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1. 发明授权

US5496848A Process for the preparation of substituted difluorobenzo-1,3-dioxoles 失效
标题翻译：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。

2. 发明授权

US5194628A Process for the preparation of substituted difluorobenzo-1,3-dioxoles 失效
标题翻译：制备取代的二氟苯-1,3-二氧杂环戊烯的方法
公开(公告)号：US5194628A
公开(公告)日：1993-03-16
申请号：US583787
申请日：1990-09-14
申请人： Peter Ackermann , Hans-Ruedi Kanel , Bruno Schaub
发明人： Peter Ackermann , Hans-Ruedi Kanel , Bruno Schaub
IPC分类号： 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 l in which Z.sup.1 is a leaving group, or with an aldehyde produces compounds of formula I ##STR1## wherein R.sup.1 l is --OH, --SH, --CHO, --CN, --COOH, --B(OH).sub.2, --COX, with X being Cl or Br, or is --COOR.sup.2, --SiR.sub.3.sup.2 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, --CO--NHR.sup.2 or --CONR.sub.2.sup.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Z1是离去基团或与醛产生的化合物R1-Z1 式I的化合物其中R 1是-OH，-SH，-CHO，-CN，-COOH，-B（OH）2，-COX，X是Cl或Br，或是-COOR 2 ，-SiR 32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，或直链或支链C 1 -C 12羟烷基，其是或者被-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 R1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（II）其中R5是-CN，-CF3，-COOR2，-CO-NHR2 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-NR6-CO-，其中R6是可除去的保护基团的基团，或其中R1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）与不饱和腈然后与磺酰基甲基异氰化物在一锅法中反应来制备。化合物III是新的中间体。

3. 发明授权

US5420301A Process for the preparation of substituted difluorobenzo-1,3-dioxoles 失效
标题翻译：制备取代的二氟苯-1,3-二氧杂环戊烯的方法
公开(公告)号：US5420301A
公开(公告)日：1995-05-30
申请号：US147617
申请日：1993-11-05
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 , C07D317/50 , C07D317/52 , C07D317/54
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.sub.3.sup.2 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.sub.2.sup.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 32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为苄基醇，其未被取代或被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，或者是C 1 -C 12酰基，或其中R 1是式II基团。（II）其中R5是-CN，-CF3，-COOR2，-CONH2，-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是可除去的保护基的基团，或其中R 1是式III的基团由式I化合物制备。3-（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。

4. 发明授权

US5493032A Process for the preparation of substituted difluorobenzo-1,3-dioxoles 失效
标题翻译：制备取代的二氟苯-1,3-二氧杂环戊烯的方法
公开(公告)号：US5493032A
公开(公告)日：1996-02-20
申请号：US399248
申请日：1995-03-06
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##
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式I（I）

5. 发明授权

US5281718A Process for the preparation of substituted difluorobenzo-1,3-dioxoles 失效
标题翻译：制备取代的二氟苯-1,3-二氧杂环戊烯的方法
公开(公告)号：US5281718A
公开(公告)日：1994-01-25
申请号：US987902
申请日：1992-12-04
申请人： Peter Ackermann , Hans-Ruedi Kanel , Bruno Schaub
发明人： Peter Ackermann , Hans-Ruedi Kanel , Bruno Schaub
IPC分类号： C07D317/46 , C07D405/04 , C07F1/00 , C07F1/02 , C07F3/00 , C07F5/02 , C07F7/08 , C07F7/10 , C07F19/00 , C07D207/36
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.sub.3.sup.2 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.sub.2.sup.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 32或-B（OR 2）2，其中R 2为不含羟基的C 1 -C 12醇部分，其中R 1还为-C n H 2n NOR 2，n为1至4的整数，或直链或支链C 1 -C 12羟烷基，被未取代或被-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，或是C 1 -C 12酰基，或其中R 1是式II的基团（*化学结构*）（II）其中R5为 -CN，-CF 3，-COOR 2，-CONH 2，-CO-NHR 2或-CONR 22，R 3和R 4为直接键或各自为H或R 3为H，且R 4独立地具有R 5或R 3和R 4的含义是-CH 2 -NR 6 -CH 2 - ， - CH 2 -NR 6 -CO-或-CO-NR 6 -CO-，其中R 6是可除去保护基团的基团，或其中R 1是式III基团（*化学结构* ）（III）杀虫剂或杀真菌剂可以由式I化合物制备。3-（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-2,2-二氟苯并二氧杂环戊烯（III））与不饱和腈，然后在一锅法中与磺酰基甲基异氰化物反应。化合物III是新的中间体。

6. 发明授权

US5514816A Process for the preparation of substituted difluorobenzo-1,3-dioxoles 失效
标题翻译：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。

7. 发明授权

US5149717A Alkanophenones useful for treating allergies 失效
标题翻译：用于治疗过敏的苯胺酮
公开(公告)号：US5149717A
公开(公告)日：1992-09-22
申请号：US795227
申请日：1991-11-15
申请人： Andreas von Sprecher , Andreas Beck , Bruno Schaub , Robert W. Lang
发明人： Andreas von Sprecher , Andreas Beck , Bruno Schaub , Robert W. Lang
IPC分类号： C07D311/24 , C07D405/04
CPC分类号： C07D405/04 , C07D311/24
摘要： Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.
摘要翻译：其中R 1为未取代或氟化的低级烷基，R 2为氢或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键的通式为（Ⅰ）的取代的烷基苯醌，低级亚烷基，n是1或2，R3是未取代的或被未取代或氟化的低级烷基取代的苯基，被醚化或酯化的羟基，被未取代或低级烷基化的氨基和/或被游离的，酯化的或酰胺化的羧基取代，或者是未取代的低级烷基，被氟和氯取代或被游离的酯化或酰胺化的羧基取代，R4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性质，并且可以使用作为药物中的抗过敏活性成分。

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