首页> 外国专利> 5 - fosforilaminopirazol Derivatives, method for their preparation, compositions containing pesticides, the use thereof for the manufacture of a product and a method for controlling pests that uses.

5 - fosforilaminopirazol Derivatives, method for their preparation, compositions containing pesticides, the use thereof for the manufacture of a product and a method for controlling pests that uses.

机译:5-磷乙胺基吡唑醇衍生物,其制备方法,含有农药的组合物,其在产品生产中的用途以及用于控制使用的害虫的方法。

摘要

This refers to Derivatives of 5 - foasforilaminopirazol. Processes for their preparation, compositions, and their use to control pests (including insects and Worms).Claim 1: a compound of the formula (1): R1 is cn or csnh2; W Halogen is C - C or - CH3, N; R2 is H, halogen, CH3 or nr8r9; R3 is haloalquilo C1 - 3 to - 3, haloalcoxi C1 or C2; R4 is H, alquenilo - 6 haloalquenilo C2 - 6, 6 - haloalquinilo alquinilo C2, C2 - C3 - 7 6, cycloalkyl alkyl -, CO2 - C1 6 CO2 alquenilo C3 - 6, 6 - alquinilo C3 - CO2, CO2 - (CH2) cor11 MR10, or so2r12,C1 - 6 or alkyl unsubstituted or substituted with one or more selected from the group formed by radical Halogen, alkoxy haloalcoxi C1 C1 - 6, - 6, - 6 haloalqueniloxi alqueniloxi C3, C3 - 6 - 6, alquiniloxi C3, C3 C3 haloalquiniloxi cycloalkyl - 6, - 7, S (OR) pr13, NS, Oh, cor11, NO2, nr8r9, S (OR) PR10 or10, and CO2 R11; X is o or s; R5 and R6 are each independently alquenilo haloalquenilo C3 C3 - 6 - 6Alquinilo haloalquinilo C3 C3 - 6, - 6, - 7 pp. ISBN cycloalkyl, R10, R14, NH2, Oh, alkyl and alkyl - 6 C1, C1 or C3 yalquenilo - 6 - 6, where the last three Radicals mentioned above are not replaced or substituted with one or more selected from the group consisting of halogen Radicals, 6 - alkoxy C1, haloalc Oxy - 6 alqueniloxi C1, C3 C3 haloalqueniloxi - 6, - 6, - 6 haloalquiniloxi alquiniloxi C3, C3 - 6Cycloalkyl C3 - 7, S (OR) pr13, CN, NO2, Oh, cor15, nr8r9, or10, R10, R14 and co2r15; or each and cycloalkyl - C3 - 7 unsubstituted or substituted with one or more selected from the group formed by radical Halogen, alkyl haloalquilo C1 and C1 - 6 - 6 or is Each One and - R10 or R5 and R6; together with the Atom United Phosphorus can form a Ring of 56 or 7 members saturated or unsaturated which is not replaced or radical is substituted with one or more selected from the group formed by Halogen, alkyl haloalquilo C1 and C1 - 6 - 6; and is o, s or nr8; R7 and R13 are each independently alkyl haloalquilo C1 C1 - 6 - 6, alquenilo C2 - 6, halo Alquenilo C2 - 6, 6 - haloalquinilo alquinilo C2 or C2 - 6; R8 and R9 are each independently h,Rent haloalquilo C1 C1 - 6, - 6, - 6 haloalquenilo alquenilo C3, C3 C3 alquinilo - 6, - 6, - 7 cicloalquil C3 or cycloalkyl alkyl C1 - C3 - 7 - 6; or with the R8 and R9 n Atom together form a Ring of 5 or 6 members which optionally saturated contains a heteroatom in The Ring which additional Select o, s and NWhere the ring is not replaced or