CN102307863A - Pyrimidine derivatives, horticultural insecticides comprising said derivatives and method of use thereof - Google Patents

Pyrimidine derivatives, horticultural insecticides comprising said derivatives and method of use thereof Download PDF

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CN102307863A
CN102307863A CN2009801560775A CN200980156077A CN102307863A CN 102307863 A CN102307863 A CN 102307863A CN 2009801560775 A CN2009801560775 A CN 2009801560775A CN 200980156077 A CN200980156077 A CN 200980156077A CN 102307863 A CN102307863 A CN 102307863A
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alkyl
halo
group
alkoxyl group
cycloalkyl
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CN102307863B (en
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原山博人
佐藤英孝
八十川伯朗
中野元文
犬饲佳代
深津浩介
笠原良太
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Nihon Nohyaku Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/541,3-Diazines; Hydrogenated 1,3-diazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/14Ectoparasiticides, e.g. scabicides
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
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    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/38One sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
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  • Dentistry (AREA)
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  • Engineering & Computer Science (AREA)
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  • Agronomy & Crop Science (AREA)
  • Epidemiology (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Pyrimidine derivatives represented by general formula (I) [wherein R1 represents an H, alkyl group, cycloalkyl group, alkenyl group, alkynyl group, haloalkyl group, halocycloalkyl group, haloalkenyl group, haloalkynyl group, alkoxyalkyl group, etc. A represents -O-, -S-, -SO-, or -SO2-; R2 represents a halogen atom, hydroxyl group, cyano group, nitro group, alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkenyl group, haloalkynyl group, halocycloalkyl group, etc. m represents an integer 0 or 1; n represents an integer 0-4; and X represents a nitrogen atom or -CH-.] and salts thereof have excellent insecticidal and miticidal activity and are effective as the active ingredient in horticultural insecticides.

Description

Pyrimidine derivatives, the horticultural pesticide that contains this derivative and method of use thereof
Technical field
The present invention relates to contain novel pyrimidine derivatives and its salt salt, garderning pesticide (agrohorticultural insecticide) or its method of use as effective constituent.
Background technology
Put down in writing pyrimidine derivatives in the patent documentation 1 and 2 respectively and can be used as antiseptic-germicide and weedicide.But they are structurally different with pyrimidine derivatives of the present invention.Patent documentation 3 has been put down in writing the pyrimidine derivatives useful as herbicides.But, do not comprise disclosed substituting group in the pyrimidine derivatives of the present invention at the substituting group of 5 of pyrimidines.In addition, in any prior art document, all do not have to instruct or disclose them to have like the insecticidal activity among the present invention.
Patent documentation 1:WO2007/148093
Patent documentation 2:WO2005/40152
Patent documentation 3:WO2002/38550.
Summary of the invention
The problem that the present invention's invention will solve
In the crop production of agricultural and gardening, still serious because of the infringement that insect etc. causes, and owing to existing medicament had the generation etc. of chemical sproof insect, thereby novel salt, garderning pesticide is developed in expectation.Because of rural labor personnel's aging needs various labour-saving application process, and need develop salt, garderning pesticide with the character that is suitable for this application process.
The means of dealing with problems
The inventor has carried out deep research in order to develop novel salt, garderning pesticide; And find that the pyrimidine derivatives by formula (I) expression of the present invention is the novel cpd that document is not put down in writing; And the crop salt, garderning pesticide is useful, and the result has accomplished the present invention.
That is, the present invention relates to
[1] pyrimidine derivatives or its salt of representing by formula (I),
Figure 704616DEST_PATH_IMAGE001
Wherein, R 1Be
(a1) hydrogen atom;
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (alkylthio) (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a22) aryl (C 1-C 6) alkyl;
(a23) has 1~5 identical or different substituent aryl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Hydrogen atom, (C can identical or different and respectively do for oneself 1-C 6) alkyl, (C 3-C 6) cycloalkyl, (C 2-C 6) thiazolinyl, (C 2-C 6) alkynyl, (C 3-C 6) cycloalkyl (C 1-C 6) alkyl, halo (C 1-C 6) alkyl, halo (C 3-C 6) cycloalkyl, halo (C 2-C 6) thiazolinyl, halo (C 2-C 6) alkynyl, halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl, phenyl or phenyl (C 1-C 6) alkyl, perhaps R 3And R 4Can bonding and form and contain a nitrogen-atoms and then optional 1 or 2 identical or different heteroatomic 5~8 yuan nitrogen heterocyclic ring that is selected from Sauerstoffatom, sulphur atom and the nitrogen-atoms that contains;
(a24) cyanic acid (C 1-C 6) alkyl;
(a25) nitro (C 1-C 6) alkyl;
(a26) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a27) (R 3) OC (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a28) (R 3) O 2C (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a29) R 3(R 4) NCO (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a32) aryl sulfonyl;
(a33) have 1~5 identical or different substituent aryl sulfonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a34) aryl carbonyl;
(a35) have 1~5 identical or different substituent aryl carbonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a36) arylthio (arylthio) (C 1-C 6) alkyl;
(a37) has 1~5 identical or different substituent arylthio (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a38) aryl sulfinyl (C 1-C 6) alkyl;
(a39) has 1~5 identical or different substituent aryl sulfinyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a40) aryl sulfonyl (C 1-C 6) alkyl;
(a41) has 1~5 identical or different substituent aryl sulfonyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a42) aryl carbonyl oxygen (C 1-C 6) alkyl;
(a43) has 1~5 identical or different substituent aryl carbonyl oxygen (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a44) (C 1-C 6) alkyl-carbonyl;
(a45) (C 1-C 6) alkoxy carbonyl;
(a46) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a47) R 3(R 4) N ketonic oxygen (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a50) (C 1-C 6) alkoxy carbonyl oxygen (C 1-C 6) alkyl;
(a51) (C 1-C 6) alkyl (C 1-C 6) alkylsulfonyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo;
(a54) heterocycle (C 1-C 6) alkyl;
(a55) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo; Perhaps
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different,
A is-O-,-S-,-SO-or-SO 2-,
R 2Can be identical or different, each is naturally
(b1) halogen atom;
(b2) hydroxyl;
(b3) cyanic acid;
(b4) nitro;
(b5) N (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b6) N (R 3) CO (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b7) N (R 3) SO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b8) N (R 3) CO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b9) CO (R 3) group, wherein R 3Like above-mentioned definition;
(b10) CO 2(R 3) group, wherein R 3Like above-mentioned definition;
(b11) CON (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b12) C (R 3)=NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b13) (C 1-C 12) alkyl;
(b14) (C 2-C 12) thiazolinyl;
(b15) (C 2-C 12) alkynyl;
(b16) (C 3-C 12) cycloalkyl;
(b17) halo (C 1-C 12) alkyl;
(b18) halo (C 2-C 12) thiazolinyl;
(b19) halo (C 2-C 12) alkynyl;
(b20) halo (C 3-C 12) cycloalkyl;
(b21) three (C 1-C 12) the alkyl silyl, wherein said alkyl can be identical or different;
(b22) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b23) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b24) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b25) (C 3-C 12) cycloalkyl (C 3-C 12) cycloalkyl;
(b26) (C 1-C 12) alkoxyl group;
(b27) (C 2-C 12) alkene oxygen base;
(b28) (C 2-C 12) alkynyloxy group;
(b29) (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b30) halo (C 1-C 12) alkoxyl group;
(b31) halo (C 2-C 12) alkene oxygen base;
(b32) halo (C 2-C 12) alkynyloxy group;
(b33) halo (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b34) (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b35) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b36) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(b37) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b38) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b39) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b40) sulfydryl;
(b41) (C 1-C 12) alkylthio;
(b42) (C 2-C 12) alkenylthio group (alkenylthio group);
(b43) (C 2-C 12) alkynes sulfenyl (alkynylthio group);
(b44) (C 3-C 12) the cycloalkyl sulfenyl;
(b45) halo (C 1-C 12) alkylthio;
(b46) halo (C 2-C 12) alkenylthio group;
(b47) halo (C 2-C 12) the alkynes sulfenyl;
(b48) halo (C 3-C 12) the cycloalkyl sulfenyl;
(b49) (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b50) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b51) (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b52) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b53) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b54) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b55) (C 1-C 12) the alkyl sulfinyl;
(b56) (C 2-C 12) the thiazolinyl sulfinyl;
(b57) (C 2-C 12) the alkynyl sulfinyl;
(b58) (C 3-C 12) the cycloalkyl sulfinyl;
(b59) halo (C 1-C 12) the alkyl sulfinyl;
(b60) halo (C 2-C 12) the thiazolinyl sulfinyl;
(b61) halo (C 2-C 12) the alkynyl sulfinyl;
(b62) halo (C 3-C 12) the cycloalkyl sulfinyl;
(b63) (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b64) halo (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b65) (C 1-C 12) alkyl sulphonyl;
(b66) (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b67) (C 2-C 12) the alkynyl alkylsulfonyl;
(b68) (C 3-C 12) the naphthene sulfamide base;
(b69) halo (C 1-C 12) alkyl sulphonyl;
(b70) halo (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b71) halo (C 2-C 12) the alkynyl alkylsulfonyl;
(b72) halo (C 3-C 12) the naphthene sulfamide base;
(b73) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b74) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b75) aryl;
(b76) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b77) aryl (C 1-C 6) alkyl;
(b78) has 1~5 identical or different substituent aryl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b79) aryloxy;
(b80) have 1~5 identical or different substituent aryloxy, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b81) aryloxy (C 1-C 6) alkyl;
(b82) has 1~5 identical or different substituent aryloxy (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b83) arylthio;
(b84) have 1~5 identical or different substituent arylthio, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b85) pyridyl oxygen base;
(b86) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl oxygen base in alkyl, (d) cyanic acid and (e) nitro;
(b87) pyridyl sulfenyl (pyridylthio group);
(b88) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl sulfenyl in alkyl, (d) cyanic acid and (e) nitro;
(b89) halo (C 1-C 6) alkylenedioxy group;
(b90) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b91) (C 3-C 8) alkylidene group;
(b92) (C 1-C 6) alkyl (C 3-C 8) alkylidene group;
(b93) three (C 1-C 12) alkyl siloxy, wherein said alkyl can be identical or different;
(b94) three (C 1-C 12) alkyl silyl (C 1-C 6) alkoxyl group, wherein said alkyl can be identical or different;
(b95) two (C 1-C 12) halogenated alkyl (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b96) two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b97) two (C 1-C 12) the alkyl hydroxy silyl, wherein said alkyl can be identical or different;
(b98) two (C 1-C 12) alkyl hydrogen silyl (alkylhydrosilyl), wherein said alkyl can be identical or different;
(b99) two (C 1-C 12) the alkyl phenyl silyl, wherein said alkyl can be identical or different;
(b100) (C 1-C 6) alkylthio (C 1-C 6) alkoxyl group;
(b101) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkoxyl group;
(b102) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkoxyl group;
(b103) (C 1-C 6) alkoxy carbonyl (C 1-C 6) alkoxyl group;
(b104) (C 1-C 6) alkyl-carbonyl (C 1-C 6) alkoxyl group;
(b105) cyanic acid (C 1-C 6) alkoxyl group;
(b106) aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation;
(b107) has 1~5 identical or different substituent aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation, and said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b108) hydroxyl (C 1-C 6) alkyl;
(b109) (C 1-C 6) alkylthio (C 1-C 6) alkyl-carbonyl;
(b110) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(b111) three (C 1-C 12) alkyl silyl (C 1-C 6) alkylthio, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b112) three (C 1-C 12) alkyl silyl (C 1-C 6) the alkyl sulfinyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b113) three (C 1-C 12) alkyl silyl (C 1-C 6) alkyl sulphonyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b114) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(b115) heterocyclic radical;
(b116) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b117) heterocyclic oxy group except that pyridyl oxygen base;
(b118) have 1~5 identical or different substituent heterocyclic oxy group except that pyridyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b119) the heterocycle sulfenyl except that the pyridyl sulfenyl;
(b120) have 1~5 identical or different substituent heterocycle sulfenyl except that the pyridyl sulfenyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b121) heterocycle sulfinyl;
(b122) have 1~5 identical or different substituent heterocycle sulfinyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b123) heterocycle alkylsulfonyl;
(b124) have 1~5 identical or different substituent heterocycle alkylsulfonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b125) heterocycle (C 1-C 6) alkyl oxy;
(b126) have 1~5 identical or different substituent Heterocyclylalkyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b127) (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b128) halo (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b129) group that is expressed from the next:
R wherein 3And R 4Like above-mentioned definition, R 5Be hydrogen atom, (C 1-C 6) alkyl, (C 3-C 6) cycloalkyl, (C 2-C 6) thiazolinyl, (C 2-C 6) alkynyl, (C 3-C 6) cycloalkyl (C 1-C 6) alkyl, halo (C 1-C 6) alkyl, halo (C 3-C 6) cycloalkyl, halo (C 2-C 6) thiazolinyl, halo (C 2-C 6) alkynyl, halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl, phenyl or phenyl (C 1-C 6) alkyl;
(b130) 4,4,5,5-tetramethyl--1,2,3-dioxane pentaborane-2-base;
(b131) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(b132) two (C 1-C 12) the alkyl benzyl silyl, wherein said alkyl can be identical or different;
(b133) heterocycle (C 1-C 6) alkyl; Perhaps
(b134) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo, perhaps
R 2Can with adjacent R on the aromatic nucleus 2Form (b135) condensed ring or dicyclo together, this condensed ring or dicyclo are optional to have one or more identical or different substituting group, and said substituting group is selected from: (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) alkyl, (d) (C 1-C 6) alkoxyl group, (e) halo (C 1-C 6) alkoxyl group, (f) (C 1-C 6) alkylthio, (g) halo (C 1-C 6) alkylthio, (h) (C 1-C 6) alkyl sulfinyl, (i) halo (C 1-C 6) alkyl sulfinyl, (j) (C 1-C 6) alkyl sulphonyl and (k) halo (C 1-C 6) alkyl sulphonyl,
M is 0 or 1 integer, and n is 0~4 integer, and
X be optional oxidized nitrogen-atoms or-CH-;
[2] according to above-mentioned [1] described pyrimidine derivatives or its salt,
Wherein A, R 2, definition in m, n and X such as above-mentioned [1],
R 1Be
(a1) hydrogen atom;
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a22) aryl (C 1-C 6) alkyl;
(a23) has 1~5 identical or different substituent aryl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like definition in above-mentioned [1];
(a24) cyanic acid (C 1-C 6) alkyl;
(a25) nitro (C 1-C 6) alkyl;
(a26) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a27) (R 3) OC (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a28) (R 3) O 2C (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a32) aryl sulfonyl;
(a33) have 1~5 identical or different substituent aryl sulfonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a34) aryl carbonyl;
(a35) have 1~5 identical or different substituent aryl carbonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a36) arylthio (C 1-C 6) alkyl;
(a37) has 1~5 identical or different substituent arylthio (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a38) aryl sulfinyl (C 1-C 6) alkyl;
(a39) has 1~5 identical or different substituent aryl sulfinyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a40) aryl sulfonyl (C 1-C 6) alkyl;
(a41) has 1~5 identical or different substituent aryl sulfonyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a44) (C 1-C 6) alkyl-carbonyl;
(a45) (C 1-C 6) alkoxy carbonyl;
(a46) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a47) R 3(R 4) N ketonic oxygen (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a50) (C 1-C 6) alkoxy carbonyl oxygen (C 1-C 6) alkyl;
(a51) (C 1-C 6) alkyl (C 1-C 6) alkylsulfonyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo;
(a54) heterocycle (C 1-C 6) alkyl;
(a55) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo; Perhaps
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
[3] according to above-mentioned [1] or [2] described pyrimidine derivatives or its salt,
Wherein definition in m, n and X such as above-mentioned [1],
R 1Be
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like definition in above-mentioned [1] and (t) phenoxy group;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a50) (C 1-C 6) alkoxy carbonyl oxygen (C 1-C 6) alkyl;
(a51) (C 1-C 6) alkyl (C 1-C 6) alkylsulfonyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo; Perhaps
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different,
A is-O-or-S-, and
R 2Can be identical or different, each is naturally
(b1) halogen atom;
(b2) hydroxyl;
(b3) cyanic acid;
(b4) nitro;
(b5) N (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b6) N (R 3) CO (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b7) N (R 3) SO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b8) N (R 3) CO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b9) CO (R 3) group, wherein R 3Like above-mentioned definition;
