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    Process for the preparation of substituted difluorobenzo-1,3-dioxoles
    32.
    发明授权
    Process for the preparation of substituted difluorobenzo-1,3-dioxoles 失效
    制备取代的二氟苯-1,3-二氧杂环戊烯的方法

    公开(公告)号：US5514816A

    公开(公告)日：1996-05-07

    申请号：US440172

    申请日：1995-05-12

    申请人： Peter Ackermann ,  Hans-Ruedi Kanel ,  Bruno Schaub

    发明人： Peter Ackermann ,  Hans-Ruedi Kanel ,  Bruno Schaub

    IPC分类号： A61K31/33 ,  C07D317/06 ,  C07D317/46 ,  C07D405/04 ,  C07F1/00 ,  C07F1/02 ,  C07F3/00 ,  C07F5/02 ,  C07F7/08 ,  C07F7/10 ,  C07F19/00

    CPC分类号： C07D405/04 ,  C07D317/46 ,  C07F1/00 ,  C07F1/02 ,  C07F19/00 ,  C07F3/00 ,  C07F5/025 ,  C07F7/0814 ,  C07F7/10 ,  Y02P20/55

    摘要： The reaction of 2,2-difluorobenzo-1,3-dioxole with (a) an alkali metal or an alkali metal compound and then (b) a compound R.sup.1 -Z.sup.1 in which Z.sup.1 is a leaving group, or with an aldehyde produces compounds of formula I ##STR1## wherein R.sup.1 is --OH, --SH, --CHO, --CN, --COOH, --B(OH).sub.2, --COX, with X being C1 or Br, or is --COOR.sup.2, --SiR.sup.2.sub.3 or --B(OR.sup.2).sub.2, with R.sup.2 being a C.sub.1 -C.sub.12 alcohol moiety without the hydroxy group, wherein R.sup.1 is further --C.sub.n H.sub.2n COOR.sup.2, with n being an integer from 1 to 4, or linear or branched C.sub.1 -C.sub.12 hydroxyalkyl which is unsubstituted or is substituted by --F, --CN, C.sub.1 -C.sub.6 alkoxy, phenyl, fluorophenyl, C.sub.1 -C.sub.4 alkoxy-phenyl, C.sub.1 -C.sub.4 alkylthio-phenyl, C.sub.1 -C.sub.4 alkylphenyl, C.sub.1 -C.sub.4 fluoroalkyl-phenyl, nitrophenyl or by cyanophenyl, or wherein R.sup.1 is a benzyl alcohol which is unsubstituted or is substituted by F, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 fluoroalkyl, nitro or by cyano, or is C.sub.1 -C.sub.12 acyl, or wherein R.sup.1 is a radical of formula II ##STR2## wherein R.sup.5 is --CN, --CF.sub.3, --COOR.sup.2, --CONH.sup.2, --CO--NHR.sup.2 or --CONR.sup.2.sub.2, R.sup.3 and R.sup.4 are a direct bond or each is H, or R.sup.3 is H and R.sup.4 independently has the meanings of R.sup.5, or R.sup.3 and R.sup.4 together are --CH.sub.2 --NR.sup.6 --CH.sub.2 --, --CH.sub.2 --NR.sup.6 --CO-- or --CO--NR.sup.6 --CO-- wherein R.sup.6 is the radical of a removable protecting group, or wherein further R.sup.1 is a radical of formula III ##STR3## Insecticides or fungicides can be prepared from the compounds of formula I.

    摘要翻译： 2,2-二氟苯-1,3-二氧杂环戊烯与（a）碱金属或碱金属化合物反应，然后（b）其中Z 1为离去基团的化合物R1-Z1或与醛反应生成化合物 其中R 1是-OH，-SH，-CHO，-CN，-COOH，-B（OH）2，-COX，X是C1或Br，或是-COOR2， - SiR 23或-B（OR 2）2，其中R 2是没有羟基的C 1 -C 12醇部分，其中R 1还是-C n H 2n COOR 2，n是1至4的整数，或未被取代的直链或支链C 1 -C 12羟基烷基 或被-F，-CN，C 1 -C 6烷氧基，苯基，氟苯基，C 1 -C 4烷氧基 - 苯基，C 1 -C 4烷硫基 - 苯基，C 1 -C 4烷基苯基，C 1 -C 4氟烷基 - 苯基，硝基苯基或氰基苯基取代，或其中R 1是 未被取代或被F，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基，C 1 -C 4氟烷基，硝基或氰基取代的苯甲醇，或者是C 1 -C 12酰基，或其中R 1是式II基团 -CONH 2，-CO-NHR 2或-CONR 22，R 3和R 4是直接键 或各自为H或R 3为H且R 4独立地具有R 5的含义，或者R 3和R 4一起为-CH 2 -NR 6 -CH 2 - ， - CH 2 -NR 6 -CO-或-CO-NR 6 -CO-，其中R 6为 可除去的保护基团的基团，或其中R 1为式III的基团。（III）杀虫剂或杀真菌剂可由式I化合物制备。