radical is substituted with one or more selected from the group formed by Halogen, alkyl haloalquilo C1 and C1 - 6 - 6; R10 is unsubstituted or substituted phenyl radical with one or more selected from the group formed by Halogen, alkyl of C1 - 6, haloalquilo C1 - 6, 6 - alkoxy haloalcoxi C1, C1 - 6 ns, NO2, S (OR) pr15, cor8, cor16, conr8r9, so2nr8r9,Nr8r9 and Oh; R11 is C1 - 6 h, alkyl, cycloalkyl haloalquilo C1 - C3 - 6, 7, cicloalquil C1 C3 alkyl - 6 - 7 - (CH2) or cycloalkyl QR10; R12 is alquenilo C3 C3 - 7 - 6, 6 - alquinilo haloalquenilo C3, C3 C3 - 6 - 6, haloalquinilo R10 or alkyl radical C1 - 6 whose last mentioned is not replaced or replacement Radical left with one or more selected from the group formed by Halogen, alkoxy C1 - 6Haloalcoxi C1 - C3 - alqueniloxi 6, 6, 6 alquiniloxi haloalqueniloxi C3, C3 - 6, haloalquiniloxi cycloalkyl C3 C3 - 6, - 7, S (OR) pr13, CN, NO2, Oh, cor15, nr11cor13, nr11so2r13, conr8r11, nr8r11 or10, and co2r15; heterociclilo R14 is replaced or not replaced with one or more selected from the group of radical Formed by c1-4 alkyl, halogen, haloalquilo c1-4, haloalcoxi C1 - 4 NS, CO2, NO2, alkyl C1 - 6S (o) pr15, oh and oxo; R15 is alkyl or haloalquilo C1 C1 - 6 - 6; R16 is unsubstituted or substituted phenyl radical with one or more selected from the group formed by Halogen, alkyl of C1 - 6, 6 - alkoxy haloalquilo C1, C1 - 6 - 6, haloalcoxi C1 CN; No2.S (o) pr15 and nr8r9; n and P are each independently 0, 1 or 2; M and q are each independently 0 OR 1; and in each heterociclilo Radicals mentioned above is regardless a Heterocyclic radical with 3 to 7 Atoms in the ring and 1, 2 or 3 heteroatoms in the ring. Onados group consisting of N, o and S; Pesticide or its acceptable Salt.Claim 2: a process for the preparation of a compound of the formula (1) or its Salt as defined in any of claims 1 to 5, which includes: (a) where a is cn and R1, R2, R3, R4, R5, R6, R7, W, X and N are defined as in claim 1, by reacting a compound of L Formula (2); where the different values are as defined in claim 1,A compound of formula (3), R5, R6, and x are as defined in claim 1, and L is a leaving Group; or (b) where R1 is CN, and R2, R3, R4, R5, R7, W, X and N are as defined in claim 1 nr8r9 R6, and, Oh,And alkyl - 6 or - C1 and C3 6 alquenilo whose last 2 Radicals mentioned above are not replaced or substituted with one or more selected from the group formed by radical Halogen, alkoxy haloalcoxi C1 C1 - 6, - 6, - 6 haloalqueniloxi alqueniloxi C3, C3 - 6, 6 - haloalquiniloxi alquiniloxi C3, C3 - 6, CIC Loalquilo C3 - 7, S (OR) pr13, CN, NO2, Oh, cor15, nr8r9, or10 R10R14 and co2r15; or are each and cycloalkyl - C3 - 7 unsubstituted or substituted with one or more selected from the group formed by radical Halogen, alkyl haloalquilo C1 and C1 - 6 - 6; or are each and R10, reacting a compound of formula (4 or group where L1 is outgoing s and other values