(b10) CO 2(R 3) group, wherein R 3Like above-mentioned definition;
(b11) CON (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b12) C (R 3)=NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b13) (C 1-C 12) alkyl;
(b14) (C 2-C 12) thiazolinyl;
(b15) (C 2-C 12) alkynyl;
(b16) (C 3-C 12) cycloalkyl;
(b17) halo (C 1-C 12) alkyl;
(b18) halo (C 2-C 12) thiazolinyl;
(b19) halo (C 2-C 12) alkynyl;
(b20) halo (C 3-C 12) cycloalkyl;
(b21) three (C 1-C 12) the alkyl silyl, wherein said alkyl can be identical or different;
(b22) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b23) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b24) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b25) (C 3-C 12) cycloalkyl (C 3-C 12) cycloalkyl;
(b26) (C 1-C 12) alkoxyl group;
(b27) (C 2-C 12) alkene oxygen base;
(b28) (C 2-C 12) alkynyloxy group;
(b29) (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b30) halo (C 1-C 12) alkoxyl group;
(b31) halo (C 2-C 12) alkene oxygen base;
(b32) halo (C 2-C 12) alkynyloxy group;
(b33) halo (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b34) (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b35) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b36) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(b37) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b38) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b39) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b41) (C 1-C 12) alkylthio;
(b42) (C 2-C 12) alkenylthio group;
(b43) (C 2-C 12) the alkynes sulfenyl;
(b44) (C 3-C 12) the cycloalkyl sulfenyl;
(b45) halo (C 1-C 12) alkylthio;
(b46) halo (C 2-C 12) alkenylthio group;
(b47) halo (C 2-C 12) the alkynes sulfenyl;
(b48) halo (C 3-C 12) the cycloalkyl sulfenyl;
(b49) (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b50) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b51) (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b52) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b53) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b54) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b55) (C 1-C 12) the alkyl sulfinyl;
(b56) (C 2-C 12) the thiazolinyl sulfinyl;
(b57) (C 2-C 12) the alkynyl sulfinyl;
(b58) (C 3-C 12) the cycloalkyl sulfinyl;
(b59) halo (C 1-C 12) the alkyl sulfinyl;
(b60) halo (C 2-C 12) the thiazolinyl sulfinyl;
(b61) halo (C 2-C 12) the alkynyl sulfinyl;
(b62) halo (C 3-C 12) the cycloalkyl sulfinyl;
(b63) (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b64) halo (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b65) (C 1-C 12) alkyl sulphonyl;
(b66) (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b67) (C 2-C 12) the alkynyl alkylsulfonyl;
(b68) (C 3-C 12) the naphthene sulfamide base;
(b69) halo (C 1-C 12) alkyl sulphonyl;
(b70) halo (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b71) halo (C 2-C 12) the alkynyl alkylsulfonyl;
(b72) halo (C 3-C 12) the naphthene sulfamide base;
(b73) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b74) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b75) aryl;
(b76) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b79) aryloxy;
(b80) have 1~5 identical or different substituent aryloxy, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b81) aryloxy (C 1-C 6) alkyl;
(b82) has 1~5 identical or different substituent aryloxy (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b83) arylthio;
(b84) have 1~5 identical or different substituent arylthio, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b85) pyridyl oxygen base;
(b86) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl oxygen base in alkyl, (d) cyanic acid and (e) nitro;
(b87) pyridyl sulfenyl;
(b88) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl sulfenyl in alkyl, (d) cyanic acid and (e) nitro;
(b89) halo (C 1-C 6) alkylenedioxy group;
(b90) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b91) (C 3-C 8) alkylidene group;
(b92) (C 1-C 6) alkyl (C 3-C 8) alkylidene group;
(b93) three (C 1-C 12) alkyl siloxy, wherein said alkyl can be identical or different;
(b94) three (C 1-C 12) alkyl silyl (C 1-C 6) alkoxyl group, wherein said alkyl can be identical or different;
(b95) two (C 1-C 12) halogenated alkyl (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b96) two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b97) two (C 1-C 12) the alkyl hydroxy silyl, wherein said alkyl can be identical or different;
(b98) two (C 1-C 12) the alkyl hydrogen silyl, wherein said alkyl can be identical or different;
(b99) two (C 1-C 12) the alkyl phenyl silyl, wherein said alkyl can be identical or different;
(b100) (C 1-C 6) alkylthio (C 1-C 6) alkoxyl group;
(b101) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkoxyl group;
(b102) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkoxyl group;
(b103) (C 1-C 6) alkoxy carbonyl (C 1-C 6) alkoxyl group;
(b104) (C 1-C 6) alkyl-carbonyl (C 1-C 6) alkoxyl group;
(b105) cyanic acid (C 1-C 6) alkoxyl group;
(b106) aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation;
(b107) has 1~5 identical or different substituent aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation, and said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b108) hydroxyl (C 1-C 6) alkyl;
(b109) (C 1-C 6) alkylthio (C 1-C 6) alkyl-carbonyl;
(b110) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(b111) three (C 1-C 12) alkyl silyl (C 1-C 6) alkylthio, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b112) three (C 1-C 12) alkyl silyl (C 1-C 6) the alkyl sulfinyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b113) three (C 1-C 12) alkyl silyl (C 1-C 6) alkyl sulphonyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b114) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(b115) heterocyclic radical;
(b116) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b117) heterocyclic oxy group except that pyridyl oxygen base;
(b118) have 1~5 identical or different substituent heterocyclic oxy group except that pyridyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b119) the heterocycle sulfenyl except that the pyridyl sulfenyl;
(b120) have 1~5 identical or different substituent heterocycle sulfenyl except that the pyridyl sulfenyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b125) heterocycle (C 1-C 6) alkyl oxy;
(b126) have 1~5 identical or different substituent Heterocyclylalkyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b127) (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b128) halo (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b129) group that is expressed from the next:
Figure 997374DEST_PATH_IMAGE003
R wherein 3, R 4And R 5Like definition in above-mentioned [1];
(b130) 4,4,5,5-tetramethyl--1,2,3-dioxane pentaborane-2-base;
(b131) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(b132) two (C 1-C 12) the alkyl benzyl silyl, wherein said alkyl can be identical or different;
(b133) heterocycle (C 1-C 6) alkyl; Perhaps
(b134) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo, perhaps
R 2Can with adjacent R on the aromatic nucleus 2Form (b135) condensed ring or dicyclo together, this condensed ring or dicyclo are optional to have one or more identical or different substituting group, and said substituting group is selected from: (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) alkyl, (d) (C 1-C 6) alkoxyl group, (e) halo (C 1-C 6) alkoxyl group, (f) (C 1-C 6) alkylthio, (g) halo (C 1-C 6) alkylthio, (h) (C 1-C 6) alkyl sulfinyl, (i) halo (C 1-C 6) alkyl sulfinyl, (j) (C 1-C 6) alkyl sulphonyl and (k) halo (C 1-C 6) alkyl sulphonyl;
[4] according to each described pyrimidine derivatives or its salt in above-mentioned [1]~[3],
Wherein definition in m, n and X such as above-mentioned [1],
R 1Be
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo; Perhaps
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different,
A is-O-or-S-, and
R 2Can be identical or different, each is naturally
(b1) halogen atom;
(b4) nitro;
(b13) (C 1-C 12) alkyl;
(b14) (C 2-C 12) thiazolinyl;
(b15) (C 2-C 12) alkynyl;
(b16) (C 3-C 12) cycloalkyl;
(b17) halo (C 1-C 12) alkyl;
(b18) halo (C 2-C 12) thiazolinyl;
(b19) halo (C 2-C 12) alkynyl;
(b20) halo (C 3-C 12) cycloalkyl;
(b21) three (C 1-C 12) the alkyl silyl, wherein said alkyl can be identical or different;
(b22) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b23) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b24) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b25) (C 3-C 12) cycloalkyl (C 3-C 12) cycloalkyl;
(b26) (C 1-C 12) alkoxyl group;
(b27) (C 2-C 12) alkene oxygen base;
(b28) (C 2-C 12) alkynyloxy group;
(b29) (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b30) halo (C 1-C 12) alkoxyl group;
(b31) halo (C 2-C 12) alkene oxygen base;
(b32) halo (C 2-C 12) alkynyloxy group;
(b33) halo (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b34) (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b35) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b36) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(b37) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b38) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b39) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b41) (C 1-C 12) alkylthio;
(b42) (C 2-C 12) alkenylthio group;
(b43) (C 2-C 12) the alkynes sulfenyl;
(b44) (C 3-C 12) the cycloalkyl sulfenyl;
(b45) halo (C 1-C 12) alkylthio;
(b46) halo (C 2-C 12) alkenylthio group;
(b47) halo (C 2-C 12) the alkynes sulfenyl;
(b48) halo (C 3-C 12) the cycloalkyl sulfenyl;
(b49) (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b50) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b51) (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b52) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b53) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b54) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b55) (C 1-C 12) the alkyl sulfinyl;
(b56) (C 2-C 12) the thiazolinyl sulfinyl;
(b57) (C 2-C 12) the alkynyl sulfinyl;
(b58) (C 3-C 12) the cycloalkyl sulfinyl;
(b59) halo (C 1-C 12) the alkyl sulfinyl;
(b60) halo (C 2-C 12) the thiazolinyl sulfinyl;
(b61) halo (C 2-C 12) the alkynyl sulfinyl;
(b62) halo (C 3-C 12) the cycloalkyl sulfinyl;
(b63) (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b64) halo (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b65) (C 1-C 12) alkyl sulphonyl;
(b66) (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b67) (C 2-C 12) the alkynyl alkylsulfonyl;
(b68) (C 3-C 12) the naphthene sulfamide base;
(b69) halo (C 1-C 12) alkyl sulphonyl;
(b70) halo (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b71) halo (C 2-C 12) the alkynyl alkylsulfonyl;
(b72) halo (C 3-C 12) the naphthene sulfamide base;
(b73) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b74) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b75) aryl;
(b76) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b79) aryloxy;
(b80) have 1~5 identical or different substituent aryloxy, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b81) aryloxy (C 1-C 6) alkyl;
(b82) has 1~5 identical or different substituent aryloxy (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b83) arylthio;
(b84) have 1~5 identical or different substituent arylthio, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b85) pyridyl oxygen base;
(b86) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl oxygen base in alkyl, (d) cyanic acid and (e) nitro;
(b87) pyridyl sulfenyl;
(b88) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl sulfenyl in alkyl, (d) cyanic acid and (e) nitro;
(b89) halo (C 1-C 6) alkylenedioxy group;
(b90) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b93) three (C 1-C 12) alkyl siloxy, wherein said alkyl can be identical or different;
(b94) three (C 1-C 12) alkyl silyl (C 1-C 6) alkoxyl group, wherein said alkyl can be identical or different;
(b95) two (C 1-C 12) halogenated alkyl (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b96) two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b99) two (C 1-C 12) the alkyl phenyl silyl, wherein said alkyl can be identical or different;
(b100) (C 1-C 6) alkylthio (C 1-C 6) alkoxyl group;
(b101) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkoxyl group;
(b102) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkoxyl group;
(b106) aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation;
(b107) has 1~5 identical or different substituent aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation, and said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b111) three (C 1-C 12) alkyl silyl (C 1-C 6) alkylthio, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b112) three (C 1-C 12) alkyl silyl (C 1-C 6) the alkyl sulfinyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b113) three (C 1-C 12) alkyl silyl (C 1-C 6) alkyl sulphonyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b114) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(b115) heterocyclic radical;
(b116) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like definition, (t) (C in above-mentioned [1] 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b117) heterocyclic oxy group except that pyridyl oxygen base;
(b118) have 1~5 identical or different substituent heterocyclic oxy group except that pyridyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b125) heterocycle (C 1-C 6) alkyl oxy;
(b126) have 1~5 identical or different substituent Heterocyclylalkyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b127) (C 1-C 12) alkyl (C 3-C 12) cycloalkyl; Perhaps
(b128) halo (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
[5] salt, garderning pesticide, it contains in good grounds above-mentioned [1]~[4] each described pyrimidine derivatives or its salt as effective constituent;
[6] method of use of salt, garderning pesticide, this method comprise that the effective constituent of using according to above-mentioned [5] described salt, garderning pesticide handles plant or soil;
[7] according to each described pyrimidine derivatives or its salt in above-mentioned [1]~[4] as the purposes of salt, garderning pesticide; Deng.
The invention effect
Pyrimidine derivatives of the present invention or its salt have good effect as salt, garderning pesticide.On the other hand, this derivative also demonstrates effect to parasitizing such as the pet animals of dog and cat and such as the insects of domestic animals such as ox, sheep.
Embodiment
In the definition of the formula (I) of pyrimidine derivatives of the present invention, " halo " is meant " halogen atom ", and expression chlorine atom, bromine atoms, iodine atom or fluorine atom." (C 1-C 6) alkyl " be straight or branched alkyl with 1~6 carbon atom; like methyl, ethyl, n-propyl, sec.-propyl, normal-butyl, isobutyl-, sec-butyl, the tertiary butyl, n-pentyl, isopentyl, tert-pentyl, neo-pentyl, 2; 3-dimethyl propyl, 1-ethyl propyl, 1-methyl butyl, n-hexyl, isohexyl, 1; 1,2-trimethylammonium propyl group etc." (C 2-C 6) thiazolinyl " be straight or branched thiazolinyl with 2~6 carbon atoms, like vinyl, allyl group, pseudoallyl, 1-butylene base, crotyl, 2-methyl-2-propenyl, 1-methyl-2-propenyl, 2-methyl isophthalic acid-propenyl, pentenyl, 1-hexenyl etc." (C 2-C 6) alkynyl " be straight or branched alkynyl with 2~6 carbon atoms, like ethynyl, 1-proyl, 2-propynyl, ethyl acetylene base, 2-butyne base, 3-butynyl, 3-methyl isophthalic acid-proyl, 2-methyl-3-proyl, pentynyl, 1-hexyn etc.
" (C 1-C 12) alkyl " be straight or branched alkyl with 1~12 carbon atom; like methyl, ethyl, n-propyl, sec.-propyl, normal-butyl, isobutyl-, sec-butyl, the tertiary butyl, n-pentyl, isopentyl, tert-pentyl, neo-pentyl, 2; 3-dimethyl propyl, 1-ethyl propyl, 1-methyl butyl, n-hexyl, isohexyl, 1; 1,2-trimethylammonium propyl group, heptyl, octyl group, nonyl, decyl, undecyl, dodecyl etc." (C 2-C 12) thiazolinyl " be straight or branched thiazolinyl with 2~12 carbon atoms, like vinyl, allyl group, pseudoallyl, 1-butylene base, crotyl, 2-methyl-2-propenyl, 1-methyl-2-propenyl, 2-methyl isophthalic acid-propenyl, pentenyl, 1-hexenyl, heptenyl, octenyl, nonene base, decene base, undecenyl, dodecenyl succinic etc." (C 2-C 12) alkynyl " be straight or branched alkynyl with 2~12 carbon atoms, like ethynyl, 1-proyl, 2-propynyl, ethyl acetylene base, 2-butyne base, 3-butynyl, 3-methyl isophthalic acid-proyl, 2-methyl-3-proyl, pentynyl, 1-hexyn, heptyne base, octyne base, n-heptylacetylene base, decynyl, hendecyne base, dodecyne base etc.
" (C 3-C 6) cycloalkyl " be cycloalkyl with 3~6 carbon atoms, like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl etc." (C 1-C 6) alkoxyl group " and instance comprise straight or branched alkoxyl group with 1~6 carbon atom; like methoxyl group, oxyethyl group, positive propoxy, isopropoxy, n-butoxy, sec-butoxy, tert.-butoxy, n-pentyloxy, isopentyloxy, uncle's pentyloxy, neopentyl oxygen, 2; 3-dimethyl propoxy-, 1-ethyl propoxy-, 1-methyl butoxy, positive hexyloxy, different hexyloxy, 1; 1,2-trimethylammonium propoxy-etc." (C 2-C 6) alkene oxygen base " and instance comprise straight or branched alkene oxygen base with 2~6 carbon atoms, like propenyloxy group, butenyloxy, amylene oxygen base etc." (C 2-C 6) alkynyloxy group " and instance comprise straight or branched alkynyloxy group with 2~6 carbon atoms, like third alkynyloxy group, fourth alkynyloxy group, penta alkynyloxy group etc.
" (C 3-C 12) cycloalkyl " be cycloalkyl with 3~12 carbon atoms, like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, suberyl, ring octyl group, ring nonyl, ring decyl, ring undecyl, cyclo-dodecyl etc." (C 1-C 12) alkoxyl group " and instance comprise straight or branched alkoxyl group with 1~12 carbon atom; like methoxyl group, oxyethyl group, positive propoxy, isopropoxy, n-butoxy, sec-butoxy, tert.-butoxy, n-pentyloxy, isopentyloxy, uncle's pentyloxy, neopentyl oxygen, 2; 3-dimethyl propoxy-, 1-ethyl propoxy-, 1-methyl butoxy, positive hexyloxy, different hexyloxy, 1; 1,2-trimethylammonium propoxy-, heptan oxygen base, octyloxy, the ninth of the ten Heavenly Stems oxygen base, the last of the ten Heavenly stems oxygen base, undecyl oxygen base, dodecyl oxygen base etc." (C 2-C 12) alkene oxygen base " and instance comprise straight or branched alkene oxygen base with 2~12 carbon atoms, like propenyloxy group, butenyloxy, amylene oxygen base, hexene oxygen base, heptene oxygen base, octene oxygen base, nonene oxygen base, decene oxygen base, undecylene oxygen base, dodecenyl succinic oxygen base etc. " (C 2-C 12) alkynyloxy group " and instance comprise straight or branched alkynyloxy group with 2~12 carbon atoms, like third alkynyloxy group, fourth alkynyloxy group, penta alkynyloxy group, own alkynyloxy group, heptan alkynyloxy group, hot alkynyloxy group, the ninth of the ten Heavenly Stems alkynyloxy group, the last of the ten Heavenly stems alkynyloxy group, hendecyne oxygen base, dodecyne oxygen base etc.
