ,  Kiyoshi Sugi ,  Yoshihide Umemoto ,  Tetsuya Shintaku ,  Nobushige Itaya

    IPC分类号： C07D21170

    CPC分类号： C07D213/42 ,  C07D213/26 ,  C07D213/48

    摘要： A series of compounds capable of deriving an intermediate for the production of a compound (A) of the following formula, which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N′-[4-(pyridin-2-yl)phenylmethylidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.

    摘要翻译： 一系列能产生下式的化合物（A）的中间体的化合物，其为抗HIV药物及其制备方法。 具体地说，4-（吡啶-2-基）苯甲醛腙，该化合物的制备方法，以及由该化合物制备N-（叔丁氧基羰基）-N' - [4-（吡啶-2-基） 苯基亚甲基]肼。 此外，2-（4-溴甲基苯基）吡啶，2-（4-二溴甲基苯基）吡啶及其盐的盐，这些化合物的制备方法和得到4-（吡啶-2-基）苯甲醛的制备方法 是来自这些化合物的4-（吡啶-2-基）苯甲醛腙的生产中间体。

    Process for production of .beta.-dihalogenoethenylcyclopropane derivatives
    4.
    发明授权
    Process for production of .beta.-dihalogenoethenylcyclopropane derivatives 失效
    生产β-二卤代乙酰基环丙烷衍生物的方法

    公开(公告)号：US4740612A

    公开(公告)日：1988-04-26

    申请号：US825966

    申请日：1986-02-05

    申请人： Takashi Matsuo ,  Nobushige Itaya ,  Osamu Magara

    发明人： Takashi Matsuo ,  Nobushige Itaya ,  Osamu Magara

    IPC分类号： C07C69/743 ,  A01N37/06 ,  A01P7/04 ,  C07C20060101 ,  C07C23/04 ,  C07C49/16 ,  C07C49/163 ,  C07C49/327 ,  C07C51/377 ,  C07C61/15 ,  C07C61/35 ,  C07C61/40 ,  C07C62/18 ,  C07C67/00 ,  C07C69/74 ,  C07C69/747 ,  C07C69/757

    CPC分类号： C07C45/65 ,  C07C45/69

    摘要： A novel process for producing a .beta.-dihalogenoethenylcyclopropane derivative of the formula, ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group, R.sub.3 is a hydrogen atom, lower alkyl, acyl, carboxyl or alkoxycarbonyl group and R is a hydrogen atom or a lower alkyl group and each of Y.sub.1 and Y.sub.2 is a fluorine, chlorine or bromine atom respectively, which is an acidic moiety of the useful synthetic insecticides of the pyrethrin type, which process comprises a combination of a series of sequential steps starting from alkyl 3-butenyl ketone derivative of the formula (I), which may be shown according to the following reaction scheme: ##STR2## According to this process, objective compound of the formula (VI) having any cis/trans ratio can be produced by selecting the reaction condition of the Stages II-1, II-2, and IV-2.

    摘要翻译： 一种制备下式的β-二卤代乙酰基环丙烷衍生物的新方法，其中R1是氢原子或烷基，R3是氢原子，低级烷基，酰基，羧基或烷氧基羰基，R是氢原子或 低级烷基，Y1和Y2各自分别是氟，氯或溴原子，它们是除虫菊酯类有用的合成杀虫剂的酸性部分，该方法包括从烷基3开始的一系列顺序步骤的组合 （VI）的目标化合物，其具有任何顺式（Ⅵ）的式（Ⅵ）的化合物， /反式比可以通过选择阶段II-1，II-2和IV-2的反应条件来产生。

    Method for preparing 4-hydroxy-3-methyl-2-(2-propynyl)-2-cyclopentenolone
    5.
    发明授权
    Method for preparing 4-hydroxy-3-methyl-2-(2-propynyl)-2-cyclopentenolone 失效
    4-羟基-3-甲基-2-（2-丙炔基）-2-环戊烯醇的制备方法

    公开(公告)号：US4343953A

    公开(公告)日：1982-08-10

    申请号：US159497

    申请日：1980-06-16

    申请人： Noritada Matsuo ,  Nobushige Itaya ,  Kohichi Aketa ,  Osamu Magara ,  Toshio Nishioka

    发明人： Noritada Matsuo ,  Nobushige Itaya ,  Kohichi Aketa ,  Osamu Magara ,  Toshio Nishioka