On as defined in claim 1,A compound of the formula (5) R6 h; where R6 are as defined in claim 1; or (c) where R1 is CN, and R2, R3, R4, R5, R7, W, X and N are as defined in claim 1, and R6 is nr8r9, Oh, and alkyl - 6 or - C1 and C3 6 alquenilo whose last 2 Radicals mentioned above are not replaced S or are replaced with one or more selected from the group consisting of halogen Radicals,6 - alkoxy haloalcoxi C1, C1 - C3 - alqueniloxi 6, 6, 6 alquiniloxi haloalqueniloxi C3, C3 - 6, haloalquiniloxi cycloalkyl C3 C3 - 6, - 7, S (OR) pr13, CN, NO2, Oh, cor15, nr8r9 or10, R10, R14, and each one is and co2r15; or cycloalkyl - C3 - 7 unsubstituted or substituted with one or more selected Radicals of Grup Formed by alkyl or Halogen, C1 and C1 haloalquilo - 6, - 6, and - are each R10Reacting a compound of formula (6): where L1 is a leaving Group, and the other values are as defined in claim 1, a compound of the formula (2) as defined above, to give the compound corresponding to formula (4), followed by reaction with a com Since the formula (5) as defined above; or (d) where R1 is CN, and R2, R3, R4, R7,W, X and N are as defined in claim 1, and R5 and R6 are each independently nr8r9, Oh, and alkyl - 6 or - C1 and C3 6 alquenilo whose last 2 Radicals mentioned above are not replaced or substituted with one or more selected from the group formed by radical Halogen, alkoxy Haloalcoxi C1 - 6, C! - 6, 6 - haloalqueniloxi alqueniloxi C3, C3 - 6, 6 - haloalquiniloxi alquiniloxi C3, C3 - 6Cycloalkyl C3 - 7, S (OR) pr13, CN, NO2, Oh, cor15, nr8r9, or10, R10, R14 and co2r15, or are each and cycloalkyl - C3 - 7 unsubstituted or substituted with one or more selected from the group formed by radical Halogen, alkyl haloalquilo C1 and C1 - 6 - 6; or are each and R10, reacting a Compound The Formula (7), where L1 is a leaving Group,And the other values are as defined in claim 1, a compound of the formula 8 R5 or R6 - formula h, 9 h, where R5 and R6 are each independently nr8r9, Oh, and alkyl - 6 or - C1 and C3 6 alquenilo whose last 2 Radicals mentioned above are not replaced or are replaced with a Or more radical selected from the group formed by Halogen, alkoxy haloalcoxi C1 C1 - 6 - 6Alqueniloxi haloalqueniloxi C3 C3 - 6, - 6, - 6 alquiniloxi C3, C3 C3 haloalquiniloxi cycloalkyl - 6, - 7, S (OR) pr13, CN, NO2, Oh, cor15, nr8r9, or10, R10, R14 and co2r15; or are each and cycloalkyl - C3 - unsubstituted or substituted with 7 one or More selected from the group consisting of halogen Radicals, alkyd ILO haloalquilo C1 and C1 - 6 - 6, and - R10 or are each; or (e) where R1 is CN, and R2, R3, R4, R7, WX and N are as defined in claim 1; and R5 and R6 are each independently nr8r9, Oh, and alkyl C! - 6 - 6 or - alquenilo and C3 Radicals whose last 2 mentioned above are not replaced or substituted with one or more selected from the group formed by radical Halogen, alkoxy haloalcoxi C1 C1 - 6, - 