" (C 1-C 6) alkylthio " be straight or branched alkylthio with 1~6 carbon atom; like methylthio group, ethylmercapto group, positive rosickyite base, iprotiazem base, positive butylthio, secondary butylthio, uncle's butylthio, positive penta sulfenyl, isoamyl sulfenyl, uncle's penta sulfenyl, new penta sulfenyl, 2; 3-dimethyl propylene sulfenyl, 1-ethyl rosickyite base, 1-methyl butylthio, just own sulfenyl, dissident's sulfenyl, 1; 1,2-trimethylammonium rosickyite base etc." (C 1-C 6) the alkyl sulfinyl " and instance comprise straight or branched alkyl sulfinyl with 1~6 carbon atom; like methyl sulfinyl; the ethylsulfinyl-1 base; the n-propyl sulfinyl; the sec.-propyl sulfinyl; the normal-butyl sulfinyl; The sec-butyl sulfinyl; Tertiary butyl sulfinyl; The n-pentyl sulfinyl; The isopentyl sulfinyl; The tert-pentyl sulfinyl; The neo-pentyl sulfinyl; 2; 3-dimethyl propyl sulfinyl; 1-ethyl propyl sulfinyl; 1-methyl butyl sulfinyl; The n-hexyl sulfinyl; The isohexyl sulfinyl; 1; 1,2-trimethylammonium propyl group sulfinyl etc." (C 1-C 6) alkyl sulphonyl " and instance comprise straight or branched alkyl sulphonyl with 1~6 carbon atom; like methyl sulphonyl, ethylsulfonyl, n-propyl alkylsulfonyl, sec.-propyl alkylsulfonyl, normal-butyl alkylsulfonyl, sec-butyl alkylsulfonyl, tertiary butyl alkylsulfonyl, n-pentyl alkylsulfonyl, isopentyl alkylsulfonyl, tert-pentyl alkylsulfonyl, neo-pentyl alkylsulfonyl, 2; 3-dimethyl propyl alkylsulfonyl, 1-ethyl propyl alkylsulfonyl, 1-methyl butyl alkylsulfonyl, n-hexyl alkylsulfonyl, isohexyl alkylsulfonyl, 1; 1,2-trimethylammonium sulfonyl propyl base etc.
" (C 1-C 12) alkylthio " and instance comprise straight or branched alkylthio with 1~12 carbon atom; like methylthio group, ethylmercapto group, positive rosickyite base, iprotiazem base, positive butylthio, secondary butylthio, uncle's butylthio, positive penta sulfenyl, isoamyl sulfenyl, uncle's penta sulfenyl, new penta sulfenyl, 2; 3-dimethyl propylene sulfenyl, 1-ethyl rosickyite base, 1-methyl butylthio, just own sulfenyl, dissident's sulfenyl, 1; 1,2-trimethylammonium rosickyite base, heptan sulfenyl, hot sulfenyl, the ninth of the ten Heavenly Stems sulfenyl, the last of the ten Heavenly stems sulfenyl, undecane sulfenyl, dodecane sulfenyl etc." (C 1-C 12) the alkyl sulfinyl " and instance comprise straight or branched alkyl sulfinyl with 1~12 carbon atom; like methyl sulfinyl; the ethylsulfinyl-1 base; the n-propyl sulfinyl; the sec.-propyl sulfinyl; the normal-butyl sulfinyl; The sec-butyl sulfinyl; Tertiary butyl sulfinyl; The n-pentyl sulfinyl; The isopentyl sulfinyl; The tert-pentyl sulfinyl; The neo-pentyl sulfinyl; 2; 3-dimethyl propyl sulfinyl; 1-ethyl propyl sulfinyl; 1-methyl butyl sulfinyl; The n-hexyl sulfinyl; The isohexyl sulfinyl; 1; 1,2-trimethylammonium propyl group sulfinyl; The heptyl sulfinyl; The octyl group sulfinyl; The nonyl sulfinyl; The decyl sulfinyl; The undecyl sulfinyl; Dodecyl sulfinyl etc." (C 1-C 12) alkyl sulphonyl " and instance comprise straight or branched alkyl sulphonyl with 1~12 carbon atom; like methyl sulphonyl; ethylsulfonyl; the n-propyl alkylsulfonyl; the sec.-propyl alkylsulfonyl; the normal-butyl alkylsulfonyl; The sec-butyl alkylsulfonyl; Tertiary butyl alkylsulfonyl; The n-pentyl alkylsulfonyl; The isopentyl alkylsulfonyl; The tert-pentyl alkylsulfonyl; The neo-pentyl alkylsulfonyl; 2; 3-dimethyl propyl alkylsulfonyl; 1-ethyl propyl alkylsulfonyl; 1-methyl butyl alkylsulfonyl; The n-hexyl alkylsulfonyl; The isohexyl alkylsulfonyl; 1; 1,2-trimethylammonium sulfonyl propyl base; The heptyl alkylsulfonyl; The octyl group alkylsulfonyl; The nonyl alkylsulfonyl; The decyl alkylsulfonyl; The undecyl alkylsulfonyl; Dodecyl alkylsulfonyl etc.
" (C 2-C 12) alkenylthio group " and instance comprise straight or branched alkenylthio group with 2~12 carbon atoms, like propylene sulfenyl, butylene sulfenyl, amylene sulfenyl, hexene sulfenyl, heptene sulfenyl, octene sulfenyl, nonene sulfenyl, decene sulfenyl, undecylene sulfenyl, dodecylene sulfenyl etc." (C 2-C 12) the alkynes sulfenyl " and instance comprise straight or branched alkynes sulfenyl with 2~12 carbon atoms, like propine sulfenyl, butine sulfenyl, pentyne sulfenyl, hexin sulfenyl, heptyne sulfenyl, octyne sulfenyl, n-heptylacetylene sulfenyl, decine sulfenyl, hendecyne sulfenyl, dodecyne sulfenyl etc.
" (C 2-C 12) the thiazolinyl sulfinyl " and instance comprise straight or branched thiazolinyl sulfinyl with 2~12 carbon atoms, like propenyl sulfinyl, butenyl sulfinyl, pentenyl sulfinyl, hexenyl sulfinyl, heptenyl sulfinyl, octenyl sulfinyl, nonene base sulfinyl, decene base sulfinyl, undecenyl sulfinyl, dodecenyl succinic sulfinyl etc." (C 2-C 12) the alkynyl sulfinyl " and instance comprise straight or branched alkynyl sulfinyl with 2~12 carbon atoms, like proyl sulfinyl, butynyl sulfinyl, pentynyl sulfinyl, hexyn sulfinyl, heptyne base sulfinyl, octyne base sulfinyl, n-heptylacetylene base sulfinyl, decynyl sulfinyl, hendecyne base sulfinyl, dodecyne base sulfinyl etc.
" (C 2-C 12) the thiazolinyl alkylsulfonyl " and instance comprise straight or branched thiazolinyl alkylsulfonyl with 2~12 carbon atoms, like propenyl alkylsulfonyl, butenyl alkylsulfonyl, pentenyl alkylsulfonyl, hexenyl alkylsulfonyl, heptenyl alkylsulfonyl, octenyl alkylsulfonyl, nonene base alkylsulfonyl, decene base alkylsulfonyl, undecenyl alkylsulfonyl, dodecenyl succinic alkylsulfonyl etc." (C 2-C 12) the alkynyl alkylsulfonyl " and instance comprise straight or branched alkynyl alkylsulfonyl with 2~12 carbon atoms, like proyl alkylsulfonyl, butynyl alkylsulfonyl, pentynyl alkylsulfonyl, hexyn alkylsulfonyl, heptyne base alkylsulfonyl, octyne base alkylsulfonyl, n-heptylacetylene base alkylsulfonyl, decynyl alkylsulfonyl, hendecyne base alkylsulfonyl, dodecyne base alkylsulfonyl etc.
" (C 3-C 6) cycloalkyl oxy " and instance comprise cycloalkyl with 3~6 carbon atoms, like ring propoxy-, cyclobutoxy group, cyclopentyloxy, cyclohexyloxy etc." (C 3-C 12) cycloalkyl oxy; Wherein this cycloalkyl can condense with phenyl ring " instance comprise: have the cycloalkyl of 3~12 carbon atoms, like ring propoxy-, cyclobutoxy group, cyclopentyloxy, cyclohexyloxy, suberyl oxygen base, ring octyl group oxygen base, ring nonyl oxygen base, ring decyl oxygen base, ring undecyl oxygen base, cyclo-dodecyl oxygen base etc.; Perhaps wherein cycloalkyl and phenyl ring condensed group (for example, indane-1-base oxygen base, 1,2,3,4-tetralin-1-base oxygen base etc.)." (C 3-C 12) the cycloalkyl sulfenyl " and instance comprise cycloalkyl sulfenyl with 3~12 carbon atoms, like ring rosickyite base, cyclobutyl sulfenyl, cyclopentyl sulfenyl, cyclohexyl sulfenyl, suberyl sulfenyl, ring octyl group sulfenyl, ring nonyl sulfenyl, ring decyl sulfenyl, ring undecyl sulfenyl, cyclo-dodecyl sulfenyl etc." (C 3-C 12) the cycloalkyl sulfinyl " and instance comprise cycloalkyl sulfinyl with 3~12 carbon atoms, like cyclopropyl sulfinyl, cyclobutyl sulfinyl, cyclopentyl sulfinyl, cyclohexyl sulfinyl, suberyl sulfinyl, ring octyl group sulfinyl, ring nonyl sulfinyl, ring decyl sulfinyl, ring undecyl sulfinyl, cyclo-dodecyl sulfinyl etc." (C 3-C 12) the naphthene sulfamide base " and instance comprise cycloalkyl with 3~12 carbon atoms, like cyclopropyl alkylsulfonyl, cyclobutyl alkylsulfonyl, cyclopentyl alkylsulfonyl, cyclohexyl alkylsulfonyl, suberyl alkylsulfonyl, ring octyl group alkylsulfonyl, ring nonyl alkylsulfonyl, ring decyl alkylsulfonyl, ring undecyl alkylsulfonyl, cyclo-dodecyl alkylsulfonyl etc.
At above-mentioned " (C 1-C 6) alkyl ", " (C 2-C 6) thiazolinyl ", " (C 2-C 6) alkynyl ", " (C 3-C 6) cycloalkyl ", " (C 3-C 6) cycloalkyl oxy ", " (C 3-C 12) cycloalkyl oxy, wherein this cycloalkyl can condense with phenyl ring ", " (C 1-C 6) alkoxyl group ", " (C 2-C 6) alkene oxygen base ", " (C 2-C 6) alkynyloxy group ", " (C 1-C 6) alkylthio ", " (C 1-C 6) the alkyl sulfinyl ", " (C 1-C 6) alkyl sulphonyl ", " (C 2-C 12) alkenylthio group ", " (C 2-C 12) the alkynes sulfenyl ", " (C 2-C 12) the thiazolinyl sulfinyl ", " (C 2-C 12) the alkynyl sulfinyl ", " (C 2-C 12) the thiazolinyl alkylsulfonyl ", " (C 2-C 12) the alkynyl alkylsulfonyl ", " (C 1-C 12) alkyl ", " (C 2-C 12) thiazolinyl ", " (C 2-C 12) alkynyl ", " (C 3-C 12) cycloalkyl ", " (C 1-C 12) alkoxyl group ", " (C 2-C 12) alkene oxygen base ", " (C 2-C 12) alkynyloxy group ", " (C 1-C 12) alkylthio ", " (C 3-C 12) the cycloalkyl sulfenyl ", " (C 1-C 12) the alkyl sulfinyl ", " (C 3-C 12) the cycloalkyl sulfinyl ", " (C 1-C 12) alkyl sulphonyl " and " (C 3-C 12) the naphthene sulfamide base " in, one or more halogen atom can replace on can substituted position, and when substituted halogen atom number is 2 when above, these halogen atoms can be identical or different.They are expressed as " halo (C respectively 1-C 6) alkyl ", " halo (C 2-C 6) thiazolinyl ", " halo (C 2-C 6) alkynyl ", " halo (C 3-C 6) cycloalkyl ", " halo (C 3-C 6) cycloalkyl oxy ", " halo (C 3-C 12) cycloalkyl oxy, wherein this cycloalkyl can condense with phenyl ring ", " halo (C 1-C 6) alkoxyl group ", " halo (C 2-C 6) alkene oxygen base ", " halo (C 2-C 6) alkynyloxy group ", " halo (C 1-C 6) alkylthio ", " halo (C 1-C 6) the alkyl sulfinyl ", " halo (C 1-C 6) alkyl sulphonyl ", " halo (C 2-C 12) alkenylthio group ", " halo (C 2-C 12) the alkynes sulfenyl ", " halo (C 2-C 12) the thiazolinyl sulfinyl ", " halo (C 2-C 12) the alkynyl sulfinyl ", " halo (C 2-C 12) the thiazolinyl alkylsulfonyl ", " halo (C 2-C 12) the alkynyl alkylsulfonyl ", " halo (C 1-C 12) alkyl ", " halo (C 2-C 12) thiazolinyl ", " halo (C 2-C 12) alkynyl ", " halo (C 3-C 12) cycloalkyl ", " halo (C 1-C 12) alkoxyl group ", " halo (C 2-C 12) alkene oxygen base ", " halo (C 2-C 12) alkynyloxy group ", " halo (C 1-C 12) alkylthio ", " halo (C 3-C 12) the cycloalkyl sulfenyl ", " halo (C 1-C 12) the alkyl sulfinyl ", " halo (C 3-C 12) the cycloalkyl sulfinyl ", " halo (C 1-C 12) alkyl sulphonyl " and " halo (C 3-C 12) the naphthene sulfamide base ".
" three (C 1-C 6) the alkyl silyl " and " three (C 1-C 12) the alkyl silyl " and instance comprise straight or branched trialkylsilkl with 1~12 carbon atom, like trimethyl silyl, triethylsilyl, t-butyldimethylsilyl, ethyl dimetylsilyl, sec.-propyl dimetylsilyl, n-propyl dimetylsilyl etc.At this moment, three alkyl can be identical or different.
Two (C 1-C 12) halogenated alkyl (C 1-C 6) instance of alkyl silyl comprises chloromethyl dimetylsilyl etc.At this moment, two alkyl can be identical or different.
Two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) instance of alkyl silyl comprises methylthiomethyl dimetylsilyl etc.At this moment, two alkyl can be identical or different.
Two (C 1-C 12) instance of alkyl hydrogen silyl comprises di-isopropyl silyl etc.At this moment, two alkyl can be identical or different.
Two (C 1-C 12) instance of alkyl hydroxy silyl comprises dimethyl hydroxyl silyl etc.At this moment, two alkyl can be identical or different.
Two (C 1-C 12) instance of alkyl phenyl silyl comprises dimethyl (phenyl) silyl etc.At this moment, two alkyl can be identical or different.
Two (C 1-C 12) instance of alkyl benzyl silyl comprises dimethyl (benzyl) silyl etc.At this moment, two alkyl can be identical or different.
The instance of " aryl " comprises the aromatic hydrocarbyl with 6~10 carbon atoms, like phenyl, 1-naphthyl, 2-naphthyl etc.
" (C 1-C 12) ", " (C 2-C 12) ", " (C 3-C 12) " etc. form of presentation represent the scope of each substituent carbonatoms.And above-mentioned definition is applicable to the wherein above-mentioned group group of bonding each other.For example, " (C 1-C 6) alkoxyl group (C 1-C 6) alkyl " be meant that the straight or branched alkoxyl group with 1~6 carbon atom is bonded to the straight or branched alkyl with 1~6 carbon atom.
" (C 3-C 8) alkylidene group ", " (C 1-C 6) alkyl (C 3-C 8) alkylidene group " and " halo (C 1-C 6) alkylenedioxy group " be can be by two adjacent R 2Group bridging and the group that forms, and " (C 3-C 8) alkylidene group " and " (C 1-C 6) alkyl (C 3-C 8) alkylidene group " and instance comprise: propylidene, butylidene, pentylidene, hexylidene, 1,1,4,4-tetramethyl-butylidene etc.; " halo (C 1-C 6) alkylenedioxy group " and instance comprise difluoro methylene dioxy base, tetrafluoro ethylidene dioxy base etc.
By R 3And R 4Each other bonding form, contain a nitrogen-atoms, also optionally contain 1 or 2 identical or different heteroatomic 5~8 yuan nitrogenous heterocyclic instance that is selected from Sauerstoffatom, sulphur atom and the nitrogen-atoms and comprise: tetramethyleneimine, piperidines, morpholine, thiomorpholine, piperazine, high piperidines (homopiperidine), high piperazine (homopiperazine), perhydro azepine
Figure 383225DEST_PATH_IMAGE004
(perhydroazepine) etc.
Can be by two adjacent R 2The condensed ring that forms and the instance of dicyclo comprise: condensed ring, and such as tetraline, naphthalene, benzo two
Figure 786524DEST_PATH_IMAGE005
Luxuriant (benzodioxole), benzo two
Figure 45467DEST_PATH_IMAGE005
Alkane, indane, indoles, cumarone, thionaphthene, benzoglyoxaline, benzothiazole, benzo
Figure 737480DEST_PATH_IMAGE005
Azoles etc.; Dicyclo, such as 1,2,3,4-tetrahydrochysene-1,4-endo-methylene group naphthalene, 1,2,3,4-tetrahydrochysene-1,4-ethano-naphthalene etc.
The instance of " heterocyclic radical " and " heterocycle " comprising: 5-or the monocyclic aromatic heterocyclic radical of 6-unit or the monocycle non-aromatic heterocycle of 3-to 6-unit, and wherein each self-contained Sauerstoffatom, sulphur atom and unitary 1~4 heteroatoms of being selected from is as the ring atom except that carbon atom; By this monocyclic aromatic or non-aromatic heterocyclic and phenyl ring condensation and the annelated heterocycles base; And by (heterocycle can the be different) condensation of this monocyclic aromatic or non-aromatic heterocyclic the annelated heterocycles base.
