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    • 63. 发明授权
    • Avermectin B1 and avermectin B1 monosaccharide derivatives having an alkoxymethyl substituent in the 4″-or 4′-position
    • 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
    • US08263566B2
    • 2012-09-11
    • US13117292
    • 2011-05-27
    • Peter MaienfischFiona Murphy KessabiJerome CassayreLaura QuarantaThomas PitternaOttmar Franz HueterPierre Jung
    • Peter MaienfischFiona Murphy KessabiJerome CassayreLaura QuarantaThomas PitternaOttmar Franz HueterPierre Jung
    • A61K31/70C07H17/04
    • C07H17/08A61K31/7042
    • 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.
    • 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。
    • 65. 发明申请
    • PREPARATION OF THIAZOLES
    • 制备THIAZOLES
    • US20090198054A1
    • 2009-08-06
    • US12424594
    • 2009-04-16
    • Thomas PitternaHenry SzczepanskiPeter MaienfischOttmar Franz HuterThomas RapoldMarcel SennThomas GobelAnthony Cornelius O'Sullivan
    • Thomas PitternaHenry SzczepanskiPeter MaienfischOttmar Franz HuterThomas RapoldMarcel SennThomas GobelAnthony Cornelius O'Sullivan
    • C07D413/02C07D277/20C07D277/70
    • C07D277/32C07D277/16C07D277/36C07D277/70C07D277/74
    • 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.
    • 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。
    • 69. 发明授权
    • Process for the preparation of thiazole derivatives
    • 噻唑衍生物的制备方法
    • US06265585B1
    • 2001-07-24
    • US09341716
    • 1999-07-15
    • Thomas PitternaPeter MaienfischDavid John WadsworthLaurenz GsellThomas RapoldHenry Szczepanski
    • Thomas PitternaPeter MaienfischDavid John WadsworthLaurenz GsellThomas RapoldHenry Szczepanski
    • C07D27732
    • C07D277/32
    • A process for the preparation of a compound of formula (I), wherein X is a leaving group; which process comprises, a) for the preparation of a compound of formula (I) wherein X is —OS(═O)2A and A is as defined in the specification, reacting a compound of formula (II) with a sulfonylating agent; or, b) for the preparation of a compound of formula (I) wherein X is iodine, reacting a compound of formula (III) with an iodinating agent, preferably sodium iodide; or, c) for the preparation of a compound of formula (I) whrein X is bromine, reacting a compound of formula (IV) with a brominating agent; or, d) for the preparation of a compound (I) wherein X is chlorine or bromine, reacting a compound (V), wherein R and X are as defined in the specification, with a chlorinating agent, a compound of formula (Ib), the use thereof and a process for the preparation of a compound of formula (II) and a compound of formula (A) are described.
    • 一种制备式(I)化合物的方法,其中X是离去基团; 该方法包括a)制备式(I)化合物,其中X为-OS(= O)2A且A如说明书中所定义,式(II)化合物与磺酰化剂反应; 或b)制备其中X为碘的式(I)化合物,使式(III)化合物与碘化剂,优选碘化钠反应; 或者,c)制备式(I)化合物,其中X是溴,式(Ⅳ)化合物与溴化剂反应; 或者d)制备其中X为氯或溴的化合物(I),其中R和X如说明书中所定义的化合物(Ⅴ)与氯化剂,式(Ib)化合物反应, 描述了其用途和制备式(II)化合物和式(A)化合物的方法。