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    • 14. 发明申请
    • NOVEL 2,7-DIOXO-BICYCLO[4.3.0]NON-5-YL-UREA DERIVATIVES
    • 新的2,7-二氧杂环十二烷[4.3.0]壬-5-赖氨酸衍生物
    • WO2005005432A1
    • 2005-01-20
    • PCT/EP2004/007246
    • 2004-07-02
    • SYNGENTA PARTICIPATIONS AGHANESSIAN, StephenMARCOTTE, Stephene, Michael, JeanHUANG, GuobinCROWLEY, Patrick, JelfLOISELEUR, Olivier
    • HANESSIAN, StephenMARCOTTE, Stephene, Michael, JeanHUANG, GuobinCROWLEY, Patrick, JelfLOISELEUR, Olivier
    • C07D493/04
    • C07D493/04C07D309/14C07D493/14
    • The present invention relates to novel fungicidal 2,7-dioxo-bicyclo[4.3.0] non-5-yl-urea derivatives, to processes for their preparation and to certain intermediate chemicals used in those processes. It also relates to the use of the compounds as biocides, to compositions containing biocidally effective amounts of the compounds and to methods of combating pathogens using the compounds. The invention encompasses 2,7-dioxo-bicyclo[4.3.0]non-5-yl-urea derivatives of formula (I) wherein R is H or C 1-6 alkyl (for example, methyl), the RO group is cis- or trans- to the NH 2 CONH group, R 1 is H, formyl, C 1-8 alkylcarbonyl, C 3-8 cycloalkylcarbonyl, or optionally substituted benzoyl, and X is a N-linked heterocyclic group of the formula (II) or of the formula (III), wherein R 2 is H, C 1-4 alkyl (especially methyl) or halo, or of the formula (IV): The compounds of formula I possess useful plant protecting properties and may advantageously be employed in agricultural practice for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.
    • 本发明涉及新型杀真菌剂2,7-二氧代 - 双环[4.3.0]非-5-基 - 脲衍生物,用于其制备方法和用于这些方法的某些中间体化学品。 它还涉及化合物作为杀生物剂的用途,含有生物有效量的化合物的组合物以及使用该化合物防治病原体的方法。 本发明包括其中R是H或C 1-6烷基(例如甲基)的式(I)的2,7-二氧代 - 双环[4.3.0]非-5-基 - 脲衍生物,RO基团是顺式 - 或 反式连接到NH 2 CONH基团,R 1是H,甲酰基,C 1-8烷基羰基,C 3-8环烷基羰基或任选取代的苯甲酰基,X是式(II)或式(III)的N-连接的杂环基 ),其中R 2是H,C 1-4烷基(特别是甲基)或卤素,或式(IV):式I化合物具有有用的植物保护性质,并且可以有利地用于农业实践中用于控制或预防 通过植物病原微生物,特别是真菌侵染植物。
    • 20. 发明申请
    • FUNGICIDES
    • 杀菌剂
    • WO2004048315A1
    • 2004-06-10
    • PCT/GB2003/004832
    • 2003-11-10
    • SYNGENTA LIMITEDSALMON, RogerCROWLEY, Patrick, JelfBACON, David, Philip
    • SALMON, RogerCROWLEY, Patrick, JelfBACON, David, Philip
    • C07C235/20
    • C07D249/08A01N39/04C07C235/20C07C255/30C07C317/28C07C323/41
    • Fungicidal compounds of the general formula (1): wherein X, Y and Z are independently H, halogen, C l-4 alkyl, halo(C 1-4 )alkyl, C 2-4 alkenyl, halo(C 2 - 4 )alkenyl, C24 alkynyl, halo(C 2-4 )alkynyl, C 1 _ 4 alkoxy, halo(C 1-4 )alkoxy, -S(O) n (C 1-4 )alkyl where n is 0, 1 or 2 and the alkyl group is optionally substituted with fluoro, -OS0 2 (C 1-4 )alkyl where the alkyl group is optionally substituted with fluoro, cyano, nitro, C, 1-4 alkoxycarbonyl, -CONR'R", -COR', -NR'COR" or -NR'COOR"' where R' and R" are independently H or C 1-4 alkyl and R"' is C l-4 alkyl, provided that at least one of X and Z is other than H; R 1 is C l - 4 alkyl, C 2-4 alkenyl or C 2-4 alkynyl in which the alkyl, alkenyl and alkynyl groups are optionally substituted on their terminal carbon atom with one, two or three halogen atoms, with a cyano group, with a C 1-4 