"Aromatic heterocyclic group" include: monocyclic aromatic heterocyclic group such as furyl, thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, pyrrolyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl,
Figure 474492DEST_PATH_IMAGE005
oxazolyl, isoxazolyl
Figure 997877DEST_PATH_IMAGE005
oxazolyl,
Figure 614672DEST_PATH_IMAGE005
oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, triazinyl, etc.; aromatic fused heterocyclic group such as quinolyl group, iso- quinolyl, quinazolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzo
Figure 590718DEST_PATH_IMAGE005
, benzothiazolyl, iso
Figure 131421DEST_PATH_IMAGE005
thiazolyl, benzothiazolyl, benzimidazolyl, benzotriazolyl , indolyl, indazolyl, pyrrolo pyrazinyl, imidazolyl and pyridyl, imidazolyl and pyrazinyl, pyrazolyl and pyridyl, pyrazolyl, and thienyl, pyrazolyl and triazinyl, etc.; like.
"Non-aromatic heterocyclic group" include: monocyclic non-aromatic heterocyclic group, such as ethylene oxide group, thiirane group, a heterocyclic group, an oxetane group, thiazolyl Tengji (thietanyl), azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, hexamethylene imino (hexamethyleniminyl),
Figure 902456DEST_PATH_IMAGE005
thiazolidinyl, thiazolidinyl , imidazole alkyl,
Figure 237622DEST_PATH_IMAGE005
oxazoline, thiazoline group, imidazoline group, alkenyl group dioxole, dioxolanyl, dihydro
Figure 966543DEST_PATH_IMAGE005
two azole group, 2 - oxo -1,3 - oxazolidine - 5 -, pyranyl, tetrahydropyranyl, thiopyranyl, tetrahydrothiopyranyl, 1 - oxide (oxido) tetrahydrothiopyranyl, 1,1 - dioxide, tetrahydrothiopyranyl, tetrahydrofuranyl , two
Figure 481018DEST_PATH_IMAGE005
alkyl, pyrazolidinyl, pyrazolinyl, tetrahydro-pyrimidinyl, dihydro-triazolyl, tetrahydro-triazolyl group, etc.; fused non-aromatic heterocyclic group, such as indolinyl, di Octahydroisoindole group, dihydro-benzofuranyl, dihydro-benzo
Figure 174037DEST_PATH_IMAGE005
alkenyl, dihydrobenzodioxyl
Figure 390255DEST_PATH_IMAGE005
diazinyl (dihydrobenzodioxepinyl), tetrahydro-benzofuranyl, benzo-pyranyl, dihydro-quinoline group, tetrahydro-quinolyl, isoquinolyl dihydro, tetrahydro-isoquinolyl, dihydro-phthalazine, etc.; like.
"Heterocyclic group" Preferred examples include: isoquinolyl, tetrazolyl group, quinolyl group, iso
Figure 272760DEST_PATH_IMAGE005
oxazolyl, pyrimidinyl, pyrazinyl, pyridyl, pyrazolyl, benzimidazolyl, 2,3 - dioxa-isoindolyl, tetrahydrofuranyl, ethylene oxide groups, ethylene oxide group, a thienyl group, a pyridazinyl group and the like.
The instance of the salt of the pyrimidine derivatives by formula (I) expression of the present invention comprises: inorganic acid salt, such as hydrochloride, vitriol, nitrate, phosphoric acid salt etc.; Organic acid salt is such as acetate, fumarate, maleate, oxalate, mesylate, benzene sulfonate, tosilate etc.; And with the salt of inorganic or organic bases, such as sodium ion, potassium ion, calcium ion, TMA (TriMethylAmine) etc.
Pyrimidine derivatives and salt thereof by formula (I) expression of the present invention can comprise one or a plurality of asymmetric center in structural formula, and can have two kinds or more kinds of optical isomer and diastereomer sometimes.The present invention comprises all these type of optical isomers and contains their mixture with arbitrary proportion.In addition, pyrimidine derivatives and the salt thereof by formula (I) expression of the present invention can have two kinds of geometrical isomers derived from carbon-to-carbon double bond in structural formula.The present invention comprises all geometrical isomers and contains their mixture with arbitrary proportion.
In the pyrimidine derivatives by formula (I) expression of the present invention,
R 1Preferably
(a1) hydrogen atom;
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a22) aryl (C 1-C 6) alkyl;
(a23) has 1~5 identical or different substituent aryl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a24) cyanic acid (C 1-C 6) alkyl;
(a25) nitro (C 1-C 6) alkyl;
(a26) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a27) (R 3) OC (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a28) (R 3) O 2C (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a32) aryl sulfonyl;
(a33) have 1~5 identical or different substituent aryl sulfonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a34) aryl carbonyl;
(a35) have 1~5 identical or different substituent aryl carbonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a36) arylthio (C 1-C 6) alkyl;
(a37) has 1~5 identical or different substituent arylthio (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a38) aryl sulfinyl (C 1-C 6) alkyl;
(a39) has 1~5 identical or different substituent aryl sulfinyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a40) aryl sulfonyl (C 1-C 6) alkyl;
(a41) has 1~5 identical or different substituent aryl sulfonyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a44) (C 1-C 6) alkyl-carbonyl;
(a45) (C 1-C 6) alkoxy carbonyl;
(a46) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a47) R 3(R 4) N ketonic oxygen (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a50) (C 1-C 6) alkoxy carbonyl oxygen (C 1-C 6) alkyl;
(a51) (C 1-C 6) alkyl (C 1-C 6) alkylsulfonyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo;
(a54) heterocycle (C 1-C 6) alkyl;
(a55) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo; Or
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different,
Be more preferably
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a50) (C 1-C 6) alkoxy carbonyl oxygen (C 1-C 6) alkyl;
(a51) (C 1-C 6) alkyl (C 1-C 6) alkylsulfonyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo; Or
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different,
Further preferably
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo; Or
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different.
A preferably-O-or-S-.
R 2Preferably
(b1) halogen atom;
(b2) hydroxyl;
(b3) cyanic acid;
(b4) nitro;
(b5) N (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b6) N (R 3) CO (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b7) N (R 3) SO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b8) N (R 3) CO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b9) CO (R 3) group, wherein R 3Like above-mentioned definition;
(b10) CO 2(R 3) group, wherein R 3Like above-mentioned definition;
(b11) CON (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b12) C (R 3)=NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b13) (C 1-C 12) alkyl;
(b14) (C 2-C 12) thiazolinyl;
(b15) (C 2-C 12) alkynyl;
(b16) (C 3-C 12) cycloalkyl;
(b17) halo (C 1-C 12) alkyl;
(b18) halo (C 2-C 12) thiazolinyl;
(b19) halo (C 2-C 12) alkynyl;
(b20) halo (C 3-C 12) cycloalkyl;
(b21) three (C 1-C 12) the alkyl silyl, wherein said alkyl can be identical or different;
(b22) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b23) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b24) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b25) (C 3-C 12) cycloalkyl (C 3-C 12) cycloalkyl;
(b26) (C 1-C 12) alkoxyl group;
(b27) (C 2-C 12) alkene oxygen base;
(b28) (C 2-C 12) alkynyloxy group;
(b29) (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b30) halo (C 1-C 12) alkoxyl group;
(b31) halo (C 2-C 12) alkene oxygen base;
(b32) halo (C 2-C 12) alkynyloxy group;
(b33) halo (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b34) (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b35) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b36) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(b37) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b38) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b39) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b41) (C 1-C 12) alkylthio;
(b42) (C 2-C 12) alkenylthio group;
(b43) (C 2-C 12) the alkynes sulfenyl;
(b44) (C 3-C 12) the cycloalkyl sulfenyl;
(b45) halo (C 1-C 12) alkylthio;
(b46) halo (C 2-C 12) alkenylthio group;
(b47) halo (C 2-C 12) the alkynes sulfenyl;
(b48) halo (C 3-C 12) the cycloalkyl sulfenyl;
(b49) (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b50) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b51) (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b52) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b53) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b54) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b55) (C 1-C 12) the alkyl sulfinyl;
(b56) (C 2-C 12) the thiazolinyl sulfinyl;
(b57) (C 2-C 12) the alkynyl sulfinyl;
(b58) (C 3-C 12) the cycloalkyl sulfinyl;
(b59) halo (C 1-C 12) the alkyl sulfinyl;
(b60) halo (C 2-C 12) the thiazolinyl sulfinyl;
(b61) halo (C 2-C 12) the alkynyl sulfinyl;
(b62) halo (C 3-C 12) the cycloalkyl sulfinyl;
(b63) (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b64) halo (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b65) (C 1-C 12) alkyl sulphonyl;
(b66) (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b67) (C 2-C 12) the alkynyl alkylsulfonyl;
(b68) (C 3-C 12) the naphthene sulfamide base;
(b69) halo (C 1-C 12) alkyl sulphonyl;
(b70) halo (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b71) halo (C 2-C 12) the alkynyl alkylsulfonyl;
(b72) halo (C 3-C 12) the naphthene sulfamide base;
(b73) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b74) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b75) aryl;
(b76) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b79) aryloxy;
(b80) have 1~5 identical or different substituent aryloxy, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b81) aryloxy (C 1-C 6) alkyl;
(b82) has 1~5 identical or different substituent aryloxy (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b83) arylthio;
(b84) have 1~5 identical or different substituent arylthio, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b85) pyridyl oxygen base;
(b86) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl oxygen base in alkyl, (d) cyanic acid and (e) nitro;
(b87) pyridyl sulfenyl;
(b88) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl sulfenyl in alkyl, (d) cyanic acid and (e) nitro;
(b89) halo (C 1-C 6) alkylenedioxy group;
(b90) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b91) (C 3-C 8) alkylidene group;
(b92) (C 1-C 6) alkyl (C 3-C 8) alkylidene group;
(b93) three (C 1-C 12) alkyl siloxy, wherein said alkyl can be identical or different;
(b94) three (C 1-C 12) alkyl silyl (C 1-C 6) alkoxyl group, wherein said alkyl can be identical or different;
(b95) two (C 1-C 12) halogenated alkyl (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b96) two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b97) two (C 1-C 12) the alkyl hydroxy silyl, wherein said alkyl can be identical or different;
(b98) two (C 1-C 12) the alkyl hydrogen silyl, wherein said alkyl can be identical or different;
(b99) two (C 1-C 12) the alkyl phenyl silyl, wherein said alkyl can be identical or different;
(b100) (C 1-C 6) alkylthio (C 1-C 6) alkoxyl group;
(b101) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkoxyl group;
(b102) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkoxyl group;
(b103) (C 1-C 6) alkoxy carbonyl (C 1-C 6) alkoxyl group;
(b104) (C 1-C 6) alkyl-carbonyl (C 1-C 6) alkoxyl group;
(b105) cyanic acid (C 1-C 6) alkoxyl group;
(b106) aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation;
(b107) has 1~5 identical or different substituent aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation, and said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group;
(b108) hydroxyl (C 1-C 6) alkyl;
(b109) (C 1-C 6) alkylthio (C 1-C 6) alkyl-carbonyl;
(b110) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(b111) three (C 1-C 12) alkyl silyl (C 1-C 6) alkylthio, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b112) three (C 1-C 12) alkyl silyl (C 1-C 6) the alkyl sulfinyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b113) three (C 1-C 12) alkyl silyl (C 1-C 6) alkyl sulphonyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b114) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(b115) heterocyclic radical;
(b116) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b117) heterocyclic oxy group except that pyridyl oxygen base;
(b118) have 1~5 identical or different substituent heterocyclic oxy group except that pyridyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b119) the heterocycle sulfenyl except that the pyridyl sulfenyl;
(b120) have 1~5 identical or different substituent heterocycle sulfenyl except that the pyridyl sulfenyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b125) heterocycle (C 1-C 6) alkyl oxy;
(b126) have 1~5 identical or different substituent Heterocyclylalkyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b127) (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b128) halo (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b129) group that is expressed from the next:
Figure 562927DEST_PATH_IMAGE006
R wherein 3, R 4And R 5Like above-mentioned definition;
(b130) 4,4,5,5-tetramethyl--1,2,3-dioxane pentaborane-2-base;
(b131) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(b132) two (C 1-C 12) the alkyl benzyl silyl, wherein said alkyl can be identical or different;
(b133) heterocycle (C 1-C 6) alkyl; Or
(b134) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo; Perhaps
R 2Can with adjacent R on the aromatic nucleus 2Form (b135) condensed ring or dicyclo together, this condensed ring or dicyclo are optional to have one or more identical or different substituting group, and said substituting group is selected from: (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) alkyl, (d) (C 1-C 6) alkoxyl group, (e) halo (C 1-C 6) alkoxyl group, (f) (C 1-C 6) alkylthio, (g) halo (C 1-C 6) alkylthio, (h) (C 1-C 6) alkyl sulfinyl, (i) halo (C 1-C 6) alkyl sulfinyl, (j) (C 1-C 6) alkyl sulphonyl and (k) halo (C 1-C 6) alkyl sulphonyl,
Be more preferably
(b1) halogen atom;
(b4) nitro;
(b13) (C 1-C 12) alkyl;
(b14) (C 2-C 12) thiazolinyl;
(b15) (C 2-C 12) alkynyl;
(b16) (C 3-C 12) cycloalkyl;
(b17) halo (C 1-C 12) alkyl;
(b18) halo (C 2-C 12) thiazolinyl;
(b19) halo (C 2-C 12) alkynyl;
(b20) halo (C 3-C 12) cycloalkyl;
(b21) three (C 1-C 12) the alkyl silyl, wherein said alkyl can be identical or different;
(b22) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b23) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b24) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b25) (C 3-C 12) cycloalkyl (C 3-C 12) cycloalkyl;
(b26) (C 1-C 12) alkoxyl group;
(b27) (C 2-C 12) alkene oxygen base;
(b28) (C 2-C 12) alkynyloxy group;
(b29) (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b30) halo (C 1-C 12) alkoxyl group;
(b31) halo (C 2-C 12) alkene oxygen base;
(b32) halo (C 2-C 12) alkynyloxy group;
(b33) halo (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b34) (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b35) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b36) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(b37) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b38) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b39) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b41) (C 1-C 12) alkylthio;
(b42) (C 2-C 12) alkenylthio group;
(b43) (C 2-C 12) the alkynes sulfenyl;
(b44) (C 3-C 12) the cycloalkyl sulfenyl;
(b45) halo (C 1-C 12) alkylthio;
(b46) halo (C 2-C 12) alkenylthio group;
(b47) halo (C 2-C 12) the alkynes sulfenyl;
(b48) halo (C 3-C 12) the cycloalkyl sulfenyl;
(b49) (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b50) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b51) (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b52) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b53) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b54) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b55) (C 1-C 12) the alkyl sulfinyl;
(b56) (C 2-C 12) the thiazolinyl sulfinyl;
(b57) (C 2-C 12) the alkynyl sulfinyl;
(b58) (C 3-C 12) the cycloalkyl sulfinyl;
(b59) halo (C 1-C 12) the alkyl sulfinyl;
(b60) halo (C 2-C 12) the thiazolinyl sulfinyl;
(b61) halo (C 2-C 12) the alkynyl sulfinyl;
(b62) halo (C 3-C 12) the cycloalkyl sulfinyl;
(b63) (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b64) halo (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b65) (C 1-C 12) alkyl sulphonyl;
(b66) (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b67) (C 2-C 12) the alkynyl alkylsulfonyl;
(b68) (C 3-C 12) the naphthene sulfamide base;
(b69) halo (C 1-C 12) alkyl sulphonyl;
(b70) halo (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b71) halo (C 2-C 12) the alkynyl alkylsulfonyl;
(b72) halo (C 3-C 12) the naphthene sulfamide base;
(b73) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b74) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b75) aryl;
(b76) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b79) aryloxy;
(b80) have 1~5 identical or different substituent aryloxy, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b81) aryloxy (C 1-C 6) alkyl;
(b82) has 1~5 identical or different substituent aryloxy (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b83) arylthio;
(b84) have 1~5 identical or different substituent arylthio, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b85) pyridyl oxygen base;
(b86) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl oxygen base in alkyl, (d) cyanic acid and (e) nitro;
(b87) pyridyl sulfenyl;
(b88) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl sulfenyl in alkyl, (d) cyanic acid and (e) nitro;
(b89) halo (C 1-C 6) alkylenedioxy group;
(b90) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b93) three (C 1-C 12) alkyl siloxy, wherein said alkyl can be identical or different;
(b94) three (C 1-C 12) alkyl silyl (C 1-C 6) alkoxyl group, wherein said alkyl can be identical or different;
(b95) two (C 1-C 12) halogenated alkyl (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b96) two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b99) two (C 1-C 12) the alkyl phenyl silyl, wherein said alkyl can be identical or different;
(b100) (C 1-C 6) alkylthio (C 1-C 6) alkoxyl group;
(b101) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkoxyl group;
(b102) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkoxyl group;
(b106) aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation;
(b107) has 1~5 identical or different substituent aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation, and said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b111) three (C 1-C 12) alkyl silyl (C 1-C 6) alkylthio, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b112) three (C 1-C 12) alkyl silyl (C 1-C 6) the alkyl sulfinyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b113) three (C 1-C 12) alkyl silyl (C 1-C 6) alkyl sulphonyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b114) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(b115) heterocyclic radical;
(b116) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b117) heterocyclic oxy group except that pyridyl oxygen base;
(b118) have 1~5 identical or different substituent heterocyclic oxy group except that pyridyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b125) heterocycle (C 1-C 6) alkyl oxy;
(b126) have 1~5 identical or different substituent Heterocyclylalkyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo;
(b127) (C 1-C 12) alkyl (C 3-C 12) cycloalkyl; Or
(b128) halo (C 1-C 12) alkyl (C 3-C 12) cycloalkyl.