6, - 6 alquiniloxi alqueniloxi C3, C3 - 6, haloalquiniloxi cycloalkyl C3 C3 - 6, - 7.S (o) pr13, CN, NO2, Oh, cor15, nr8r9, or10, R10, R14 and co2r15; or are each and cycloalkyl - C3 - 7 unsubstituted or substituted with one or more selected from the group formed by radical Halogen, alkyl haloalquilo C1 and C1 - 6 - 6; or each and - R10, reacting a compound of formula (10) Where L1 is a leaving Group with a compound of formula (2) as defined above,The Compound corresponding to formula (7) as defined above, followed by reaction with a compound of formula (8) or (9) as defined above; (f) where R1 or R2 is nr8r9 is CN, and other values are as defined in claim 1 make reac The Compound of the formula (1) wherein R2 is Halogen,A compound of the formula (11) or its Salt r8r9n - H where R8 and R9 are as defined in claim 1; or (g) where R1 is csnh2, and other values are as defined in claim 1, reacting The Compound corresponding to formula (1) wherein R1 is cn with a D, HYDROSULFIDE And alkali or Alkaline Earth Metal, or with H2S in the presence of an organic base.Or with the Reagent ph2ps2; or (H) where R1 is csnh2, and other values are as defined in claim 1, reacting The Compound corresponding to formula (1) wherein R1 is CN, with a bis (trialquilsilil) SULFIDE in the presence of a base; or (i) where R1 and
机译:这是指5-foasforilaminopirazol的衍生物。制备方法,组合物及其用于防治害虫(包括昆虫和蠕虫)的方法。权利要求1:式(1)的化合物:R1为cn或csnh2; W卤素是C-C或-CH3,N; R2是H,卤素,CH3或nr8r9; R3是卤代alquilo C1-3至-3,卤代alcoxi C1或C2; R4是H,alquenilo-6卤代alquenilo C2-6,6-卤代喹啉alquinilo C2,C2-C3-7 6,环烷基烷基-,CO2-C1 6 CO2 alquenilo C3-6,6,6-alquinilo C3-CO2,CO2-(CH2 )cor11 MR10或so2r12,C1-6或未被取代或被一个或多个选自以下基团的烷基取代:卤素,烷氧基卤代烷氧基C1 C1-6,-6,-6卤代烷烃基alqueniloxi C3,C3-6-6, Alquiniloxi C3,C3 C3卤代喹啉环烷基-6,-7,S(OR)pr13,NS,Oh,cor11,NO2,nr8r9,S(OR)PR10 or10,以及CO2 R11; X是o或s; R 5和R 6各自独立地为Alquenilo haloalquenilo C3-6-6 Alquinilo haloalquinquin C3 C3-6-6-7 pp.ISBN环烷基,R10,R14,NH2,Oh,烷基和烷基-6 C1,C1或C3 yalquenilo- 6-6,其中上述最后三个基团未被卤素基团,6-烷氧基C1,卤代烷氧基Oxy-6烷氧基C1,C3 C3卤代烷氧基中的一种或多种取代或取代。 -6卤代喹啉基alquiniloxi C3,C3-6环烷基C3-7,S(OR)pr13,CN,NO2,Oh,cor15,nr8r9,or10,R10,R14和co2r15;环烷基-C 3-7未取代或被选自卤素,烷基卤代烷基C 1和C 1-6-6形成的组中的一个或多个取代,或各自为-R 10或R 5和R 6;或与原子联合磷一起可以形成56或7个饱和或不饱和的环,该环未被取代或自由基被选自卤素,烷基卤代alquilo C1和C1-6-6形成的组中的一种或多种取代或被基团取代。并且是o,s或nr8; R7和R13各自独立地为烷基卤代alquiloCl C1-6-6,烷基alquenilo C2-6,卤代烷基alquenilo C2-6,6-卤代喹啉alquinilo C2或C2-6; R 8和R 9各自独立地为:h,Rent卤代alquilo C1-6--6--6卤代alquenilo Alquenilo C3,C3 C3 alquinilo-6-6-7 cicloalquil C3或环烷基C1-C3-7-6;或与R8和R9 n原子一起形成5或6个成员的环,该环可选地饱和包含在该环中​​的杂原子,其另外选择o,s和N,其中环不被取代或自由基被选自以下的一个或多个取代由卤素,烷基卤代烷基C1和C1-6-6形成的基团; R 10是未被取代的或被取代的苯基,其具有一个或多个选自卤素,C 1-6的烷基,卤代alquilo的C 1-6,6-烷氧基的卤代醇C 1,C 1-6 ns,NO 2,S(OR)pr15,cor8 ,cor16,conr8r9,so2nr8r9,Nr8r9和Oh; R11为C1-6h烷基,环烷基,卤代烷基C1至C3-6、7,环烷基C1至C3烷基-6-7-(CH2)或环烷基QR10; R 12是alquenilo C3 C3-6-6,-alquinilo haloalquenilo C3,C3 C3-6-6,卤代喹啉R10或烷基C1-6,其最后一个未被取代或被取代的基团,其自由基残基是从形成的组中选择的一个或多个由卤素,烷氧基C1-6,卤代烷C1-C3-喹啉6、6、6卤代喹啉卤代烷3,C3-6,卤代喹啉环烷基C3 C3-6-7,S(OR)pr13,CN,NO2,Oh,cor15,nr11cor13 ,nr11so2r13,conr8r11,nr8r11 or10和co2r15;杂环基R14被一个或多个选自以下的基团取代或不取代:c1-4烷基,卤素,卤代alquilolo c1-4,卤代考克司C1-4NS,CO2,NO2,烷基C1-6s(o)pr15,哦,还有氧R15是烷基或卤代烷基C1C1-6-6; R16是未取代的或取代的苯基,其具有一个或多个选自卤素,C1-6、6-烷氧基卤代alquiloCl,C1-6-6,卤代烷氧基C1 CN的烷基; No2.S(o)pr15和nr8r9; n和P分别独立地为0、1或2; M和q分别独立为0或1;在上述每个杂基自由基中,无论是在环中具有3至7个原子,在环中具有1、2或3个杂原子的杂环基团。