    Process for the preparation of substituted difluorobenzo-1,3-dioxoles
    33.
    发明授权
    Process for the preparation of substituted difluorobenzo-1,3-dioxoles 失效
    制备取代的二氟苯-1,3-二氧杂环戊烯的方法

    公开(公告)号：US5496848A

    公开(公告)日：1996-03-05

    申请号：US440171

    申请日：1995-05-12

    申请人： Peter Ackermann ,  Hans-Ruedi Ka/ nel ,  Bruno Schaub

    发明人： Peter Ackermann ,  Hans-Ruedi Ka/ nel ,  Bruno Schaub

    IPC分类号： A61K31/33 ,  C07D317/06 ,  C07D317/46 ,  C07D405/04 ,  C07F1/00 ,  C07F1/02 ,  C07F3/00 ,  C07F5/02 ,  C07F7/08 ,  C07F7/10 ,  C07F19/00

    CPC分类号： C07D405/04 ,  C07D317/46 ,  C07F1/00 ,  C07F1/02 ,  C07F19/00 ,  C07F3/00 ,  C07F5/025 ,  C07F7/0814 ,  C07F7/10 ,  Y02P20/55

    摘要： The reaction of 2,2-difluorobenzo-1,3-dioxole with (a) an alkali metal or an alkali metal compound and then (b) a compound R.sup.1 -Z.sup.1 in which Z.sup.1 is a leaving group, or with an aldehyde produces compounds of formula I ##STR1## wherein R.sup.1 is --OH, --SH, --CHO, --CN, --COOH, --B(OH).sub.2, --COX, with X being Cl or Br, or is --COOR.sup.2, --SIR.sup.2.sub.3 or --B(OR.sup.2).sub.2, with R.sup.2 being a C.sub.1 -C.sub.12 alcohol moiety without the hydroxy group, wherein R.sup.1 is further --C.sub.n H.sub.2n COOR.sup.2, with n being an integer from 1 to 4, or linear or branched C.sub.1 -C.sub.12 hydroxyalkyl which is unsubstituted or is substituted by --F, --CN, C.sub.1 -C.sub.6 alkoxy, phenyl, fluorophenyl, C.sub.1 -C.sub.4 alkoxy-phenyl, C.sub.1 -C.sub.4 alkylthio-phenyl, C.sub.1 -C.sub.4 alkyl-phenyl, C.sub.1 -C.sub.4 fluoroalkyl-phenyl, nitrophenyl or by cyanophenyl, or wherein R.sup.1 is a benzyl alcohol which is unsubstituted or is substituted by F, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 fluoroalkyl, nitro or by cyano, or is C.sub.1 -C.sub.12 acyl, or wherein R.sup. 1 is a radical of formula II ##STR2## wherein R.sup.5 is --CN, --CF.sub.3, --COOR.sup.2, --CONH.sup.2, --CO--NHR.sup.2 or --CONR.sup.2.sub.2, R.sup.3 and R.sup.4 are a direct bond or each is H, or R.sup.3 is H and R.sup.4 independently has the meanings of R.sup.5, or R.sup.3 and R.sup.4 together are --CH.sub.2 --NR.sup.6 --CH.sub.2 --, --CH.sub.2 --NR.sup.6 --CO-- or --CO--NR.sup.6 --CO-- wherein R.sup.6 is the radical of a removable protecting group, or wherein further R.sup.1 is a radical of formula III ##STR3## Insecticides or fungicides can be prepared from the compounds of formula I.3-(2,2-difluorobenzodioxol-4-yl)-4-cyanopyrrole can be prepared by reacting 4-metallo-2,2-difluorobenzodioxole (III) with an unsaturated nitrile and then with a sulfonylmethyl isocyanide in a one-pot process. The compounds III are novel intermediates.

    摘要翻译： 2,2-二氟苯-1,3-二氧杂环戊烯与（a）碱金属或碱金属化合物反应，然后（b）其中Z 1为离去基团的化合物R1-Z1或与醛反应生成化合物 其中R 1是-OH，-SH，-CHO，-CN，-COOH，-B（OH）2，-COX，X是Cl或Br，或者是-COOR 2， - SIR 23或-B（OR 2）2，其中R 2是没有羟基的C 1 -C 12醇部分，其中R 1还是-C n H 2n NOR 2，n是1至4的整数，或未被取代的直链或支链C 1 -C 12羟基烷基 被-F，-CN，C 1 -C 6烷氧基，苯基，氟苯基，C 1 -C 4烷氧基 - 苯基，C 1 -C 4烷硫基 - 苯基，C 1 -C 4烷基 - 苯基，C 1 -C 4氟烷基 - 苯基，硝基苯基或氰基苯基取代，或其中R 1 未被取代或被F，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基，C 1 -C 4氟烷基，硝基或氰基取代的苄醇或C 1 -C 12酰基，或其中R 1是式II的基团， （II）其中R5是-CN，-CF3，-COOR2，-CONH2，-CO-N HR 2或-CONR 22，R 3和R 4是直接键，或者各自是H，或者R 3是H，R 4独立地具有R 5的定义，或者R 3和R 4一起是-CH 2 -NR 6 -CH 2 - ， - CH 2 -NR 6 -CO - 或-CO-NR6-CO-，其中R6是可除去的保护基团的基团，或其中R 1是式III的基团。（III）杀虫剂或杀真菌剂可以由式I化合物制备。 - （2,2-二氟苯并二氧杂环戊烯-4-基）-4-氰基吡咯可以通过4-金属-2,2-二氟苯并间二氧杂环戊烯（III）与不饱和腈然后与一种磺酰基甲基异氰化物反应来制备。 化合物III是新的中间体。