As X, preferred nitrogen atom (this nitrogen-atoms can be oxidized) or-CH-.
As m, be preferably 0.
As n, be preferably 1,2 or 3.
The following representational preparation method of the expression pyrimidine derivatives by formula (I) expression of the present invention, but the present invention is not limited to this.
In the pyrimidine derivatives by formula (I) expression, A is-compound of O-can be through following preparing method's manufacturing.
The preparation method 1
Figure 505475DEST_PATH_IMAGE007
R wherein 1, R 2, X and n such as above-mentioned definition; L 1Be leavings group, like chlorine atom, bromine atoms, iodine atom etc.; L is B (OH) 2Group or B (OQ) 2Group, the wherein Q (C that can identical or different and respectively do for oneself 1-C 6) alkyl and two Q bonding and forming-CH each other 2CH 2-group or-C (CH 3) 2C (CH 3) 2-group.
Make by the 5-methoxy pyrimidine compound of formula (III) expression with by the compound of formula (IV) expression in the presence of catalyzer and alkali, in inert solvent, react; So that the pyrimidine derivatives by formula (II) expression to be provided; Make this derivative separate or unsegregated situation under hydrogenation and change into derivative by formula (I-A) expression; Make this derivative demethylation under separation or unsegregated situation under separation or unsegregated situation, in this derivative, import R so that the 5-hydroxy pyrimidine derivative by formula (I-B) expression to be provided 1Group is to provide the pyrimidine derivatives by formula (I) expression.
Compound by formula (IV) expression can directly use the commercial product that obtains of ability.For can not the commercial compound that obtains, they can be based on the method manufacturing of putting down in writing among the JP2001-519347 A.
From formula (III) to formula (II)
Make by the pyrimidine compound of formula (III) expression with by the compound of formula (IV) expression in the presence of catalyzer and alkali, in inert solvent, react, so that the pyrimidine derivatives of being represented by formula (II) to be provided.
The instance of the catalyzer that can in this reaction, use comprises: palladium catalyst; Such as palladium-carbon, Palladous chloride, acid chloride, tetrakis triphenylphosphine palladium, [1,1 '-two (diphenylphosphino) ferrocene] dichloro palladium methylene dichloride complex compound, two (triphenylphosphine) palladium chloride etc.The usage quantity of catalyzer is about 0.0001 to 0.1 times of mole with respect to the compound by formula (IV) expression.
The instance of the alkali that can use in the present invention comprises: mineral alkali, such as sodium hydroxide, potassium hydroxide, yellow soda ash, salt of wormwood, cesium carbonate, sodium hydrogencarbonate, saleratus etc.; Organic salt is such as sodium acetate, potassium acetate etc.The usage quantity of alkali is generally about 0.5 to 10 times of mole with respect to the compound by formula (IV) expression.
This reaction can be carried out under the existence of phase-transfer catalyst (for example quaternary ammonium salt, such as Tetrabutyl amonium bromide, benzyl triethyl ammonium bromide etc.) as required.
May be used in the present reaction inert solvent that does not significantly inhibit the present reaction may be any solvent include, for example: alcohols, such as methanol, ethanol, propanol, butanol, 2 - propanol and the like; chain or cyclic ethers, such as diethyl ether, tetrahydrofuran, two
Figure 943410DEST_PATH_IMAGE005
alkyl, etc.; aromatic hydrocarbons, such as benzene, toluene, xylene and the like; halogenated hydrocarbons, such as dichloromethane, chloroform, carbon tetrachloride and the like; halogenated aromatic hydrocarbons, such as chlorine benzene, chlorobenzene and the like; nitriles, such as acetonitrile and the like; esters such as ethyl acetate, etc.; polar solvent such as N, N-dimethylformamide, N, N-dimethylacetamide, dimethyl sulfoxide sulfone, 1,3 - dimethyl-2 - imidazolidinone, and water.These inert solvents can use or mix two kinds or more kinds of use separately.
Temperature of reaction in this reaction can be the boiling point from 20 ℃ to solvent for use usually.Reaction times can suitably be selected several minutes to 48 hours scope according to changes such as reaction scale, temperature of reaction.
Compound by formula (IV) expression uses in the scope that is generally about 0.8 to 5 times of mole with respect to the pyrimidine compound by formula (III) expression.
This reaction is preferably carried out under the atmosphere of inert gases of for example nitrogen and argon gas and so on.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and come the manufacturing objective thing through the purifying that utilizes recrystallization, column chromatography etc. as required.
From formula (II) to formula (I-A)
Make the pyrimidine derivatives of representing by formula (II) in the presence of catalyzer and alkali, in inert solvent, carry out catalytic hydrogenation and prepare pyrimidine derivatives of the present invention by formula (I-A) expression with hydrogen.
The instance of the catalyzer that can in this reaction, use comprises: palladium-carbon, platinum, draw Buddhist nun's nickel etc.The usage quantity of catalyzer is about 0.0001 to 0.1 times of mole with respect to the compound by formula (II) expression.
The instance of the alkali that can use in the present invention comprises: mineral alkali, such as sodium hydroxide, potassium hydroxide, yellow soda ash, salt of wormwood, cesium carbonate, sodium hydrogencarbonate, saleratus etc.; Organic salt is such as sodium acetate, potassium acetate etc.The usage quantity of alkali is generally about 0.5 to 10 times of mole with respect to the compound by formula (II) expression.
May be used in the present reaction inert solvents include: alcohols, such as methanol, ethanol and the like; ethers such as tetrahydrofuran, diethyl alkyl, etc.; water.These inert solvents can use or mix two kinds or more kinds of use separately.
Temperature of reaction in this reaction can be the boiling point from 0 ℃ to solvent for use usually.Reaction times can suitably be selected in several minutes to 48 hours then according to changes such as reaction scale, temperature of reaction.
Hydrogen-pressure can suitably be selected in normal pressure to 10 atm.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.
From formula (I-A) to (I-B)
This reaction can pass through Greene ' s Protective Groups in Organic Synthesis the 4th edition (John Wiley & Sons, Inc.) or new experimental chemistry lecture 14 volumes (the synthetic and reaction I of organic compound, Maruzen) in record method or carry out based on this method.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.In addition, can not separate target compound after reaction finishes yet and supply in next reaction.
From formula (I-B) to formula (I)
This reaction can be passed through the method for record among Greene ' s Protective Groups in Organic Synthesis the 4th edition (John Wiley & Sons, Inc.) or the 4th edition vol. 20 of experimental chemistry lecture (organic synthesis II, Japanization association compiles) or carry out based on this method.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.
As by formula (II) and (IV) expression starting compound, can directly use commercially available article.Perhaps, can prepare through the method put down in writing in the known document (for example experimental chemistry lecture, the 4th edition, vol. 24, Japanization association are compiled) or based on this method by the compound of formula (IV) expression.
The preparation method 2
R wherein 2, X and n such as above-mentioned definition; L 1Be halogen atom, such as chlorine atom, bromine atoms, iodine atom etc.
The 5-methoxy pyrimidine compound by formula (I-A) expression to making among the preparation method 1 carries out nitration reaction; So that the nitro-derivative by formula (I-C) expression to be provided; Make this derivative under separation or unseparated situation, carry out catalytic hydrogenation so that the derivative by formula (I-D) expression to be provided; And make this derivative under separation or unseparated situation, carry out sandmeyer reaction (Sandmeyer reaction), thereby make pyrimidine derivatives by formula (I-E) expression.
From formula (I-A) to formula (I-C)
This reaction can (reaction of organic compound and synthetic I, Maruzen) method of middle record be perhaps carried out based on this method through new experimental chemistry lecture 14 volumes.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.In addition, can not separate target compound after reaction finishes yet and supply in next reaction.
From formula (I-C) to formula (I-D)
This reaction can be through carrying out in the above-mentioned catalytic hydrogenation of putting down in writing from formula (II) to the operation of formula (I-A) or based on this method.
Perhaps, its can through new experimental chemistry lecture 14 volumes (oxidation and reduction II, Maruzen) in record method or carry out based on this method.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.In addition, can not separate target compound after reaction finishes yet and supply in next reaction.
From formula (I-D) to formula (I-E)
This reaction can (reaction of organic compound and synthetic I, Maruzen) method of middle record be perhaps carried out based on this method through new experimental chemistry lecture 14 volumes.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.In addition, can not separate target compound after reaction finishes yet and supply in next reaction.
In the pyrimidine derivatives by formula (I) expression, A is-S-,-SO-or-SO 2-compound can make through following preparation method.
The preparation method 3
R wherein 1, R 2, X and n such as above-mentioned definition; Q is C 1-C 6Alkyl; L 1Be leavings group, such as chlorine atom, bromine atoms and iodine atom etc.; M is hydrogen atom or basic metal, such as sodium atom, potassium atom etc.; And p is 1 or 2.
Acetyl compound and the halogenating agent represented by formula V are reacted so that the derivative by formula (VI) expression to be provided; Make this derivative under separation or unseparated situation; In the existence of alkali or not; With sulfhydryl compound reaction by formula (X) expression; So that the derivative by formula (VII) expression to be provided; Make this derivative react the derivative of representing by formula (VIII) to provide with the compound of representing by formula (XI) in the inert solvent existence or or not separation or the unseparated situation; Make this derivative separate or unseparated situation under with compound cyclisation by formula (XII) expression, thereby can obtain the pyrimidine derivatives by formula (I-F) expression of the present invention.And then with this compound oxidation so that the pyrimidine derivatives by formula (I-G) expression to be provided.
From the formula V to the formula (VI)
The inert solvent that can in this reaction, use only otherwise significantly suppressing this reaction then can be solvent arbitrarily for example can be enumerated: alcohol, such as methyl alcohol, ethanol etc.; Aromatic hydrocarbon is such as benzene, chlorobenzene etc.; Halohydrocarbon is such as methylene dichloride, chloroform, tetracol phenixin etc.; Nitrile is such as acetonitrile, propionitrile etc.; Organic acid is such as acetate etc.These inert solvents can use or mix two kinds or more kinds of use separately.
The instance of halogenating agent comprises: chlorine, bromine, iodine, SULPHURYL CHLORIDE.Its usage quantity can suitably be selected in the scope that with respect to the compound of being represented by formula V is 0.8 to 5 times of mole
Temperature of reaction can suitably be selected in the scope of the boiling point from 0 ℃ to used reaction solvent usually.Reaction times can suitably be selected in several minutes to 48 hours according to changes such as reaction scale, temperature of reaction.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.In addition, can not separate target compound after reaction finishes yet and supply in next reaction.
From formula (VI) to formula (VII)
May be used in the present reaction inert solvent that does not significantly inhibit the present reaction may be any solvent include, for example: alcohols, such as methanol, ethanol, etc.; chain or cyclic ethers, such as diethyl ether, tetrahydrofuran,
Figure 734331DEST_PATH_IMAGE005
alkyl, etc. ; ketones, such as acetone, methyl ethyl ketone and the like; aromatic hydrocarbons, such as benzene, chlorobenzene and the like; halogenated hydrocarbons, such as dichloromethane, chloroform, carbon tetrachloride and the like; nitriles, such as acetonitrile, propionitrile and the like; amides, such as dimethylformamide, dimethylacetamide, N-methylpyrrolidone, etc.; dimethyl sulfoxide, sulfolane and the like.These inert solvents can use or mix two kinds or more kinds of use separately.
The instance of the alkali that can use in the present invention comprises: mineral alkali, such as sodium hydroxide, potassium hydroxide, yellow soda ash, salt of wormwood, cesium carbonate, sodium hydrogencarbonate, saleratus etc.; Organic salt is such as sodium acetate, potassium acetate etc.The usage quantity of alkali is generally about 1.0 to 10 times of moles with respect to the sulfhydryl compound by formula (X) expression.
Usage quantity by the sulfhydryl compound of formula (X) expression is generally about 0.5 to 10 times of mole with respect to the derivative by formula (VI) expression.
Temperature of reaction can suitably selected to the boiling point that reacts solvent for use from 0 ℃ usually.Reaction times can suitably be selected in several minutes to 48 hours according to changes such as reaction scale, temperature of reaction.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.In addition, can not separate target compound after reaction finishes yet and supply in next reaction.
From formula (VII) to formula (VIII)
May be used in the present reaction inert solvent that does not significantly inhibit the present reaction may be any solvent include, for example: alcohols, such as methanol, ethanol, etc.; chain or cyclic ethers, such as diethyl ether, tetrahydrofuran,
Figure 958639DEST_PATH_IMAGE005
alkyl, etc. ; ketones, such as acetone, methyl ethyl ketone and the like; aromatic hydrocarbons, such as benzene, chlorobenzene and the like; halogenated hydrocarbons, such as dichloromethane, chloroform, carbon tetrachloride and the like; nitriles, such as acetonitrile, propionitrile and the like; amides, such as dimethylformamide, dimethylacetamide, N-methylpyrrolidone, etc.; dimethyl sulfoxide, sulfolane and the like.These inert solvents can use or mix two kinds or more kinds of use separately.Can also not use solvent, and use excessive acetyl compound to react by formula (XI) expression.Its usage quantity is generally about 1.0-to 10 times of mole with respect to the compound by formula (VII) expression.
Temperature of reaction can suitably selected to the boiling point that reacts solvent for use from 0 ℃ usually.Reaction times can suitably be selected in several minutes to 48 hours according to changes such as reaction scale, temperature of reaction.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.In addition, can not separate target compound after reaction finishes yet and supply in next reaction.
From formula (VIII) to formula (I-F)
May be used in the present reaction inert solvent that does not significantly inhibit the present reaction may be any solvent include, for example: alcohols, such as methanol, ethanol, etc.; chain or cyclic ethers, such as diethyl ether, tetrahydrofuran,
Figure 472666DEST_PATH_IMAGE005
alkyl, etc. ; ketones, such as acetone, methyl ethyl ketone and the like; aromatic hydrocarbons, such as benzene, chlorobenzene and the like; halogenated hydrocarbons, such as dichloromethane, chloroform, carbon tetrachloride and the like; nitriles, such as acetonitrile, propionitrile and the like; amides, such as dimethylformamide, dimethylacetamide, N-methylpyrrolidone, etc.; dimethyl sulfoxide, sulfolane and the like.These inert solvents can use or mix two kinds or more kinds of use separately.
The instance of the alkali that can use in the present invention comprises: mineral alkali, such as sodium hydroxide, potassium hydroxide, yellow soda ash, salt of wormwood, cesium carbonate, sodium hydrogencarbonate, saleratus etc.; Organic salt is such as sodium acetate, potassium acetate etc.The usage quantity of alkali is generally about 1.0 to 10 times of moles with respect to the amidine compound by formula (XII) expression.
Usage quantity by the amidine compound of formula (XII) expression is generally about 1.0 to 10 times of moles with respect to the derivative by formula (VIII) expression.
Temperature of reaction can suitably selected to the boiling point that reacts solvent for use from 0 ℃ usually.Reaction times can suitably be selected in several minutes to 48 hours according to changes such as reaction scale, temperature of reaction.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.In addition, can not separate target compound after reaction finishes yet and supply in next reaction.
From formula (I-F) to formula (I-G)
The inert solvent that can in this reaction, use only otherwise significantly suppressing this reaction then can be solvent arbitrarily for example can be enumerated: ester, such as ethyl acetate etc.; Ketone is such as acetone, methyl ethyl ketone etc.; Aromatic hydrocarbon is such as benzene, chlorobenzene etc.; Halohydrocarbon is such as methylene dichloride, chloroform, tetracol phenixin etc.; Nitrile is such as acetonitrile, propionitrile etc.; Organic acid is such as acetate etc.; Acid amides is such as dimethyl formamide, N,N-DIMETHYLACETAMIDE, N-Methyl pyrrolidone etc.; Water etc.These inert solvents can use or mix two kinds or more kinds of use separately.
The instance of the oxygenant that can in this reaction, use comprises: peracid, such as hydrogen peroxide, peroxyformic acid, peracetic acid, metachloroperbenzoic acid etc.; And hypochlorite, such as clorox etc.The usage quantity of oxygenant is generally about 1.0 to 10 times of moles with respect to the derivative by formula (I-F) expression.Temperature of reaction can suitably selected to the boiling point that reacts solvent for use from 0 ℃ usually.Reaction times can suitably be selected in several minutes to 48 hours according to changes such as reaction scale, temperature of reaction.
After reaction finishes, can be through ordinary method separate targets thing from the reaction system that contains target compound, and as required through coming the manufacturing objective thing with purifying such as recrystallization, distillation method, column chromatographies.
The preparation method 4
Figure 757017DEST_PATH_IMAGE010
R wherein 1, R 2, XI, XII and n such as above-mentioned definition; Q is C 1-C 6Alkyl; And p is 1 or 2.
