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    • 1. 发明申请
    • NAPHTHYRIDINE DERIVATIVES AND THEIR USE AS FUNGICIDES
    • 萘啶衍生物及其作为杀真菌剂使用
    • WO2004056824A3
    • 2004-10-14
    • PCT/GB0305248
    • 2003-12-03
    • SYNGENTA LTDSYNGENTA PARTICIPATIONS AGCROWLEY PATRICK JELFDOBLER MARKUSMUELLER URSWILLIAMS JOHN
    • CROWLEY PATRICK JELFDOBLER MARKUSMUELLER URSWILLIAMS JOHN
    • A01N43/90C07D471/04
    • C07D471/04A01N43/90
    • Fungicidal compositions of the general formula (1): wherein one of W, X, Y and Z is N and the others are CR ; R is H, halo, C1-4 alkyl, C1-4 alkoxy or halo(C1-4)alkyl, provided that when X is CH, Z is N, R is NHNH2, R is phenyl and R is Cl, W and Y are not both CCH3; one of R and R is NR R and the other is halo, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C2-8 alkenyl, C2-8 alkynyl or cyano; R is aryl, heteroaryl, morpholino, piperidino or pyrrolidino; R and R are independently H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, aryl(C1-8)-alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-6)alkyl, heteroaryl, heteroaryl(C1-8)alkyl, NR R , provided that not both R and R are H or NR R , or R and R together form a C3-7 alkylene or C3-7 alkenylene chain optionally substituted with one or more C1-4 alkyl or C1-4 alkoxy groups, or, together with the nitrogen atom to which they are attached, R and R form a morpholine, thiomorpholine, thiomorpholine S-oxide or thiomorpholine S-dioxide ring or a piperazine or piperazine N-(C1-4)alkyl (especially N-methyl) ring; and R and R are independently H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, aryl(Cl-8)-alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-6)alkyl, heteroaryl or heteroaryl(C1-8)alkyl; any of the foregoing alkyl, alkenyl, alkynyl or cycloalkyl groups or moieties (other than for R ) being optionally substituted with halogen, cyano, C1-6 alkoxy C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 haloalkoxy, C1-6 alkylthio, tri(C1-4)alkylsilyl, C1-6 alkylamino or C1-6 ialkylamino, any of the foregoing morpholine, thiomorpholine, piperidine, piperazine and pyrrolidine rings being optionally substituted with C1-4 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, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C2-6 alkenyloxy, C2-6 alkynyloxy, halo(C1-6)alkyl, halo(C1-6)alkoxy, C1-6 alkylthio, halo(C1-6)alkylthio, hydroxy(C1-6)alkyl, C1-4 alkoxy(C1-6)alkyl, C 1-6 cycloalkyl, C3-6 cycloalkyl(C1-4)alkyl, phenoxy, benzyloxy, benzoyloxy, cyano, isocyano, thiocyanato, isothiocyanato, nitro, -NHCOR"', -NHCONR"'R"", -CONK"'R"", SO2R"', -OSO2R"', -COR"', -CR"'=NR" or -N=CR "'R"", in which R"' and R"" are independently hydrogen, C1-4 alkyl, halo-(C1-4)alkyl, C1-4 alkoxy, halo(C1
    • 通式(1)的杀真菌组合物:其中W,X,Y和Z中的一个为N,其余为CR 8; R 8为H,卤素,C 1-4烷基,C 1-4烷氧基或卤代(C 1-4)烷基,条件是当X为CH时,Z为N,R为NHNH 2,R 1为苯基且R <2>是Cl,W和Y不同时为CCH3; R 2和R 2之一是NR 3 R 4,另一个是卤素,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炔基或氰基; R 1是芳基,杂芳基,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, ,或其中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,或与氮原子一起 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( C 1-6)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 -C 6烷氧羰基,C 1-6烷氧基羰基, 6卤代烷氧基,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烷基取代 甲基),并且任何前述芳基或杂芳基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 2-6烯氧基,C 2-6炔氧基,卤代(C 1-6)烷基,卤代(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, 烷氧基(C 1-6)烷基,C 1-6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,异氰基,氰硫基,异硫氰酸根合,硝基,-NHCOR“ R“”,“ON”,“R”“,SO2R”',-OSO R“', - ”“,”NR“或-N = CR”'R“”,其中R“'和R”“独立地为氢,C 1-4烷基,卤代(C1- 4)烷基,C 1-4烷氧基,卤代(C 1〜
    • 3. 发明专利
    • DE60312889T2
    • 2008-01-17
    • DE60312889
    • 2003-12-03
    • SYNGENTA LTDSYNGENTA PARTICIPATIONS AG
    • CROWLEY PATRICK JELFDOBLER MARKUSMUELLER URSWILLIAMS JOHN S
    • C07D487/04A01N43/90C07D471/04
    • 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, thiomopholine, 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.