    Certain 1-(3-pyridyl)-2-phenoxy-alkanones having anti-microbial activity
    35.
    发明授权
    Certain 1-(3-pyridyl)-2-phenoxy-alkanones having anti-microbial activity 失效
    某些具有抗微生物活性的1-（3-吡啶基）-2-苯氧基 - 烷酮

    公开(公告)号：US5036084A

    公开(公告)日：1991-07-30

    申请号：US456057

    申请日：1989-12-21

    申请人： Hans Tobler ,  Peter Ackermann ,  Robert Nyfeler

    发明人： Hans Tobler ,  Peter Ackermann ,  Robert Nyfeler

    IPC分类号： C07D213/28 ,  A01N43/40 ,  A01P3/00 ,  C07D213/30 ,  C07D213/50

    CPC分类号： C07D213/30 ,  A01N43/40 ,  C07D213/50

    摘要： Pyridinyl derivatives of formula I ##STR1## wherein R.sub.1 to R.sub.5 are each independently hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, cyano, C.sub.1 -C.sub.6 alkoxycarbonyl or phenyl,R.sub.6 and R.sub.7 are each independently of the other hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl, or phenyl or benzyl, each of which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 haloalkoxy,R.sub.8 is ##STR2## and R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, or benzyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 haloalkoxy, or R.sub.9 is an acyl radical.The preparation of these compounds and the use thereof in pest control, in particular against bacteria and fungi, are described.

    摘要翻译： 式I的吡啶基衍生物其中R 1至R 5各自独立地为氢，卤素，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基，氰基，C 1 -C 6烷氧基羰基或苯基，R 6和R 7为 C 1 -C 6烷基，C 1 -C 6卤代烷氧基，C 1 -C 6烷氧基或C 1 -C 6卤代烷氧基取代的苯基或苄基， R 8是氢，C 1 -C 6烷基，C 3 -C 6链烯基，C 3 -C 6炔基或苄基，其未被取代或被卤素，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基或C 1 -C 6卤代烷氧基或R 9 是酰基。 描述了这些化合物的制备及其在害虫防治中的用途，特别是针对细菌和真菌的用途。

    Substituted phenoxybenzyl-(Dihalodimethylcyclopropyl-methyl)ethers
    36.
    发明授权
    Substituted phenoxybenzyl-(Dihalodimethylcyclopropyl-methyl)ethers 失效
    取代的苯氧基苄基 - （二卤代二甲基环丙基 - 甲基）醚

    公开(公告)号：US4798912A

    公开(公告)日：1989-01-17

    申请号：US118816

    申请日：1987-11-09

    申请人： Laurenz Gsell ,  Peter Ackermann

    发明人： Laurenz Gsell ,  Peter Ackermann

    IPC分类号： A01N31/14 ,  A01N31/16 ,  C07C43/29 ,  C07C43/225

    CPC分类号： C07C43/29 ,  A01N31/14 ,  A01N31/16

    摘要： Novel substituted phenoxybenzyldihalodimethyl-cyclopropylmethyl ethers of the formula ##STR1## in which X.sub.1 and X.sub.2 each independently of the other represents fluorine, chlorine or bromine;R.sub.1 represents hydrogen or flourine; andR.sub.2 represents hydrogen, fluorine, chlorine, bromine, methyl, trifluoromethyl or methoxy, and, if X.sub.1 and X.sub.2 have different meanings, the optical isomers of the compound of the formula I; processes for the manufacture of those compounds, and compositions containing them for use in pest control, especially for the control of insects, especially the larval stages thereof, that attack plants and animals, and of phytopathogenic fungi. The novel compounds exhibit good activity especially against insects that damage plants in rice crops.

    摘要翻译： 新颖的取代苯基苄基二卤代二甲基 - 环丙基甲基醚，其中X1和X2各自独立地表示氟，氯或溴; R1代表氢或氟; 并且R 2表示氢，氟，氯，溴，甲基，三氟甲基或甲氧基，并且如果X1和X2具有不同含义，则式I化合物的光学异构体; 用于制造这些化合物的方法，以及含有它们的用于病虫害防治的组合物，特别是用于防治攻击植物和动物的昆虫，特别是幼虫阶段以及植物病原性真菌的组合物。 新型化合物表现出良好的活性，特别是对于损害水稻作物中的植物的昆虫。