    IPC分类号： C07C45/66 ,  C07C45/67 ,  C07C45/72 ,  C07C49/24 ,  C07C45/45

    CPC分类号： C07C49/24 ,  C07C45/66 ,  C07C45/673 ,  C07C45/72

    摘要： The present invention relates to a novel method for producing cyclopentenolone of the formula (I), ##STR1## which is a useful intermediate for producing agricultural chemicals, which comprises reacting an acetonedicarboxylic ester of the formula (VII), ##STR2## wherein R is a C.sub.1 -C.sub.6 alkyl group, with 2-propynyl chloride in the presence of magnesium alkoxide and in the presence of alkali iodide to obtain novel mono-(2-propynyl)-substituted acetonedicarboxylic ester of the formula (VI), ##STR3## wherein R is as defined above; hydrolyzing the mono-(2-propynyl)-substituted acetonedicarboxylic ester of the formula (VI) under alkaline conditions with an alkali and then reacting the hydrolyzed product with methylglyoxal of the formula, ##STR4## to obtain novel .gamma.-diketone of the formula (V), ##STR5## and ring-closing the .gamma.-diketone of the formula (V) under alkaline condition.

    摘要翻译： 本发明涉及一种制备式（I）的环戊烯醇酮的新方法，其是用于生产农药的有用的中间体，其包括使式（VII）的丙酮二羧酸酯， （Ⅶ）其中R是C 1 -C 6烷基，与2-丙炔基氯在烷氧基镁存在下，在碱金属碘化物的存在下，得到式（Ⅵ）的新型单 - （2-丙炔基） - 取代的丙酮二羧酸酯 ），其中R如上定义; 在碱性条件下用碱水解式（Ⅵ）的单 - （2-丙炔基） - 取代的丙二酸二羧酸酯，然后使水解产物与下式的甲基乙二醛反应，得到式（Ⅵ）的新的γ-二酮 V），（V）并在碱性条件下闭合式（V）的γ-二酮。

    Insecticides
    7.
    发明授权
    Insecticides 失效
    杀虫剂

    公开(公告)号：US4053625A

    公开(公告)日：1977-10-11

    申请号：US634850

    申请日：1975-11-24

    申请人： Isao Ono ,  Yoshitoshi Okuno ,  Toshio Nishioka ,  Nobushige Itaya

    发明人： Isao Ono ,  Yoshitoshi Okuno ,  Toshio Nishioka ,  Nobushige Itaya

    IPC分类号： A01N37/32 ,  A01N53/04 ,  A01P7/04 ,  C07D207/00 ,  C07D207/44 ,  C07D207/448 ,  C07D207/452 ,  C07D207/456 ,  A01N9/22

    CPC分类号： C07D207/448 ,  C07D207/452

    摘要： A cyclopropanecarboxylic acid ester of the formula (I), ##STR1## wherein R.sub.1 is a hydrogen atom, methyl group or a fluorine, chlorine or bromine atom, R.sub.2 is a fluorine, chlorine or bromine atom, and each of R.sub.3 and R.sub.4 is independently a hydrogen atom, a C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl or C.sub.2 -C.sub.3 alkynyl group, an alkyl- or halogen-substituted aryl, unsubstituted aryl group or an aralkyl group, which possesses various useful insecticidal and acaricidal activities and can be prepared by reacting an alcohol, halide or arylsulfonate compound of the formula (II), ##STR2## wherein R.sub.3 and R.sub.4 have the same meanings as defined above and A is a hydroxyl group, a halogen atom or an arylsulfoxy group, with a cyclopropanecarboxylic acid of the formula (III), ##STR3## wherein R.sub.1 and R.sub.2 have the same meanings as defined above, or its reactive derivative.

    Novel cyclopropanecarboxylates
    8.
    发明授权
    Novel cyclopropanecarboxylates 失效
    新型环丙烷羧酸酯

    公开(公告)号：US4003945A

    公开(公告)日：1977-01-18

    申请号：US461029

    申请日：1974-04-15

    申请人： Shigeyoshi Kitamura ,  Nobushige Itaya ,  Yoshitoshi Okuno ,  Nobuo Ohno ,  Takashi Matsuo ,  Masachika Hirano ,  Toshio Mizutani ,  Hisami Takeda

    发明人： Shigeyoshi Kitamura ,  Nobushige Itaya ,  Yoshitoshi Okuno ,  Nobuo Ohno ,  Takashi Matsuo ,  Masachika Hirano ,  Toshio Mizutani ,  Hisami Takeda

    IPC分类号： C07C69/743 ,  A01N53/10 ,  C07C69/74 ,  C07D307/28 ,  C07D307/45 ,  C07D309/06 ,  C07D309/22 ,  C07D317/54 ,  C07D333/16