To make with preparation method 3 method by the derivative of formula (VII) expression at first oxidation so that the derivative by formula (VII-A) expression to be provided; This derivative is reacted in the existence of inert solvent or not so that the derivative by formula (VIII-A) expression to be provided with the compound of being represented by formula (XI) under separation or unseparated situation; And the compound cyclisation that this derivative is represented with formula (XII), thereby can obtain the pyrimidine derivatives by formula (I-G) expression of the present invention under separation or unseparated situation.
From formula (VII) to formula (VII-A)
This reaction can be carried out through the preparation method from formula (I-F) to formula (I-G) of record in above-mentioned preparation method 3 or based on this method.
From formula (VII-A) to formula (VIII-A)
This reaction can be carried out through the preparation method from formula (VII) to formula (VIII) of record in above-mentioned preparation method 3 or based on this method.
From formula (VIII-A) to formula (I-G)
This reaction can be carried out through the preparation method from formula (VIII) to formula (I-F) of record in above-mentioned preparation method 3 or based on this method.
The typical example of the derivative by formula (I) expression of the present invention is shown in table 1 to 4, but the present invention is not limited to this.In the table, " Me " be methyl, " Et " be ethyl, " Pr " be propyl group, " Bu " be butyl, " Pen " be amyl group, " Hex " and be hexyl, " Bn " be benzyl, " Ph " be phenyl, " n-" be just, " i-" be different, " s-" be secondary, " t-" be uncle, " c-" be alicyclic hydrocarbon radical, " Py " be that pyridyl and " Ts " they are p-toluenesulfonyls.
When recording " 1-oxide compound " in the physics value hurdle, its 1-position that is meant pyrimidine ring is oxidized, and promptly m is 1 in the formula (I).
" the position of substitution " is meant the position of substitution in each structural formula, rerum natura represent fusing point (℃) or refractive index n D(measure temperature; ℃).
[table 1-1]
Table 1 (X=CH)
Compound N o. R 2 A-R 1 Physics value
1-1 4-t-Bu OH 104-106
1-2 3-Cl-4-t-Bu OH 155-163
1-3 4-n-Pr OMe 1.5141(26.3)
1-4 4-i-Pr OMe 1.5821(25.5)
1-5 4-c-Hex OMe 74-76
1-6 4-F OMe 56-57
1-7 3,5-F 2 OMe 88-89
1-8 4-CF 3 OMe 1.5224(24.0)
1-9 3-CF 3 OMe 53-54
1-10 3-SiMe 3 OMe 1.5653(23.3)
1-11 4-Ph OMe 133-134
1-12 4-O-n-Pr OMe ?
1-13 4-OPh OMe 50-51
1-14 3,4-OCF 2O- OMe 1.5489(27.0)
1-15 3,4-OCF 2CF 2O- OMe 61-62
1-16 4-COMe OMe 101-102
1-17 4-CO 2Me OMe 127-128
1-18 4-CONHMe OMe 146-154
1-19 4-CONMe 2 OMe 99-100
1-20 4-CN OMe 112-113
1-21 4-NH 2 OMe 1.6217(27.0)
1-22 4-NHCOMe OMe 140-142
1-23 4-NHSO 2Me OMe 187-189
1-24 4-NO 2 OMe 135-136
1-25 4-CH 2-c-Pr OMe 1.5898(25.5)
1-26 4-CH 2SiMe 3 OMe 1.5733(26.5)
1-27 4-CH 2-t-Bu OMe 1.5643(26.3)
[table 1-2]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-28 3-F-4-CH 2-t-Bu OMe ?
1-29 3-Cl-4-CH 2-t-Bu OMe 41-43
1-30 3-Br-4-CH 2-t-Bu OMe 44-46
1-31 2,5-Br 2-4-CH 2-t-Bu OMe 1.5921(24.6)
1-32 3-I-4-CH 2-t-Bu OMe ?
1-33 3-NH 2-4-CH 2-t-Bu OMe 1.5778(26.1)
1-34 3-NO 2-4-CH 2-t-Bu OMe 1.5549(26.1)
1-35 2-Cl-4-CH 2-t-Bu OMe ?
1-36 4-i-Bu OMe 1.5783(26.5)
1-37 3-F-4-i-Bu OMe ?
1-38 3-Cl-4-i-Bu OMe 1.5857(27.5)
1-39 3-Br-4-i-Bu OMe ?
1-40 3-I-4-i-Bu OMe ?
1-41 3-NH 2-4-i-Bu OMe 1.6112(27.5)
1-42 3-NO 2-4-i-Bu OMe 1.5892(27.5)
1-43 2-Cl-4-i-Bu OMe ?
1-44 4-OCF 3 OMe 1.5306(27.0)
1-45 3-Cl-4-OCF 3 OMe ?
1-46 4-OCHMe-i-Pr OMe 1.5663(26.5)
1-47 4-O-i-Pr OMe 1.5804(29.0)
1-48 3-F-4-O-i-Pr OMe 36-38
1-49 3-Cl-4-O-i-Pr OMe 1.6056(26.3)
1-50 4-SiMe 3 OMe 1.5731(29.0)
1-51 3-Cl-4-SiMe 3 OMe 101-103
1-52 4-S-i-Pr OMe 1.6277(25.8)
1-53 4-t-Bu OMe 1.5689(26.6)
1-54 3-F-4-t-Bu OMe ?
1-55 3-Cl-4-t-Bu OMe 1.5930(27.3)
1-56 3-Br-4-t-Bu OMe ?
1-57 3-I-4-t-Bu OMe ?
1-58 2-Cl-4-t-Bu OMe 1.5818(27.2)
[table 1-3]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-59 2-Br-4-t-Bu OMe 1.5900(26.9)
1-60 2,5-Cl 2-4-t-Bu OMe 1.5291(27.3)
1-61 2,5-Br 2-4-t-Bu OMe 113-114
1-62 4-(2-i-PrOPhOCH 2) OMe 1.5952(26.0)
1-63 (1,3-two for 4-
Figure 869646DEST_PATH_IMAGE005
Alkane-2-yl)
OMe 100-101
1-64 4-CH 2-t-Bu OEt 1.5612(22.5)
1-65 3-Cl-4-CH 2-t-Bu OEt ?
1-66 4-i-Bu OEt 1.5572(22.5)
1-67 3-Cl-4-i-Bu OEt ?
1-68 4-OCF 3 OEt ?
1-69 3-Cl-4-OCF 3 OEt ?
1-70 4-O-i-Pr OEt 1.5781(24.0)
1-71 3-Cl-4-O-i-Pr OEt ?
1-72 4-SiMe 3 OEt 1.5558(23.5)
1-73 3-Cl-4-SiMe 3 OEt ?
1-74 4-t-Bu OEt 1.5607(24.5)
1-75 3-Cl-4-t-Bu OEt ?
1-76 4-CH 2-t-Bu O-n-Pr 1.5556(22.5)
1-77 3-Cl-4-CH 2-t-Bu O-n-Pr 1.5658(22.3)
1-78 4-i-Bu O-n-Pr 1.5527(22.5)
1-79 3-Cl-4-i-Bu O-n-Pr 1.5672(24.5)
1-80 4-OCF 3 O-n-Pr 1.5140(24.7)
1-81 3-Cl-4-OCF 3 O-n-Pr ?
1-82 4-O-i-Pr O-n-Pr 1.5745(24.0)
1-83 3-Cl-4-O-i-Pr O-n-Pr ?
1-84 4-SiMe 3 O-n-Pr 1.5458(23.5)
1-85 3-Cl-4-SiMe 3 O-n-Pr ?
1-86 4-t-Bu O-n-Pr 1.5618(25.5)
1-87 3-Cl-4-t-Bu O-n-Pr ?
1-88 4-CH 2-t-Bu O-i-Pr ?
1-89 3-Cl-4-CH 2-t-Bu O-i-Pr ?
[table 1-4]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-90 4-i-Bu O-i-Pr ?
1-91 3-Cl-4-i-Bu O-i-Pr ?
1-92 4-OCF 3 O-i-Pr ?
1-93 3-Cl-4-OCF 3 O-i-Pr ?
1-94 4-O-i-Pr O-i-Pr ?
1-95 3-Cl-4-O-i-Pr O-i-Pr ?
1-96 4-SiMe 3 O-i-Pr ?
1-97 3-Cl-4-SiMe 3 O-i-Pr ?
1-98 4-t-Bu O-i-Pr 1.5511(25.5)
1-99 3-Cl-4-t-Bu O-i-Pr ?
1-100 4-CH 2-t-Bu O-n-Bu ?
1-101 3-Cl-4-CH 2-t-Bu O-n-Bu ?
1-102 4-i-Bu O-n-Bu ?
1-103 3-Cl-4-i-Bu O-n-Bu ?
1-104 4-OCF 3 O-n-Bu ?
1-105 3-Cl-4-OCF 3 O-n-Bu ?
1-106 4-O-i-Pr O-n-Bu 1.5684(24.0)
1-107 3-Cl-4-O-i-Pr O-n-Bu ?
1-108 4-SiMe 3 O-n-Bu 1.5501(24.0)
1-109 3-Cl-4-SiMe 3 O-n-Bu ?
1-110 4-t-Bu O-n-Bu 1.5537(27.0)
1-111 3-Cl-4-t-Bu O-n-Bu ?
1-112 4-CH 2-t-Bu O-i-Bu ?
1-113 3-Cl-4-CH 2-t-Bu O-i-Bu ?
1-114 4-i-Bu O-i-Bu ?
1-115 3-Cl-4-i-Bu O-i-Bu ?
1-116 4-OCF 3 O-i-Bu ?
1-117 3-Cl-4-OCF 3 O-i-Bu ?
1-118 4-O-i-Pr O-i-Bu ?
1-119 3-Cl-4-O-i-Pr O-i-Bu ?
1-120 4-SiMe 3 O-i-Bu ?
1-121 3-Cl-4-SiMe 3 O-i-Bu ?
[table 1-5]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-122 4-t-Bu O-i-Bu 43-44
1-123 3-Cl-4-t-Bu O-i-Bu ?
1-124 4-CH 2-t-Bu O-s-Bu ?
1-125 3-Cl-4-CH 2-t-Bu O-s-Bu ?
1-126 4-i-Bu O-s-Bu ?
1-127 3-Cl-4-i-Bu O-s-Bu ?
1-128 4-OCF 3 O-s-Bu ?
1-129 3-Cl-4-OCF 3 O-s-Bu ?
1-130 4-O-i-Pr O-s-Bu ?
1-131 3-Cl-4-O-i-Pr O-s-Bu ?
1-132 4-SiMe 3 O-s-Bu ?
1-133 3-Cl-4-SiMe 3 O-s-Bu ?
1-134 4-t-Bu O-s-Bu 1.5539(25.5)
1-135 3-Cl-4-t-Bu O-s-Bu ?
1-136 4-CH 2-t-Bu O-3-Pen ?
1-137 3-Cl-4-CH 2-t-Bu O-3-Pen ?
1-138 4-i-Bu O-3-Pen ?
1-139 3-Cl-4-i-Bu O-3-Pen ?
1-140 4-OCF 3 O-3-Pen ?
1-141 3-Cl-4-OCF 3 O-3-Pen ?
1-142 4-O-i-Pr O-3-Pen ?
1-143 3-Cl-4-O-i-Pr O-3-Pen ?
1-144 4-SiMe 3 O-3-Pen ?
1-145 4-SiMe 3 O-3-Pen ?
1-146 4-t-Bu O-3-Pen 60-64
1-147 3-Cl-4-t-Bu O-3-Pen ?
1-148 4-t-Bu O-n-Pen 1.5321(27.0)
1-149 4-t-Bu OCH 2OMe 1.5696(25.5)
1-150 4-t-Bu OCH 2CH 2OMe 1.5660(24.5)
1-151 4-t-Bu OCH 2CH 2SMe 1.5685(24.5)
1-152 4-t-Bu OCH 2CH 2SOMe 72-74
[table 1-6]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-153 4-t-Bu OCH 2CH 2SO 2Me 122-124
1-154 4-t-Bu OCH 2CH 2NMe 2 ?
1-155 4-t-Bu OCH 2CH 2NO 2 124-126
1-156 4-t-Bu OCH 2CH 2Cl 165-166
1-157 4-t-Bu OCH 2Ph 1.5906(25.5)
1-158 4-t-Bu OCH 2C≡CH 1.5547(27.0)
1-159 4-t-Bu OCH 2CN 82-84
1-160 4-t-Bu OCH 2CH 2CN 172-174
1-161 4-t-Bu OCH 2CH=CH 2 1.5732(24.5)
1-162 4-t-Bu OCH 2CF 3 74-76
1-163 4-CH 2-t-Bu OCH 2OMe ?
1-164 4-CH 2-t-Bu OCH 2CH 2OMe ?
1-165 4-CH 2-t-Bu OCH 2CH 2SMe ?
1-166 4-CH 2-t-Bu OCH 2CH 2SOMe ?
1-167 4-CH 2-t-Bu OCH 2CH 2SO 2Me ?
1-168 4-CH 2-t-Bu OCH 2CH 2NMe 2 ?
1-169 4-CH 2-t-Bu OCH 2CH 2NO 2 ?
1-170 4-CH 2-t-Bu OCH 2CH 2Cl ?
1-171 4-CH 2-t-Bu OCH 2Ph ?
1-172 4-CH 2-t-Bu OCH 2C≡CH ?
1-173 4-CH 2-t-Bu OCH 2CN ?
1-174 4-CH 2-t-Bu OCH 2CH 2CN ?
1-175 4-CH 2-t-Bu OCH 2CH=CH 2 ?
1-176 4-CH 2-t-Bu OCH 2CF 3 ?