alkylcarbonyl group, with a C 1-4 alkoxycarbonyl group or with a hydroxy group; R 2 is H, C 1-4 alkyl, C 1-4 alkoxymethyl or benzyloxymethyl in which the phenyl ring of the benzyl moiety is optionally substituted with CI-4 alkoxy; R 3 and R 4 are independently H, C 1-3 alkyl, C 2-3 alkenyl or C 2-3 alkynyl provided that both are not H and that when both are other than H their combined total of carbon atoms does not exceed 4, or R 3 and R 4 join with the carbon atom to which they are attached to form a 3 or 4 membered carbocyclic ring optionally containing one 0, S or N atom and optionally substituted with halo or C 1-4 alkyl; and R 5 is unsubstituted C 3-4 alkyl, unsubstituted C 3-6 cycloalkyl or C l-4 alkyl or C 3-6 cycloalkyl in which the alkyl and cycloalkyl groups are substituted with halo, hydroxy, C 1-6 alkoxy, cyano, C 1-4 alkylcarbonyloxy, aminocarbonyloxy, mono- or di(C 1 _ 4 )alkylaminocarbonyloxy, -S(O)"(C 1-6 )alkyl where n is 0, 1 or 2, triazolyl, tri(C 1-4 )alkylsilyloxy, optionally substituted phenoxy, optionally substituted thienyloxy, optionally substituted benzyloxy or optionally substituted thienyl-methoxy, in which the optionally substituted phenyl and thienyl rings of phenoxy, thienyloxy, benzyloxy and thienylmethoxy are optionally substituted with one, two or three substituents selected from halo, hydroxy, mercapto, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C1-4 alkoxy, C 2-4 alkenyloxy, C 2-4 alkynyloxy, halo(C 1-4 )­alkyl, halo(C 1-4 )alkoxy, C 1-4 alkylthio; halo(C 1-4 )alkylthio, hydroxy(C 1-4 )alkyl, C 1-4 alkoxy(C 1-4 )alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl(C 1-4 )alkyl, phenoxy, benzyloxy, benzoyloxy, cyano, isocyano, thiocyanato, isothiocyanato, nitro, -NR - R', -NHCOR m , -NHCONR m R", -CONRmR", -S02R m , -OS02R m , -COR M , -CR'=NR" or -N=CR m R", in which R"' and R" are independently hydrogen, CI-4 alkyl, halo(C 1-4 )alkyl, C1-4 alkoxy, halo(C 1-4 )alkoxy, C 1-4 alkylthio, C 3-6 cycloalkyl, C 3-6 cycloalkyl(C 1-4 )alkyl, phenyl or benzyl, the phenyl and benzyl groups being optionally substituted with halogen, C 1-4 alkyl or C 1-4 alkoxy.
    • 通式(1)的杀真菌化合物:其中X,Y和Z独立地为H,卤素,C 1-4烷基,卤代(C 1-4)烷基,C 2-4烯基,卤代(C 2-4)烯基,C 24炔基 ,卤素(C 2-4)炔基,C 1-4烷氧基,卤代(C 1-4)烷氧基,-S(O)n(C 1-4)烷基,其中n为0,1或2,烷基任选被氟取代, -OCO 2(C 1-4)烷基,其中烷基任选被氟,氰基,硝基,C 1-4烷氧基羰基,-CONR'R“,-COR',-NR'COR”或-NR'COOR“ 其中R'和R“独立地是H或C 1-4烷基,R”'是C 1-4烷基,条件是X和Z中的至少一个不是H; R 1是C 1-4烷基,C 2-4烯基 或C2-4炔基,其中烷基,烯基和炔基在其末端碳原子上任选被一个,两个或三个卤素原子与氰基,C 1-4烷基羰基和C 1-4烷氧基羰基 基团或羟基; R 2是H,C 1-4烷基,C 1-4烷氧基甲基或苄氧基甲基,其中苄基 部分任选被C 1-4烷氧基取代; R3和R4分别是H,C1-3烷基,C2-3烯基或C2-3炔基,条件是两者都不是H,当两者都不是H时,它们的总碳原子数不超过4,或者R3和R4 与它们所连接的碳原子一起形成任选含有一个O,S或N原子并任选被卤素或C 1-4烷基取代的3或4元碳环; R5是未取代的C3-4烷基,未取代的C3-6环烷基或C1-C4烷基或C3-6环烷基,其中烷基和环烷基被卤素,羟基,C1-6烷氧基,氰基,C1-4烷基羰基氧基, 氨基羰基氧基,单或二(C 1-4)烷基氨基羰基氧基,-S(O)“(C 1-6)烷基,其中n为0,1或2,三唑基,三(C 1-4)烷基甲硅烷氧基,任选取代的苯氧基,任选取代的噻吩氧基, 任选取代的苄氧基或任选取代的噻吩基 - 甲氧基,其中苯氧基,噻吩氧基,苄氧基和噻吩基甲氧基的任选取代的苯基和噻吩环任选被一个,两个或三个选自卤素,羟基,巯基,C 1-4烷基, C 2-4烷氧基,C 2-4烷氧基,C 2-4烷氧基,卤代(C 1-4)烷基,卤代(C 1-4)烷氧基,C 1-4烷硫基;卤代(C1- 4)烷硫基,羟基(C 1-4)烷基,C 1-4烷氧基(C 1-4)烷基,C 3-6环烷基,C 3-6环烷基(C 1-4)烷基,苯氧基,苄氧基,苯甲酰氧基,氰基, 异氰酸,硫氰酸酯,异硫氰酸酯,硝基,-NR'R',-NHCOR m,-NHCONR m R“,-CONRmR”,-SO 2 R m,-OSO 2 R m,-COR M >,-CR'= NR“或