由N,o和S组成的Onados组;农药或其可接受的盐。权利要求2:制备如权利要求1-5中任一项所定义的式(1)化合物或其盐的方法,该方法包括:(a)其中a为cn且R1,R2权利要求1中,R 3,R 4,R 5,R 6,R 7,W,X和N通过使L式(2)的化合物反应而定义。其中不同的值如权利要求1所定义,式(3)的化合物,R5,R6和x如权利要求1所定义,且L为离去基团; (b)R1为CN,R2,R3,R4,R5,R7,W,X和N如权利要求1所定义。nr8r9 R6,以及,-烷基,烷基-6或-C1和C3 6为烷基,上面提到的最后2个基团没有被选自卤素,烷氧基卤代醇盐C1 C1-6-6-6卤代烷烃3,C3-6、6-卤代喹啉基alquiniloxi C3形成的组中的一种或多种取代或取代,C3-6,CIC Loalquilo C3-7,S(OR)pr13,CN,NO2,Oh,cor15,nr8r9或10 R10R14和co2r15;或环烷基-C3-7各自未被取代或被选自卤素,烷基卤代alquilolo C1和C1-6-6形成的组中的一种或多种取代;式(4)的化合物或基团,其中L 1为输出的s和其它值On,如权利要求1所述,或式(5)的化合物为R 6 h;其中R 6如权利要求1所定义;或(c)其中R1为CN,且R2,R3,R4,R5,R7,W,X和N如权利要求1所定义,并且R6为nr8r9,Oh和烷基-6或-C1和C3 6烷基其最后2个基团未被取代的S或被一个或多个选自卤素基团的基团取代,6-烷氧基卤代alcoxi C1,C1-C3-烷氧基西洛西6,6,6,alquiniloxi卤代烷氧基C3,C3-6,卤代喹啉基环烷基C3 -6--7,S(OR)pr13,CN,NO2,Oh,cor15,nr8r9或10,R10,R14和各自为and co2r15;或环烷基-C3-7未取代或被一个或一个取代由烷基或卤素,C 1和C 1卤代alquilo-6,-6和-形成的更多选择的基团基团分别是R 10反应式(6)的化合物:其中L 1是离去基团,并且其他值如权利要求中所定义1,化合物,如上所定义的式(2),得到对应于式(4)的化合物,然后与化合物反应。或(d)其中R1为CN,且R2,R3,R4,R7,W,X和N如权利要求1所定义,并且R5和R6各自独立地为nr8r9,Oh和烷基-6或-C1和C3 6个上述提到的最后2个基团没有被一个或多个选自卤素,烷氧基卤代醇C1-6,C! -6,6-卤代喹啉基C3,C3-6,6,6-卤代喹啉基alquiniloxi C3,C3-6环烷基C3-7,S(OR)pr13,CN,NO2,哦,cor15,nr8r9,or10,R10,R14和co2r15,或环烷基-C3-7各自未被取代或被选自卤素,烷基卤代alquilolo C1和C1-6-6形成的组中的一种或多种取代;或R 10和R 10各自是使式(7)的化合物反应,其中L 1是离去基团,以及其他值如权利要求1所定义,式8的化合物R 5或R 6-式h,9h, R 5和R 6各自独立地为nr 8r 9,Oh和烷基-6或-C 1和C 3 6烷基,其上述最后两个基团未被取代或被一个或多个选自卤素,烷氧基卤代烷氧基C 1 C 1的基团取代。 -6-6 Alqueniloxi卤代烷基C3 C3-6-6-6 alquiniloxi C3,C3 C3卤代喹啉基环烷基-6、7,S(OR)pr13,CN,NO2,Oh,cor15,nr8r9,or10,R10,R14和co2r15;或分别为环烷基-C 3-未被取代或被7个一个或多个选自卤素基团,醇酸ILO卤代alquilolo C 1和C 1-6-6和-R 10的一个或多个,或各自为;或(e)其中R1是CN,并且R2,R3,R4,R7,WX和N如权利要求1所定义;或R5和R6分别独立地为nr8r9,Oh和烷基C! -6-6或-alquenilo和C3基团,其上述最后2个基团未被选自由卤素,烷氧基卤代醇盐C1 C1 -6--6-6 alquiniloxi alqueniloxi C3,C3形成的组中的一种或多种取代或取代-6,卤代喹啉基环烷基C3,C3-6,-7.S(o)pr13,CN,NO2,Oh,cor15,nr8r9,or10,R10,R14和co2r15;或环烷基-C3-7各自未被取代或被选自卤素,烷基卤代alquilolo C1和C1-6-6形成的组中的一种或多种取代;或-和R 10中的每一个与-R 10,其中L 1为离去基团的式(10)化合物与如上定义的式(2)化合物反应,与如上定义的式(7)对应的化合物,然后与化合物反应如上定义的式(8)或(9); (f)其中R1或R2为nr8r9为CN,且其他值如权利要求1中所定义。式(1)的化合物,其中R2为卤素,式(11)的化合物或其盐r8r9n-H其中R8和R9如权利要求1所定义;或(g),其中R1为csnh2,且其他值如权利要求1所定义,使其中R1为cn的对应于式(1)的化合物与D,氢硫化物和碱金属或碱土金属,或与H2S反应有机碱或与试剂ph2ps2一起使用;或(H),其中R 1为csnh 2,且其他值如权利要求1所定义,在碱的存在下,使对应于其中R 1为CN的式(1)的化合物与双(三芳基硅烷基)硫化物反应;或或(i)其中R1和

著录项

  • 公开/公告号AR048070A1

    专利类型

  • 公开/公告日2006-03-29

    原文格式PDF

  • 申请/专利权人 BAYER CROPSCIENCE S.A.;

    申请/专利号AR2005P100676

  • 发明设计人

    申请日2005-02-24

  • 分类号C07F9/24;C07F9/6503;A01N57/32;A61K31/675;

  • 国家 AR

  • 入库时间 2022-08-21 21:40:29

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