1-177 4-t-Bu OPh 1.5592(23.0)
1-178 4-t-Bu OCH 2-c-Pr 1.5550(24.5)
1-179 4-t-Bu OCHMe-c-Pr 1.5558(21.5)
1-180 4-(3,3-Me 2-oxyethane-2-yl) OMe 1.5759(21.5)
1-181 4-i-Bu OCH 2OMe 1.5505(24.5)
[table 1-7]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-182 4-t-Bu OCH 2CO 2Me 1.5474(24.5)
1-183 4-t-Bu OCOMe 1.5643(24.5)
1-184 4-O-c-Pen OMe 43-45
1-185 4-i-Bu OH 142-143
1-186 4-t-Bu OCH 2CH 2F 1.5622(22.5)
1-187 4-i-Bu OCH 2CH 2Cl 1.5689(22.5)
1-188 4-t-Bu OCH 2CMe=CH 2 1.5585(22.5)
1-189 4-t-Bu OTs 1.5677(23.5)
1-190 4-t-Bu OCO 2Me 1.5419(23.5)
1-191 4-t-Bu OCH 2CH 2C≡CH 1.5760(23.5)
1-192 4-t-Bu OCOPh 1.5792(23.5)
1-193 3-NO 2-4-i-Bu O-n-Pr 1.5663(25.0)
1-194 4-i-Bu O(4-ClPh) 1.5650(25.0)
1-195 3-NH 2-4-i-Bu O-n-Pr 68-69
1-196 4-i-Bu OPh 1.5921(24.5)
1-197 4-i-Bu O(2-ClPh) 1.5696(24.5)
1-198 4-i-Bu O(4-MeOPh) 1.4578(24.5)
1-199 4-CHMeEt OH 1.4681(24.5)
1-200 4-CHMeEt OMe 1.5600(24.5)
1-201 4-CHMeEt O-n-Pr 1.4965(24.5)
1-202 4-CHMeEt OCH 2OMe 1.5280(24.5)
1-203 4-OCH 2OMe OMe 1.5875(24.5)
1-204 4-OH OMe 189-190
1-205 4-CMe 2Et O-n-Pr 1.5503(23.5)
1-206 4-t-Bu OCHMe-n-Pr 1.5156(23.5)
1-207 4-t-Bu OCH 2CH=CHMe 1.5518(23.5)
1-208 4-t-Bu OCONMe 2 1.5578(23.5)
1-209 4-(2-pyrazinyl oxygen base) OMe 119-121
[table 1-8]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-210 4-(3-CF 3-pyrazine-2-base oxygen base) OMe 114-115
1-211 4-t-Bu OCH 2OEt 45-56
1-212 4-t-Bu OCH 2SMe 68-69
1-213 3,4-(CH 2) 4 OCH 2OMe 1.5831(20.0)
1-214 4-CHMe-i-Pr OH 134-135
1-215 4-CHMe-i-Pr OCH 2OMe 1.5432(22.0)
1-216 4-CHMe-i-Pr OMe 1.5749(22.0)
1-217 4-CHMe-i-Pr O-n-Pr 1.5403(22.0)
1-218 4-i-Bu O(3-ClPh) 1.5566(22.0)
1-219 4-i-Bu O(3-Py) 1.5340(24.5)
1-220 4-SiMe 3 OH 101-102
1-221 4-t-Bu 2-pyrimidyl oxygen base 68-69
1-222 4-t-Bu O(2-Py) 67-68
1-223 4-t-Bu 3-CF 3-pyrazine-2-base oxygen base 121-122
1-224 3,4-(CH 2) 4 O-n-Pr 1.5916(21.8)
1-225 3,4-(CH) 4 OMe 95-96
1-226 4-c-Pen OCH 2OMe 1.5709(24.6)
1-227 4-CHMe-i-Pr OEt 1.5689(23.5)
1-228 4-i-Bu O(4-CF 3Ph) 1.5561(23.5)
1-229 4-O-i-Pr OCH 2OMe 1.5757(24.0)
1-230 4-SiMe 3 OCH 2OMe 1.5651(24.0)
1-231 4-c-Pen O-n-Pr 27-28
1-232 4-OPh O-n-Pr 1.6194(22.8)
1-233 4-OPh OCH 2OMe 1.6200(22.8)
1-234 4-CMe 2Et OMe 1.5821(25.0)
1-235 4-CMe 2Et OCH 2OMe 1.5549(25.0)
1-236 4-i-Bu Different Azoles-3-base oxygen base 1.5793(25.0)
1-237 4-SiMe 3 OSiMe 2-t-Bu 69-70
[table 1-9]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-238 4-(3-Cl-pyrazine-2-base oxygen base) OMe 151-153
1-239 4-(3-CF 3Ph) OMe 114-116
1-240 4-(3-ClPh) OMe 103-104
1-241 4-(2-CF 3Ph) OMe 114-115
1-242 4-(3-MeS-pyrazine-2-base oxygen base) OMe 181-182
1-243 4-OCF 3 OH 154-157
1-244 4-OCF 3 OCH 2OMe 1.5189(25.5)
1-245 4-OCF 3 OCH 2SMe 35-36
1-246 4-OCF 3 OCH 2OEt 1.5162(24.7)
1-247 4-SiMe 3 OCH 2OEt 1.5531(24.0)
1-248 4-OSiMe 3 OMe 76-77
1-249 3,4-C(Me) 2CH 2CH 2C(Me) 2- OCH 2OMe 1.5271(19.6)
1-250 4-c-Pen OEt 1.5877(20.0)
1-251 4-(2-ClPh) OMe 165-166
1-252 4-O(2-CF 3Ph) OMe 1.5915(25.5)
1-253 4-(2-CF 3Ph) O-n-Bu 1.5648(25.5)
1-254 4-(2-CF 3Ph) O-n-Pr 1.5689(25.5)
1-255 4-O(2-CF 3Ph) O-n-Pr 1.5759(22.9)
1-256 4-O(2-CF 3Ph) OEt 1.5799(22.9)
1-257 3,4-C(Me) 2CH 2CH 2C(Me) 2- O-n-Pr 1.5499(21.2)
1-258 4-SiMe 2Et OMe 1.5732(23.7)
1-259 4-SiMe 3 OCH 2C≡CH 1.5524(23.2)
1-260 4-SiMe 3 OCH 2SMe 1.5782(23.2)
1-261 4-SiMe 2Et O-n-Pr 1.5573(22.5)
1-262 4-SiMe 2Et OCH 2OMe 1.5611(23.1)
1-263 4-SiMe 2Et OH 108-110
1-264 4-(3-MeO-pyrazine-2-base oxygen base) OMe 125-127
1-265 4-OSiMe 2-t-Bu OMe 68-70
1-266 4-CMe 2Et OEt 30-31
[table 1-10]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-267 4-CMe 2CH 2Cl OMe 44-45
1-268 4-SiMe 2-t-Bu OMe 94-96
1-269 4-SiEt 3 OMe 1.5757(22.3)
1-270 4-SiEt 3 OCH 2OMe 1.5539(22.5)
1-271 4-SiEt 3 OH 133-135
1-272 4-SiMe 3 OCH 2O-n-Pr 1.5468(22.2)
1-273 4-SiMe 3 OCH 2O-i-Pr 1.5460(22.0)
1-274 4-SiMe 3 OCH 2OCH 2CH 2OMe 1.5380(22.0)
1-275 4-SiMe 3 OCH 2OCO 2Me 1.5545(23.5)
1-276 4-t-Bu OCH 2OCO 2Et 1.5334(23.5)
1-277 4-CMe 2Et OCH 2OEt 1.5589(21.5)
1-278 3,4-OCF 2CF 2O- O-n-Pr 29-30
1-279 4-OCF 3 OPh 1.5611(21.5)
1-280 4-(2,2-Cl 2-c-Pr) OMe 1.5609(20.6)
1-281 4-SiEt 3 O-n-Pr 1.5610(20.4)
1-282 4-SiMe 2-t-Bu OCH 2OMe 58-60
1-283 4-SiMe 2-t-Bu OH 144-148
1-284 4-(3-ethynyl pyrazine-2-base oxygen base) OMe 164-166
1-285 4-(3-ethyl pyrazine-2-base oxygen base) OMe 102-103
1-286 4-CMe 2CH 2Cl OEt 49-50
1-287 4-t-Bu OCH 2OCONMe 2 1.5602(20.8)
1-288 4-SiMe 3 OCH 2CH 2Ph 1.5638(20.8)
1-289 4-SiMe 2-t-Bu O-n-Pr 57-59
1-290 4-SiMe 2-i-Pr OMe 1.5495(22.5)
1-291 4-SiMe 2-n-Pr OMe 1.5677(23.0)
1-292 4-CMe 2CH 2Cl O-n-Pr 45-46
1-293 4-O-t-Bu OMe 1.5828(22.1)
1-294 4-SiMe 3 OCH 2C≡CMe 1.5703(22.8)
1-295 4-O-i-Pr OCH 2SMe 1.6035(23.2)
[table 1-11]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-296 4-OCMe 2-i-Pr OMe 1.5675(22.1)
1-297 4-SiMe 2-i-Pr O-n-Pr 1.5596(22.0)
1-298 4-SiMe 2-i-Pr OCH 2OMe 1.5585(22.0)
1-299 4-SiMe 2-n-Pr OEt 1.5569(22.0)
1-300 4-SiMe 2-n-Pr O-n-Pr 1.5533(22.0)
1-301 4-O-i-Pr OPh 1.6078(22.0)
1-302 4-OCF 3 OCH 2SOMe 100-101
1-303 4-OCF 3 OCH 2SO 2Me 119-120
1-304 4-SiMe 3 OCH 2O-i-Bu 1.5460(22.5)
1-305 4-SiMe 3 OCH 2O-n-Bu 1.5413(22.7)
1-306 4-CF(CF 3) 2 O-n-Pr 35-36
1-307 4-SiMe 3 OCH 2CH 2(2-Py) 1.5871(22.7)
1-308 4-SiMe 2-t-Bu OCH 2OEt 35-36
1-309 4-SiMe 2-n-Pr OCH 2C≡CH 1.5672(24.5)
1-310 4-SiMe 2-n-Pr OCH 2OMe 1.5523(24.5)
1-311 4-CMe 2CH 2Cl OCH 2OMe 63-64
1-312 4-OCMe 2-i-Pr OCH 2OMe 1.5639(24.8)
1-313 4-O-t-Bu OCH 2OMe 1.4501(24.8)
1-314 4-O-i-Pr OCH 2SOMe 85-87
1-315 4-SiMe 3 OCH 2OCO 2Et 1.5419(24.0)
1-316 4-t-Bu OCH 2OCOPh 1.5855(23.5)
1-317 4-t-Bu OSO 2Me 1.5700(24.0)
1-318 4-OCF 3 OCH 2SPh 1.5691(24.0)
1-319 4-t-Bu OCH 2COMe 1.5661(20.5)
1-320 4-OCMe 2-i-Pr O-n-Pr 1.5618(21.5)
1-321 4-O-t-Bu O-n-Pr 1.5613(21.5)
1-322 4-OCF 3 OCH 2SOPh 72-74
1-323 4-OCF 3 OCH 2SO 2Ph 108-110
1-324 4-SiMe 3 OCH 2SOMe 1.5777(20.0)
1-325 4-i-Bu 4-PhOPhO 1.6020(22.0)
1-326 4-i-Bu 4-(2-quinolyl oxygen base) 71-72
[table 1-12]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-327 2-Me-4-OCF 3 OMe 59-60
1-328 4-SiMe 2Et OCHF 2 1.5350(20.0)
1-329 4-i-Bu O(2-MeSPh) 1.5318(21.0)
1-330 4-OCF 2CHFOCF 3 OMe 1.5420(21.0)
1-331 4-SiMe 3 OCH 2SO 2Me 102-104
1-332 4-(3-Py) OMe 146-148
1-333 4-OCH 2CH 2SiMe 3 OMe 1.5650(24.6)
1-334 4-OCH 2SiMe 3 OMe 1.5654(24.6)
1-335 3-NO 2-4-t-Bu O-n-Pr 1.5661(22.5)
1-336 2-NO 2-4-t-Bu O-n-Pr 1.5570(22.5)
1-337 4-i-Bu O(2-MeSOPh) 1.5472(22.5)
1-338 4-i-Bu O(2-MeOPh) 1.5863(22.5)
1-339 4-OCH 2SMe OMe 1.6261(21.7)
1-340 4-(5-pyrimidyl) OCH 2OMe 130-135
1-341 4-(3-NO 2-pyridine-2-base oxygen base) OMe 161-162
1-342 4-(5-CF 3-pyridine-2-base sulfenyl (thio)) OMe 1.5905(21.7)
1-343 4-i-Bu O(2-MeSO 2Ph) 76-77
1-344 3-NO 2-4-CH 2-t-Bu O-n-Pr 1.5636(22.2)
1-345 2-NO 2-4-CH 2-t-Bu O-n-Pr 1.5569(22.6)
1-346 3-NH 2-4-CH 2-t-Bu O-n-Pr 99-101
1-347 4-(3-CF 3-pyridine-2-base oxygen base) OMe 109-110
1-348 4-(5-NO 2-pyridine-2-base oxygen base) OMe 135-137
1-349 4-(6-CF 3-pyridine-2-base oxygen base) OMe 99-100
1-350 4-OCH 2SOMe OMe 96-97
1-351 4-OCH 2SO 2Me OMe 112-113
[table 1-13]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-352 4-(3-CN-pyridine-2-base oxygen base) OMe 160-161
1-353 4-(5-Br-pyridine-2-base oxygen base) OMe 103-104
1-354 4-(6-Br-pyridine-2-base oxygen base) OMe 134-135
1-355 4-(3-Br-pyridine-2-base oxygen base) OMe 116-119
1-356 4-(6-Cl-pyrazine-2-base oxygen base) OMe 129-131
1-357 4-O(2-Py) OMe 76-78
1-358 4-(3-CF 3-pyrazine-2-base oxygen base) O-n-Pr 125-126
1-359 2-Cl-4-(3-CF 3-pyrazine-2-base oxygen base) OMe 114-115
1-360 4-OCF 2CHFOCF 3 OCH 2SMe 1.5261(24.8)
1-361 4-OCF 2CHFOCF 3 OCH 2SOMe 58-59
1-362 4-OCH 2SMe O-n-Pr 1.5325(24.8)
1-363 4-OCH 2SOMe O-n-Pr 84-85
1-364 4-SiMe 2Et OCH 2CF 3 1.5339(24.6)
1-365 4-(3-CF 3-pyrazine-2-base oxygen base) OCH 2OEt 76-77
1-366 3-OCH 2OMe OMe 1.5714(24.5)
1-367 4-CO-i-Pr OMe 72-74
1-368 3-Cl-4-SiMe 2Et OMe 36-38
1-369 3-OCH 2SMe OMe 1.5430(27.5)
1-370 3-OCH 2SOMe OMe 51-52
1-371 2-OCH 2OMe OMe 1.5693(27.5)
1-372 2-Cl-4-OCF 3 OMe 52-53
1-373 3-F-4-SiMe 3 OMe 46-48
1-374 3-OCH 2SO 2Me OMe 80-81
1-375 2-OCH 2SMe OMe 1.5600(29.0)
[table 1-14]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-376 4-(2-Me-1-MeOCH 2-n-Pr-1-yl) OMe 1.5565(27.8)
1-377 4-CHF-i-Pr OMe 1.5645(28.0)
1-378 4-OCH 2F OMe 1.5862(27.0)
1-379 3-Me-4-SiMe 3 OMe 75-77
1-380 2-Me-4-SiMe 3 OMe 46-47
1-381 2-Cl-4-OCF 3 OCH 2SMe 53-55
1-382 2-OCH 2SOMe OMe 1.5471(27.5)
1-383 2-OCH 2SO 2Me OMe 1.5682(27.5)
1-384 4-SiMe 3 O-n-Pr 1.5150(27.5)
1-385 2-Cl-4-OCF 3 OCH 2SOMe 84-86
1-386 2-Cl-4-OCF 3 OCH 2SO 2Me 106-108
1-387 4-(2-Me-1-MeSCH 2The O-n-Pr-1-yl) OMe 1.5746(26.5)
1-388 4-OCH 2S-n-Pr OMe 1.6052(26.6)
1-389 4-(2-Me-1-MeSO-n-Pr-1-yl) OMe 30-31
1-390 4-SiMe 2CH 2Cl OMe 1.5717(27.5)
1-391 4-SiMe 2CH 2SMe OMe 1.5966(27.6)
1-392 4-SiMe 2OH OMe 1.5750(25.8)
1-393 3-OCF 3-4-SiMe 3 OMe 1.5689(26.0)
1-394 4-OCF 2CHFCF 3 OCH 2SMe 1.5242(26.7)
1-395 4-OCF 3 OCH 2SEt 32-34
1-396 4-SiH-i-Pr 2 OMe 1.5720(27.0)
1-397 4-SiMe 2Ph OMe 1.6090(27.0)
1-398 4-N=CMeNMe 2 OMe 1.6094(27.0)
1-399 4-OCH 2SO-n-Pr OMe 1.5273(26.5)
1-400 2-Cl-4-OCH 2OMe OMe 1.5630(27.0)
1-401 2-Cl-4-OCH 2SMe OMe 100-101
[table 1-15]
Table 1 (continuous table)
[table 1-16]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-430 4-NHCOCF 3 OMe 86-88
1-431 4-NHCOO-t-Bu OMe 172-174
1-432 4-CHMeOH OMe 1.6045(26.5)
1-433 4-OCH 2(4-ClPh) OMe 135-136
1-434 4-CHMeOPh OMe 60-63
1-435 4-COCH 2SMe OMe 100-101
1-436 4-NHCO-i-Pr OMe 139-140
1-437 4-CH 2CH 2SMe OMe 1.6077(26.5)
1-438 4-OCH 2(4-MePh) OMe 87-88
1-439 4-OCH 2CF 3 OMe 90-91
1-440 4-OCF 2CF 2H OMe 1.5843(27.0)
1-441 4-SO 2CF 2CF 3 OMe 77-78
1-442 4-CONHCH 2CF 3 OMe 161-162
1-443 4-OCF 2CHFCF 3 OCH 2SOMe 1.5171(26.8)
1-444 4-OCF 2CHFCF 3 OCH 2SO 2Me 46-48
1-445 4-OCF 2CHFOCF 3 OCH 2SO 2Me 82-84
1-446 4-(5-C 2F 5-tetrazolium-1-yl) OMe 1.5382(20.0)
1-447 4-SCH 2CF 3 OMe 1.5882(22.5)
1-448 4-SOCH 2CF 3 OMe 94-95
1-449 4-SO 2CH 2CF 3 OMe 153-154
1-450 4-(3-CF 3-pyridine-2-base sulfenyl) OMe 162-163
1-451 4-CONHPh OMe 161-162
1-452 4-(1-isoquinolyl oxygen base) OMe 124-125
1-453 4-OCHMe(2-ClPh) OMe 104-105
1-454 4-OCH 2(2-Py) OMe 75-76
1-455 4-SCH 2SiMe 3 OMe 80-81
1-456 4-SOCH 2SiMe 3 OMe 1.6000(22.7)
1-457 4-SO 2CH 2SiMe 3 OMe 51-52
[table 1-17]
Table 1 (continuous table)
Figure 596184DEST_PATH_IMAGE013
[table 1-18]
Table 1 (continuous table)
Compound N o. R 2 A-R 1 Physics value
1-483 4-OCF 3 5,6-Me 2-benzoglyoxaline-1-ylmethoxy 193-195
1-484 4-OCF 3 1,3-dioxo-isoindole-2-ylmethoxy 149-150
1-485 4-OCF 3 2,2-Cl 2-c-PrCH 2O 1.5398(25.5)
1-486 4-SCF 2CF 3 OCH 2OMe 1.5250(26.5)
1-487 4-OCHMe(2-CF 3Ph) OMe 134-135
1-488 4-(1-Ph-2-Me-Pr) oxygen base OMe 1.5647(25.0)
1-489 4-(1-(2-naphthyl)) oxyethyl group OMe 1.4421(25.0)
1-490 4-(1,2,3,4-tetralyl-1-oxygen base) OMe 1.5714(25.0)
1-491 4-OCF 3 3-tetrahydrofuran (THF) ylmethoxy 1.5272(22.5)
1-492 4-OCF 3 The oxyethane ylmethoxy 1.5352(22.5)
1-493 4-OCF 3 4-(2,2-Me 2-1, the 3-dioxolanyl) methoxyl group 1.5160(22.5)
1-494 4-OCF 2CHFOCF 3 2,2-Cl 2-c-PrCH 2O 1.5039(22.5)
1-495 4-SCF 2CF 3 OCH 2SMe 51-52
1-496 4-OCF 3 3-tetrahydrofuran base oxygen base 32-34
1-497 4-OCF 3 O-c-Pen 1.5306(21.5)
1-498 4-OCF 3 OCH 2CH 2CH 2Cl 1.5275(21.5)
1-499 4-OCHCF 3(Ph) OMe 1.4710(25.0)
1-500 4-OCHMe(2-Py) OMe 1.6940(25.0)
1-501 4-OCHMe (2-thienyl) OMe 1.4054(25.0)
[table 2-1]
Figure 162295DEST_PATH_IMAGE011
Table 2 (X=CH)
Compound N o. R 2 AR 1 Physics value
2-1 4-F SMe ?