    • 8. 发明专利
    • FUNGICIDES BASED ON NITROGEN-CONTAINING HETEROCYCLES
    • CA2510376A1
    • 2004-07-08
    • CA2510376
    • 2003-12-03
    • SYNGENTA LTDSYNGENTA PARTICIPATIONS AG
    • DOBLER MARKUSCROWLEY PATRICK JELFMUELLER URSWILLIAMS JOHN
    • C07D471/04C07D487/04A01N43/90
    • 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 CR8; R8 is H, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio or halo(C1-4)alkyl; R and R2 are independently H, halo, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C2-8alkenyl, C2-8 alkynyl, cyano or NR3R4, provided that at least one of R and R2 is NR3R 4; R1 is halo, C1-8 alkyl, C2-8 alkenyl, C2-8alkynyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-6)~-alkyl, C1-8 alkoxy, C1-8 alkylthio, aryl, aryloxy, arylthi o, heteroaryl, heteroaryloxy, heteroarylthio, aryl(C1-4)alkyl, aryl(C1-4)alkoxy , heteroaryl(C1-4)alkyl, heteroaryl~(C1-4)alkoxy, aryl(C1-4)alkylthio, heteroaryl(C1-4)alkylthio, morpholino, piperidino or pyrrolidino; R3 and R4 are independently H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, aryl(C1-8 )~- alkyl, C3-8cycloalkyl, C3-8 cycloalkyl(C1-6)alkyl, heteroaryl, heteroaryl(C 1- 8)alkyl, NR5R6, provided that not both R3 and R4 are H or NR5R6, or R3 and R 4 together form a C3-7 alkylene or C3-7 alkenylene chain optionally substitute d with one or more C1-4 alkyl or C1-4 alkoxy groups, or, together with the nitrogen atom to which they are attached, R3 and R4 form a morpholine, thiomorpholine, thiomorpholine S-oxide or thiomorpholine S-dioxide ring or a piperazine or piperazine N-(C1-4)alkyl (especially N-methyl) ring; and R5 an d R6 are independently H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, aryl(C 1- 8)~alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-6)alkyl, heteroaryl or heteroaryl(C1-8)alkyl; any of the foregoing alkyl, alkenyl, alkynyl or cycloalkyl groups or moieties (other than for R8) being optionally substitut ed with halogen, cyano, C1-6 alkoxy, C1-6alkylcarbonyl, C1-6 alkoxycarbonyl, C1 -6 haloalkoxy, C1-6 alkylthio, tri(C1-4)alkylsilyl, C1-6 alkylamino or C1-6 dialkylamino, any of the foregoing morpholine, thiomorpholine, piperidine, piperazine and pyrrolidine rings being optionally substituted with C1-4 alky l (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, C1-6alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C2-6 alkenyloxy, C2-6 alkynyloxy, halo(C1-6)alkyl, halo(C1-6)alkoxy, C1-6 alkylthio, halo(C1-6)alkylthio, hydroxy(C1-6)alkyl, C1-4 alkoxy(C1- 6)alkyl, C3-6 cycloalkyl, C3-6cycloalkyl(C1-4)alkyl, phenoxy, benzyloxy, benzoyloxy, cyano, isocyano, thiocyanato, isothiocyanato, nitro, -NR"'R"", NHCOR"', -NHCONR"'R"", -CONR"'R"", -SO2R"', -OSO2R"', -COR"', -CR"'=NR"" or - N=CR "'R"", in which R"' and R"" are independently hydrogen, C1-4 alkyl, hal o- (C1-4)alkyl, C1-4 alkoxy, halo(C1-4)alkoxy, C1-4 alkylthio, C3-6 cycloalkyl, C3-6 cycloalkyl(C1-4)alkyl, phenyl or benzyl, the phenyl and benzyl groups being optionally substituted with halogen, C1-4 alkyl or C1-4 alkoxy.
