Avermectin B1 and avermectin B1 monosaccharide derivatives having an alkoxymethyl substituent in the 4″-or 4′-position
    73.
    发明授权
    Avermectin B1 and avermectin B1 monosaccharide derivatives having an alkoxymethyl substituent in the 4″-or 4′-position 有权
    在4“ - 或4”位具有烷氧基甲基取代基的阿维菌素B1和除虫菌素B1单糖衍生物

    公开(公告)号:US08263566B2

    公开(公告)日:2012-09-11

    申请号:US13117292

    申请日:2011-05-27

    IPC分类号: A61K31/70 C07H17/04

    CPC分类号: C07H17/08 A61K31/7042

    摘要: What is described are a compound of the formula wherein n is 0 or 1; A-B is —CH═CH— or —CH2—CH2—; R1 is C1-C12-alkyl, C3-C8-cycloalkyl or C2-C12-alkenyl; R2 is for example C1-C12-alkyl, C2-C12-alkenyl or C2-C12-alkinyl; which are optionally substituted with one to five substituents selected from the group consisting of OH, halogen, CN, —N3, —NO2, C3-C8-Cycloalkyl, norbornylenyl-, C3-C8-Cycloalkenyl; C3-C8-halocycloalkyl, C1-C12-alkoxy, C1-C6-alkoxy-C1-C6-alkoxy, C3-C8-cycloalkoxy, C1-C12-haloalkoxy, C1-C12-alkylthio, C3-C8-cycloalkylthio, C1-C12-haloalkylthio, C1-C12-alkylsulfinyl, C3-C8-cycloalkylsulfinyl, C1-C12-haloalkylsulfinyl, C3-C8-halocycloalkylsulfinyl, C1-C12-alkylsulfonyl, C3-C8-cycloalkylsulfonyl, C1-C12-haloalkylsulfonyl, C3-C8-halocycloalkylsulfonyl, —NR4R6, —X—C(═Y)—R4, —X—C(═Y)—Z—R4, —P(═O)(OC1-C6-alkyl)2, aryl, heterocyclyl, aryloxy, arylthio and heterocyclyloxy; R3 is for example H, C1-C12-alkyl or C1-C12-alkyl which is optionally substituted and, where applicable, to E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in salt form; 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n是0或1; A-B是-CH = CH-或-CH 2 -CH 2 - ; R1是C1-C12-烷基,C3-C8-环烷基或C2-C12-烯基; R2是例如C1-C12-烷基,C2-C12-烯基或C2-C12-炔基; 其任选被一至五个选自OH,卤素,CN,-N 3,-NO 2,C 3 -C 8 - 环烷基,降冰片基 - ,C 3 -C 8 - 环烯基的取代基取代; C 3 -C 8卤代环烷基,C 1 -C 12烷氧基,C 1 -C 6烷氧基-C 1 -C 6 - 烷氧基,C 3 -C 8环烷氧基,C 1 -C 12卤代烷氧基,C 1 -C 12烷硫基,C 3 -C 8环烷硫基, C 1 -C 12烷基亚磺酰基,C 3 -C 8环烷基亚磺酰基,C 1 -C 12卤代烷基亚磺酰基,C 3 -C 8卤代环烷基亚磺酰基,C 1 -C 12烷基磺酰基,C 3 -C 8环烷基磺酰基,C 1 -C 12卤代烷基磺酰基, 卤代环烷基磺酰基,-NR4R6,-X-C(= Y)-R4,-X-C(= Y)-Z-R4,-P(= O)(OC1-C6-烷基)2,芳基,杂环基,芳氧基, 芳硫基和杂环氧基; R3是例如任选取代的H,C 1 -C 12 - 烷基或C 1 -C 12 - 烷基,并且在适用的情况下,E / Z异构体,E / Z异构体和/或互变异构体的混合物,在每种情况下为游离形式或 盐形式; 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。

    PREPARATION OF THIAZOLES
    76.
    发明申请
    PREPARATION OF THIAZOLES 失效
    制备THIAZOLES

    公开(公告)号:US20090198054A1

    公开(公告)日:2009-08-06

    申请号:US12424594

    申请日:2009-04-16

    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是未取代的或取代的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,未取代的 或取代的芳基,未取代或取代的杂芳基或-SR1; 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),亚硫酰溴(SOBr 2),三氯氧化磷(POCl 3),三溴氧化磷(POBr 3) ,五氯化磷或磺酰氯或溴化物。

    Preparation of thiazoles
    77.
    发明授权
    Preparation of thiazoles 失效
    噻唑的制备

    公开(公告)号:US07538229B2

    公开(公告)日:2009-05-26

    申请号:US11947891

    申请日:2007-11-30

    IPC分类号: C07D277/36

    摘要: A process for the preparation of a compound of formula I wherein R is a range of organic groups and X is a leaving group which process comprises a) reacting a compound of the formula II where R is defined for formula (I) with a water-removing reagent; or b) for the preparation of a compound of formula (I) wherein K is halogen or a sulfonate, reacting a compound of the formula III where R is defined for formula (I) with a halogenating agent or a sulfonylating agent; or c) for the preparation of a compound of formula (I) wherein X is halogen, reacting a compound of the formula IV where R is as defined for formula (I) and R2 and R3 are defined organic groups with a compound of the formula halogen-C(—O)—O—C1-C8alkyl, halogen-C(—O)—O-aryl or halogen-C(—O)—O-benzyl.

