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    • 9. 发明申请
    • FUNGICIDES BASED ON NITROGEN-CONTAINING HETEROCYCLES
    • 基于含氮杂质的杀真菌剂
    • WO2004056829A1
    • 2004-07-08
    • PCT/GB2003/005261
    • 2003-12-03
    • SYNGENTA LIMITEDSYNGENTA PARTICIPATIONS AGCROWLEY, Patrick, JelfDOBLER, MarkusMUELLER, UrsWILLIAMS, John
    • CROWLEY, Patrick, JelfDOBLER, MarkusMUELLER, UrsWILLIAMS, John
    • C07D487/04
    • C07D471/04
    • Fungicidal compounds having the general formula (1): formula (1) wherein W, Z and one of X and Y are N and the other one of X and Y is CR 8 ; R 8 is H, halo, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio or halo(C 1-4 )alkyl; R and R 2 are independently H, halo, C 1-8 alkyl, C 1-8 alkoxy, C 1-8 alkylthio, C 2-8 alkenyl, C 2-8 alkynyl, cyano or NR 3 R 4 , provided that at least one of R and R 2 is NR 3 R 4 ; R 1 is halo, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl(C 1-6 )­-alkyl, C 1-8 alkoxy, C 1-8 alkylthio, aryl, aryloxy, arylthio, heteroaryl, heteroaryloxy, heteroarylthio, aryl(C 1-4 )alkyl, aryl(C 1-4 )alkoxy, heteroaryl(C 1-4 )alkyl, heteroaryl­(C 1-4 )alkoxy, aryl(C 1-4 )alkylthio, heteroaryl(C 1-4 )alkylthio, morpholino, piperidino or pyrrolidino; R 3 and R 4 are independently H, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, aryl(C 1-8 )­- alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl(C 1-6 )alkyl, heteroaryl, heteroaryl(C 1-8 )alkyl, NR 5 R 6 , provided that not both R 3 and R 4 are H or NR 5 R 6 , or R 3 and R 4 together form a C 3-7 alkylene or C 3-7 alkenylene chain optionally substituted with one or more C 1-4 alkyl or C 1-4 alkoxy groups, or, together with the nitrogen atom to which they are attached, R 3 and R 4 form a morpholine, thiomorpholine, thiomorpholine S-oxide or thiomorpholine S-dioxide ring or a piperazine or piperazine N -(C 1-4 )alkyl (especially N -methyl) ring; and R 5 and R 6 are independently H, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, aryl(C 1-8 )­alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-8 )alkyl; any of the foregoing alkyl, alkenyl, alkynyl or cycloalkyl groups or moieties (other than for R 8 ) being optionally substituted with halogen, cyano, C 1-6 alkoxy, C 1-6 alkylcarbonyl, C 1-6 alkoxycarbonyl, C 1-6 haloalkoxy, C 1-6 alkylthio, tri(C 1-4 )alkylsilyl, C 1-6 alkylamino or C 1-6 dialkylamino, any of the foregoing morpholine, thiomorpholine, piperidine, piperazine and pyrrolidine rings being optionally substituted with C 1-4 alkyl (especially methyl), and any of the foregoing aryl or heteroaryl groups or moieties being optionally substituted with one or more substituents selected from halo, hydroxy, mercapto, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 alkoxy, C 2-6 alkenyloxy, C 2-6 alkynyloxy, halo(C 1-6 )alkyl, halo(C 1-6 )alkoxy, C 1-6 alkylthio, halo(C 1-6 )alkylthio, hydroxy(C 1-6 )alkyl, C 1-4 alkoxy(C 1-6 )alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl(C 1-4 )alkyl, phenoxy, benzyloxy, benzoyloxy, cyano, isocyano, thiocyanato, isothiocyanato, nitro, -NR"'R"", NHCOR"', -NHCONR"'R"", -CONR"'R"", -SO 2 R"', -OSO 2 R"', -COR"', -CR"'=NR"" or -N=CR "'R"", in which R"' and R"" are independently hydrogen, C 1-4 alkyl, halo-(C 1-4 )alkyl, C 1-4 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.
    • 其中W,Z和X和Y之一是N,X和Y中的另一个是CR 8的通式(1):式(1)的杀真菌化合物:式 R 8是H,卤素,C 1-4烷基,C 1-4烷氧基,C 1-4烷硫基或卤代(C 1-4)烷基; R和R 2独立地是H,卤素,C 1-8烷基,C 1-8烷氧基,C 1-8烷硫基,C 2-8烯基,C 2-8炔基,氰基或NR 3 R 4,条件是 R 3和R 2中的至少一个是NR 3 R 4; R 1是卤素,C 1-8烷基,C 2-8烯基,C 2-8炔基,C 3-8环烷基,C 3-8环烷基(C 1-6) - 烷基,C 1-8烷氧基,C 1-8烷硫基,芳基 ,芳氧基,芳硫基,杂芳基,杂芳氧基,杂芳硫基,芳基(C1-4)烷基,芳基(C1-4)烷氧基,杂芳基(C1-4)烷基,杂芳基(C1-4)烷氧基,芳基(C1-4) ,杂芳基(C 1-4)烷硫基,吗啉代,哌啶子基或吡咯烷子基; R 3和R 4独立地是H,C 1-8烷基,C 2-8烯基,C 2-8炔基,芳基,芳基(C 1-8) - 烷基,C 3-8环烷基,C 3-8环烷基 -6)烷基,杂芳基,杂芳基(C 1-8)烷基,NR 5 R 6,条件是不是R 3和R 4都不是H或NR 5 R 6,或 R 3和R 4一起形成任选被一个或多个C 1-4烷基或C 1-4烷氧基取代的C 3-7亚烷基或C 3-7亚烯基链,或者与它们所在的氮原子一起 R 3和R 4形成吗啉,硫代吗啉,硫代吗啉S-氧化物或硫代吗啉S-二氧化环或哌嗪或哌嗪N-(C 1-4)烷基(特别是N-甲基)环; R 5和R 6独立地为H,C 1-8烷基,C 2-8烯基,C 2-8炔基,芳基,芳基(C 1-8)烷基,C 3-8环烷基,C 3-8环烷基 -6)烷基,杂芳基或杂芳基(C 1-8)烷基; 氰基,C 1-6烷氧基,C 1-6烷基羰基,C 1-6烷氧基羰基,C 1-6卤代烷氧基,任选被烷基,烯基,炔基或环烷基中的任何一个(除R 8之外) ,C 1-6烷硫基,三(C 1-4)烷基甲硅烷基,C 1-6烷基氨基或C 1-6二烷基氨基,任何上述吗啉,硫代吗啉,哌啶,哌嗪和吡咯烷环任选被C 1-4烷基(特别是甲基) 并且任何前述芳基或杂芳基基团或部分任选被一个或多个选自卤素,羟基,巯基,C 1-6烷基,C 2-6烯基,C 2-6炔基,C 1-6烷氧基, C 1-6烷氧基,C 1-6烷氧基,C 1-6烷氧基,C 1-6烷硫基,卤代(C 1-6)烷硫基,羟基(C 1-6)烷基, C 1-6)烷基,C 3-6环烷基,C 3-6环烷基