    CPC分类号： C07D307/42 ,  C07C403/12 ,  C07D307/28 ,  C07D309/06 ,  C07D309/22 ,  C07D317/54 ,  C07D333/16 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2101/16 ,  Y10S514/937 ,  Y10S514/952 ,  Y10S514/953 ,  Y10S514/957

    摘要： Novel alkynylcyclopropanecarboxylic acid esters represented by the formula, ##STR1## wherein R.sub.1 represents hydrogen, halogen, lower alkyl having up to 5 carbon atoms, lower alkenyl having up to 5 carbon atoms, lower alkynyl having up to 5 carbon atoms, C.sub.1 -C.sub.4 alkoxy C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio C.sub.1 -C.sub.4 alkyl, aryl, aryl C.sub.1 -C.sub.4 alkyl, furyl, substituted furyl, thienyl, substituted thienyl, furfuryl, substituted furfuryl, thenyl, substituted thenyl, cyclo C.sub.3 -C.sub.6 alkyl, substituted cyclo C.sub.3 -C.sub.6 alkyl, cyclo C.sub.3 -C.sub.6 alkenyl or substituted cyclo C.sub.3 -C.sub.6 alkenyl; R.sub.2 and R.sub.3 individually represent hydrogen, halogen, lower alkyl having up to 5 carbon atoms, lower alkenyl having up to 5 carbon atoms, lower alkynyl having up to 5 carbon atoms, aryl, aryl C.sub.1 -C.sub.4 alkyl or may form a carbon-carbon bond; or R.sub.1 and R.sub.3 are bonded to each other at the ends to form a polymethylene chain containing or not containing an oxygen or a sulfur atom, or R.sub.1 and R.sub.2 are bonded to each other at the ends to form a polymethylene chain containing or not containing an oxygen or a sulfur atom; R.sub.4 represents hydrogen or methyl; R.sub.5 represents hydrogen, methyl, vinyl, 1-propenyl, 2-methyl-1-propenyl, 2-methoxymethyl-1-propenyl, 2-methoxycarbonyl-1-propenyl, 2,2-dichlorovinyl or cyclopentyl-idenemethyl when R.sub.4 is hydrogen, and R.sub.5 represents methyl when R.sub.4 is methyl; and R.sub.6 and R.sub.7 represent hydrogen or methyl. These novel esters are produced by reacting an alcohol or its halide or arylsulfonate of the formula, ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.6 are defined above, and A is hydroxy, halogen or arylsulfoxy, with a cyclopropane-carboxylic acid of the formula, ##STR3## wherein R.sub.4, R.sub.5 and R.sub.7 are as defined above, or its reactive derivative. These esters are useful as an insecticide harmless to mammals.

    摘要翻译： 由式表示的新型炔基环丙烷羧酸酯，其中R 1表示氢，卤素，具有至多5个碳原子的低级烷基，具有至多5个碳原子的低级链烯基，低至5个碳原子的低级炔基，C1-C4烷氧基 C 1 -C 4烷基，C 1 -C 4烷硫基C 1 -C 4烷基，芳基，芳基C 1 -C 4烷基，呋喃基，取代的呋喃基，噻吩基，取代的噻吩基，糠基，取代的糠基，噻吩基，取代的芳基，环C 3 -C 6烷基，取代的环 C 3 -C 6烷基，环C 3 -C 6烯基或取代的环C 3 -C 6烯基; R 2和R 3各自表示氢，卤素，具有至多5个碳原子的低级烷基，具有至多5个碳原子的低级链烯基，具有至多5个碳原子的低级炔基，芳基，芳基C 1 -C 4烷基或可形成碳 - 碳 键; 或者R 1和R 3在末端彼此键合以形成含有或不含有氧原子或硫原子的多亚甲基链，或者R 1和R 2在末端彼此结合形成含有或不含有 氧或硫原子; R4代表氢或甲基; 当R4为氢时，R5代表氢，甲基，乙烯基，1-丙烯基，2-甲基-1-丙烯基，2-甲氧基甲基-1-丙烯基，2-甲氧基羰基-1-丙烯基，2,2-二氯乙烯基或环戊基 - 当R 4为甲基时，R 5表示甲基; 并且R 6和R 7表示氢或甲基。 这些新型酯通过使下式的醇或其卤化物或芳基磺酸盐与其中R1，R2，R3和R6定义如上，A是羟基，卤素或芳基磺酰基的醇或其卤化物或芳基磺酸酯与 式，其中R 4，R 5和R 7如上所定义，或其反应性衍生物。 这些酯可用作对哺乳动物无害的杀虫剂。