    摘要翻译: 一种制备式I化合物的方法,其中R是有机基团的范围,X是离去基团,该方法包括:a)将式II化合物(其中R定义为式(I))与水 - 去除试剂; 或b)用于制备其中K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,使式IV化合物(其中R如式(I)所定义)与R 2和R 3定义为有机基团的化合物与式 卤素-C(-O)-O-C 1 -C 8烷基,卤素-C(-O)-O-芳基或卤素-C( - ) - O-苄基。

    Avermectin B1 monosaccharide derivatives
    78.
    发明授权
    Avermectin B1 monosaccharide derivatives 有权
    阿维菌素B1单糖衍生物

    公开(公告)号:US07521429B2

    公开(公告)日:2009-04-21

    申请号:US10560390

    申请日:2004-06-15

    IPC分类号: A61K31/70 C07H17/08

    CPC分类号: C07H19/01 C07H17/08

    摘要: A compound of formula (I) wherein the bond between carbon atoms 22 and 23 may be a single or a double bond; R1 is C1-C12alkyl, C3-C8cycloalkyl, or C2-C12alkenyl; R2 and R3 are, for example, independently of each other hydrogen, C1-C12alkyl, C3-C12cycloalkyl, C2-C12alkenyl, C2-C12alkynyl, aryl or heteroaryl; and, where applicable, to E/Z isomers, mixtures of E/Z isomers, diastereomers and/or tautomers, in each case in free form or in salt form; pesticidal compositions in which the active ingredient has been selected from those compounds and their tautomers; and a method of controlling pests using those compositions are described.

    摘要翻译: 式(I)的化合物,其中碳原子22和23之间的键可以是单键或双键; R1是C1-C12烷基,C3-C8环烷基或C2-C12链烯基; R 2和R 3例如彼此独立地为氢,C 1 -C 12烷基,C 3 -C 12环烷基,C 2 -C 12烯基,C 2 -C 12炔基,芳基或杂芳基; 在适用的情况下,E / Z异构体,E / Z异构体,非对映异构体和/或互变异构体的混合物,在每种情况下为游离形式或盐形式; 其中活性成分选自那些化合物及其互变异构体的杀虫组合物; 并描述了使用这些组合物来控制害虫的方法。

    Avermectins substituted in the 4″ and 4′-positions having pesticidal properties
    79.
    发明授权
    Avermectins substituted in the 4″ and 4′-positions having pesticidal properties 有权
    在4“和4”位取代的阿维菌素具有杀虫特性

    公开(公告)号:US07378399B2

    公开(公告)日:2008-05-27

    申请号:US10544274

    申请日:2004-02-03

    CPC分类号: C07H17/08

    摘要: What is described are a compound of the formula (I) Wherein A-B is —CH═CH— or —CH2—CH2—; n is 0 or 1; R1, is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; R2 and R3 for instance are either, (i) independently from each other for instance -Q, —C(═Y)-Q, or —C(═Y)—O-Q; or (ii) together form with the nitrogen atom to which they are bound a three- to seven-membered ring, (iii) together are ═C(R4)R5; R4 and R5 are, independently from each other, for instance -Q, —C(═Y)-Q, or —C(═Y)—O-Q; Y is O or S; Q is for instance H or unsubstituted or mono- to pentasubstituted C1-C12alkyl; or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof; a process for preparing these compounds, their isomers and tautomers and the use of these compounds, their isomers and tautomers; pesticidal compositions whose active compound is selected from these compounds and their tautomers; intermediates for the preparation of the said compounds of the formula (I), methods for the preparation of the compounds of the formula (I), and a method for controlling pests using these compositions

    摘要翻译: 描述的是式(I)的化合物,其中A-B是-CH-CH-或-CH 2 -CH 2 - 。 n为0或1; R 1是C 1 -C 12烷基,C 3 -C 8烷基,C 3 -C 12烷基,C 3 -C 12烷基,C 3 -C 12烷基, >环烷基或C 2 -C 12 - 烯基; 例如,R 2和R 3是(i)彼此独立地例如-Q,-C(-Y)-Q或-C( - Y)-OQ; 或(ii)与其结合的氮原子一起形成三至七元环,(iii)一起为-C(R 4)R 5 >; R 4和R 5各自独立地为例如-Q,-C(-Y)-Q或-C(-Y)-O-Q; Y为O或S; Q是例如H或未被取代或单取代或未取代的C 1 -C 12烷基; 或者,如果合适的话,E / Z异构体,E / Z异构体混合物和/或其互变异构体; 制备这些化合物,其异构体和互变异构体的方法以及这些化合物,其异构体和互变异构体的用途; 活性化合物选自这些化合物及其互变异构体的杀虫组合物; 用于制备所述式(I)化合物的中间体,式(I)化合物的制备方法和使用这些组合物来控制害虫的方法

    Avermectins substituted in the 4
    80.
    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

    IPC分类号: A01N43/04 C07H17/08

    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。