    • 10. 发明专利
    • NAPHTHYRIDINE DERIVATIVES AND THEIR USE AS FUNGICIDES
    • CA2507670A1
    • 2004-07-08
    • CA2507670
    • 2003-12-03
    • SYNGENTA LTDSYNGENTA PARTICIPATIONS AG
    • MUELLER URSCROWLEY PATRICK JELFWILLIAMS JOHNDOBLER MARKUS
    • A01N43/90C07D471/04
    • Fungicidal compositions of the general formula (1): wherein one of W, X, Y a nd Z is N and the others are CR8; R8 is H, halo, C1-4 alkyl, C1-4 alkoxy or halo(C1-4)alkyl, provided that when X is CH, Z is N, R is NHNH2, R1 is pheny l and R2 is Cl, W and Y are not both CCH3; one of R and R2 is NR3R4 and the other is halo, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C2-8 alkenyl, C2-8 alkynyl or cyano; R1 is aryl, heteroaryl, morpholino, piperidino or pyrrolidino; R3 and R4 are independently H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, aryl(C1-8)-alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-6)alkyl , heteroaryl, heteroaryl(C1-8)alkyl, NR5R6, provided that not both R3 and R4 a re H or NR5R6,or R3 and R4 together form a C3-7 alkylene or C3-7 alkenylene cha in optionally substituted with one or more C1-4 alkyl or C1-4 alkoxy groups, or , together with the nitrogen atom to which they are attached, R3 and R4 form a morpholine, thiomorpholine, thiomorpholine S-oxide or thiomorpholine S-dioxi de ring or a piperazine or piperazine N-(C1-4)alkyl (especially N-methyl) ring; and R5 and R6 are independently H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, aryl(Cl-8)-alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-6)alkyl, heteroaryl or heteroaryl(C1-8)alkyl; any of the foregoing alkyl, alkenyl, alkynyl or cycloalkyl groups or moieties (other than for R8) being optionall y substituted with halogen, cyano, C1-6 alkoxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 haloalkoxy, C1-6 alkylthio, tri(C1-4)alkylsilyl, C1-6 alkylamino or C1-6 ialkylamino, any of the foregoing morpholine, thiomorpholine, piperidine, piperazine and pyrrolidine rings being optionall y substituted with C1-4 alkyl (especially methyl), and any of the foregoing ar yl or heteroaryl groups or moieties being optionally substituted with one or mo re substituents selected from halo, hydroxy, mercapto, C1-6 alkyl, C2-6 alkenyl , C2-6 alkynyl, C1-6 alkoxy, C2-6 alkenyloxy, C2-6 alkynyloxy, halo(C1-6)alkyl , halo(C1-6)alkoxy, C1-6 alkylthio, halo(C1-6)alkylthio, hydroxy(C1-6)alkyl, C 1- 4 alkoxy(C1-6)alkyl, C 1-6 cycloalkyl, C3-6 cycloalkyl(C1-4)alkyl, phenoxy, benzyloxy, benzoyloxy, cyano, isocyano, thiocyanato, isothiocyanato, nitro, - NHCOR"', -NHCONR"'R"", -CONK"'R"", SO2R"', -OSO2R"', -COR"', -CR"'=NR" or - N=CR "'R"", in which R"' and R"" are independently hydrogen, C1-4 alkyl, hal o- (C1-4)alkyl, C1-4 alkoxy, halo(C1-4)alkoxy, C1-4 alkylthio, C3-6 cycloalkyl, C3-6 cycloalkyl(C 1-4)alkyl, phenyl or benzyl groups beings optionally substituted with halogen, C1-4 alkyl or C1-4 alkoxy.