2-2 4-Cl SMe ?
2-3 4-Br SMe ?
2-4 4-I SMe ?
2-5 3,4-Cl 2 SMe 106-107
2-6 2,4-Cl 2 SMe ?
2-7 4-CH 2-t-Bu SMe 68-70
2-8 3-Cl-4-CH 2-t-Bu SMe ?
2-9 4-i-Bu SMe 1.5189(24.5)
2-10 4-i-Bu SOMe 1.4911(23.3)
2-11 4-i-Bu SO 2Me 57-58
2-12 3-Cl-4-i-Bu SMe ?
2-13 4-OCF 3 SMe 1.5633(23.0)
2-14 3-Cl-4-OCF 3 SMe ?
2-15 4-O-i-Pr SMe 1.5398(24.5)
2-16 3-Cl-4-O-i-Pr SMe 1.5451(24.5)
2-17 4-SiMe 3 SMe 1.4850(22.5)
2-18 3-Cl-4-SiMe 3 SMe ?
2-19 4-SiMe 3 SOMe 1.5342(21.0)
2-20 4-t-Bu SMe 1.6042(27.0)
2-21 4-t-Bu SOMe 1.5331(27.0)
2-22 3-Cl-4-t-Bu SMe ?
2-23 4-CH 2-t-Bu SEt 1.5069(22.7)
2-24 3-Cl-4-CH 2-t-Bu SEt ?
2-25 4-i-Bu SEt 1.4318(24.0)
2-26 3-Cl-4-i-Bu SEt ?
[table 2-2]
Table 2 (continuous table)
Compound N o. R 2 AR 1 Physics value
2-27 4-OCF 3 SEt 1.5482(23.0)
2-28 3-Cl-4-OCF 3 SEt ?
2-29 4-O-i-Pr SEt 1.5361(24.5)
2-30 3-Cl-4-O-i-Pr SEt ?
2-31 4-SiMe 3 SEt ?
2-32 3-Cl-4-SiMe 3 SEt ?
2-33 4-t-Bu SEt 1.5809(27.0)
2-34 3-Cl-4-t-Bu SEt ?
2-35 4-CH 2-t-Bu S-n-Pr ?
2-36 3-Cl-4-CH 2-t-Bu S-n-Pr ?
2-37 4-i-Bu S-n-Pr 1.5121(23.0)
2-38 3-Cl-4-i-Bu S-n-Pr ?
2-39 4-OCF 3 S-n-Pr ?
2-40 3-Cl-4-OCF 3 S-n-Pr ?
2-41 4-O-i-Pr S-n-Pr 1.5965(24.5)
2-42 3-Cl-4-O-i-Pr S-n-Pr ?
2-43 4-SiMe 3 S-n-Pr ?
2-44 3-Cl-4-SiMe 3 S-n-Pr ?
2-45 4-t-Bu S-n-Pr 1.5809(22.5)
2-46 3-Cl-4-t-Bu S-n-Pr ?
2-47 4-CH 2-t-Bu S-i-Pr 1.5365(22.7)
2-48 3-Cl-4-CH 2-t-Bu S-i-Pr ?
2-49 4-i-Bu S-i-Pr 1.4551(27.0)
2-50 3-Cl-4-i-Bu S-i-Pr ?
2-51 4-OCF 3 S-i-Pr ?
2-52 3-Cl-4-OCF 3 S-i-Pr ?
2-53 4-O-i-Pr S-i-Pr ?
2-54 3-Cl-4-O-i-Pr S-i-Pr ?
2-55 4-SiMe 3 S-i-Pr ?
2-56 3-Cl-4-SiMe 3 S-i-Pr ?
2-57 4-t-Bu S-i-Pr 1.5814(27.0)
[table 2-3]
Table 2 (continuous table)
Compound N o. R 2 AR 1 Physics value
2-58 3-Cl-4-t-Bu S-i-Pr ?
2-59 4-n-Bu S-n-Pr 1.5988(22.5)
2-60 4-t-Bu S-n-Bu 1.5766(22.5)
2-61 4-OMe SEt 1.5520(21.5)
2-62 4-OMe S-n-Pr 1.6220(21.5)
2-63 4-i-Bu Benzothiazolyl-2-sulfenyl 1.6409(22.5)
2-64 4-CMe 2Et SMe 1.5808(23.5)
2-65 4-CMe 2Et SEt 1.5881(23.5)
2-66 4-CHMeEt SMe 1.5912(24.5)
2-67 4-CHMeEt SEt 1.6039(24.5)
2-68 4-CHMe-i-Pr SMe 1.5608(20.5)
2-69 4-CHMe-i-Pr SEt 1.5589(20.5)
2-70 3,4-(CH 2) 4 SEt 1.5569(20.0)
2-71 4-c-Pen SEt 54-55
2-72 4-i-Bu SOEt 1.5860(22.0)
2-73 4-t-Bu SO-n-Pr 76-77
2-74 4-i-Bu SPh 1.5770(21.0)
2-75 4-i-Bu SOPh 1.6018(21.0)
2-76 4-i-Bu SO 2Ph 1.5650(22.5)
2-77 i-Bu SCF 2CF 3 1.5105(26.5)
2-78 i-Bu SCH 2CF 3 1.5431(26.5)
2-79 i-Bu SOCH 2CF 3 136-137
2-80 i-Bu SCONMe 2 1.5938(21.0)
2-81 i-Bu SCH 2SMe 1.6142(24.5)
[table 3-1]
Figure 198384DEST_PATH_IMAGE014
Table 3
Figure 762221DEST_PATH_IMAGE015
[table 3-2]
Table 3 (continuous table)
Compound N o. R AR 1 Physics value
3-7
Figure 149339DEST_PATH_IMAGE016
OMe 131-132
3-8
Figure 440512DEST_PATH_IMAGE017
OMe 1.5828(23.2)
3-9
Figure 596687DEST_PATH_IMAGE018
OMe 1.5672(24.5)
3-10
Figure 393742DEST_PATH_IMAGE019
OMe 1.5848(24.5)
3-11 OMe 77-78
3-12
Figure 113753DEST_PATH_IMAGE021
OMe 78-79
[table 4]
Figure 311385DEST_PATH_IMAGE011
Table 4 (X=N)
Compound N o. R 2 A-R 1 Physics value
4-4 2-Cl-4-CF 3 SMe 64-65
4-5 4-CH 2-t-Bu SMe ?
4-7 4-i-Bu SMe ?
4-11 4-O-i-Pr SMe ?
4-13 4-t-Bu SMe ?
Contain the pyrimidine derivatives by formula (I) expression of the present invention and be suitable for control to deleterious various insects such as paddy rice, fruit tree, vegetables, other crop, flowers and ornamental plants, such as agricultural gardening pest insect, storage grain pest, sanitary insect pest, nematode etc. as the salt, garderning pesticide of effective constituent.They have remarkable insecticidal effect for following insect: lepidopteran ( Lepidoptera), comprise fruit leaf roller in summer ( AdoXIophyes oranfasciata), Adoxophyes spp belong to ( AdoXIophyesSp.), manchurian fruit ( Grapholita inopinata), oriental fruit months ( Grapholita molesta), eating-core bean worm ( Leguminivora glycinivorella), the mulberry tree tortrix moth ( Olethreutes mori), the thin moth of tea ( Caloptilia thevivora), suddenly spend thin moth ( Caloptilia zachrysa), the little thin moth of diving of golden line ( Phyllonorycter ringoniella), pear pear barkminer ( Spulerrina astaurota), small white Japan subspecies ( Piers rapae crucivora), Heliothis ( HeliothisSp.), the Pericarpium Mali pumilae steinernema ( Laspey resia pomonella), small cabbage moth ( Plutella XIylostella), apple silver moth ( Argyresthia conjugella), peach post fruit moth ( Carposina niponensis), striped rice borer ( Chilo suppressalis), cnaphalocrocis medinalls guenee ( Cnaphalocrocis medinalis), tobacco powder sp ( Ephestia elutelia), the wild snout moth's larva of mulberry thin,tough silk ( Glyphodes pyloalis), yellow rice borer ( Scirpophaga incertulas), the straight burr rice hesperiidae ( Parnara guttata), mythimna separata ( Pseudaletia separata), Sesamia inferens ( Sesamia inferens), the greedy noctuid of twill ( Spodoptera litura), greedy noctuid ( Spodoptera egigua) etc.;
Hemiptera ( Hemiptera), comprise two leafhoppers ( Macrosteles fascifrons), rice green leafhopper ( NephotettXI cincticepts), brown paddy plant hopper ( Nilaparvata lugens), white backed planthopper ( Sogatella furcifera), the tangerine wood louse ( Diaphorina citri), grape white fly (Trialeurodes vittata) ( Aleurolobus taonabae), sweet potato whitefly ( Bemisia tabaci), greenhouse whitefly ( Trialeurodes vaporariorum), radish aphid ( Lipaphis erysimi), black peach aphid ( Myzus persicae), ceroplastes ( Ceroplastes ceriferus), the tangerine giant coccid ( Pulvinaria aurantii), camphor tree net armored scale ( Pseudaonidia dupleXI), the Sheng Qiongsikang armored scale ( Comstockaspis perniciosa), unaspis shield kuwana ( Unaspis yanonensis) etc.;
Coleoptera ( Coleoptera), comprise meadow nematode ( PratylenchusSp.), the polychrome different beetle ( Anomala rufocuprea), Japan popillia flavosellata fairmaire ( Popilla japonica), lasioderma serricorne ( Lasioderma serricorne), Lyctus brunneus Stephens ( Lyctus brunneus), potato bug ( Epilachna vigintioctopunctata), red bean resemble ( Callosobruchus chinensis), vegetables resemble ( Listroderes costirostris), sitophilus zea-mais ( Sitophilus zeamais), cotton boll resemble ( Anthonomus grandis grandis), rice water resemble ( Lissorhoptrus oryzophilus), aulacophora femoralis ( Aulacophora femoralis), Oulema oryzae ( Oulema oryzae), Phyllotreta striolata ( Phyllotreta striolata), vertical pit cutting pin small moth ( Tomicus piniperda), colorado potato beetles ( Leptinotarsa decemlineata), mexican bean ladybird ( Epilachna varivestis), pumpkin 12 asterophyllite first ( DiabroticaSp.) etc.;
Diptera ( Diptera), comprise the few hair on the neck trypetid of melon ( Dacus( Zeugodacus) Cucurbitae), the tangerine fruit fly ( Dacus( Bactrocera) Dorsalis), barley king eye ephydrid ( Agromyza oryzae), green onion ground plant fly ( Delia antiqua), delia platura ( Delia platura), soybean pod gall-midge ( AsphondyliaSp.), housefly ( Musca domestica), tame mosquito ( CuleXI pipiens pipiens) etc.;
Tylenchida ( Tylenchida), comprise Pratylenchidae belong to ( PratylenchusSp.), potato nematode ( Glabodera rostchiensis), Meloidogyne ( MeloidogyneSp.), partly puncture nematode ( Tylenchulus semipenetrans), true Aphelenchoides kind ( Aphelenchus avenae), Aphelenchoides ritzema-bosi ( Aphelenchoides ritzemabosi) etc.; And
Acarina ( Acarina), comprise citrus red mite (crm) ( Panonychus citri), panonychus ulmi ( Panonychus uimi), pearl sand tetranychid ( Tetranychus cinnabarinus), refreshing Ze Shi tetranychid ( Tetranychus KanzawaI Kishida), Tetranychus urticae ( Tetranychus urticae Koch), tea point leaf goitre mite ( Acaphylla theae), tangerine peronium goitre mite ( Aculops pelekassi), the dragon first beautiful goitre mite ( Calacarus carinatus), goitre mite on the pears ( Epitrimerus pyri) etc.
In addition, its any white ants for infringement dwelling house, building materials, furniture, leather, fiber, plastic working article, electric wire, cable etc. demonstrates the significant termite effect of killing with low dosage, and said white ants comprises: Rhinotermitidae ( Rhinotermitidae), such as coptotermes formosanus of taiwan ( Coptotermes formosanus Shiraki), Japanese subteranean termite ( Reticulitermessperatus( Kolbe)); Be present in North America the west reticulitermes flavipe ( Reticulitermes Hesperus), U.S. black shin reticulitermes flavipe ( Reticulitermes tibialis), the North America reticulitermes flavipe ( Reticulitermes flavipes) etc.; Be present in Mediterranean Sea bank southern Europe reticulate pattern termite ( Reticulitermes lucifugus), the Sang Te reticulitermes flavipe ( Reticulitermes santonensis) etc.; The common dry-wood termite of the U.S. ( Incisitermes minor( Hagen)); Termitidae ( Termitidae), such as the Taiwan formosanes ( Odontotermes formosanus( Shiraki)); Kalotermitidae ( Kalotermitidae), such as big black dry-wood termite ( Cryptotermes domesticus( Haviland)); And Termopsidae ( Termopsidae), such as the wet carpented ant of Japan ( Hodotermopsis jzponica( Holmgren)) etc.In addition, it is for communal facility and dwelling house in make inroads on crop, the park etc., and the ant class of harm people demonstrates the significant ant effect of killing with low dosage, and said ant class comprises: Formicidae ( Formicidae), such as little black ant ( Monomorium pharaoni Linnes), Japanese honey ant ( Monomorium nipponense Wheeler), nine divisions of China in remote antiquity back of a bow ant ( Camponotus kiusiuensis Santschi), black ant ( Formica japonica Motschulsky), bright hair ant ( Lasius fuliginosus (Latreille)) etc., and fiery ant (the black fiery ant (S that is present in North America Olenopsis richteri), red fire ant ( Solenopsis invicta), Solenopsis geminata ( Solenopsis geminata( F))) etc.
Further, the pyrimidine derivatives by formula (I) expression of the present invention also can be used for resisting the epizoon of animal, and said animal is: domestic animal, such as ox, horse, sheep etc.; Pet is such as dog, cat etc.; Simple gate tooth order ( Simplicidentata) animal, such as mouse, rat, hamster, squirrel etc.; Lagomorpha ( Lagomorpha) animal; Carnivora ( Carnivora) animal, such as ferret etc.; And birds, such as duck, chicken, pigeon etc., and have the intensive insecticidal effect for following epizoa, for example: Siphonaptera ( Aphaniptera) insect, such as cat flea ( Ctenocephalides felis), dog flea ( Ctenocephalides canis), Xanthopsyllacheopis ( XIenopsylla cheopis) etc.; Acarina ( Acari) insect, such as haemaphysalis longicornis ( HaemaphyXlalis longicornis), boophilus microplus ( Boophilus microplus) etc.; Anoplura ( Anoplura) insect, such as ox louse ( Haematopinus eurysternus), the sheep lice ( Damalinia ovis) or the like.
Contain the pyrimidine derivatives by formula (I) expression of the present invention and have remarkable control action kou as the salt, garderning pesticide of effective constituent for above insect of giving an example, these insects are harmful to wet crop, dry crop, fruit tree, vegetables and other crop, flowers and ornamental plant etc.Therefore, can be through estimating period that insect can occur, before their occur or when confirming that they occur, this agent administration being shown the desired effect of agriculture and garden sterilant of the present invention in the cultivation carriers such as the seed of culture facility, paddy field, field, fruit tree, vegetables, other crop, flowers and ornamental plant, water, stem and the leaf or the soil in paddy field etc.Especially preferred use form is to utilize to be known as metastatic the using of infiltration, and said infiltration transitivity is to allow via soil or do not absorb The compounds of this invention via soil from root, wherein to the soil of growing seedlings of crop, flowers and ornamental plant etc.; Planting hole soil during transplanting; Plant food; Irrigation water; The cultivation water that hydroponic culture is used etc. is handled.
Recently; Gene recombination crop (herbicide-resistant crop, introduced pest-resistant harmful crop that Pesticidal toxins produces gene, disease-resistant crop, the mouthfeel of having introduced disease resistance inductor producer gene improved crop, keeping quality improves crop, yield improvement crop etc.), insect sex pheromone (pheromone of leaf roller, lopper worm etc. is disturbed chemical), use IPM (integrated pest management) technology of natural enemy insect etc. to make progress, and salt, garderning pesticide of the present invention can use or through using with this type of technological systemization with this type of technical tie-up.
Can use the plant of salt, garderning pesticide of the present invention to have no particular limits, for example it can be used for following plant.
It can be applied to following plants; For example: cereal (for example, paddy rice; Barley; Wheat; Rye; Oat; Corn etc.); Beans (soybean; Red bean; Broad bean; Pea; Kidney bean; Peanut etc.); Fruit tree and fruit class (apple; Oranges and tangerines; Pears; Grape; Peach; Plum; Cherry; English walnut; Sweet chestnut; Almond; Banana; Strawberry etc.); Greengrocery (wild cabbage; Tomato; Spinach; Cauliflower; Lettuce; Onion; Shallot; Green pepper; Eggplant; Pepper etc.); Root vegetables (Radix Dauci Sativae; Potato; Sweet potato; Taro; Radish; Lotus rhizome; Turnip; Burdock; Garlic etc.); Processing is with crop (cotton; Fiber crops; Beet tails; Golden hop; Sugarcane; Beet; Olive; Rubber; Coffee; Tobacco; Tea etc.); Melon (pumpkin; Cucumber; Muskmelon; Watermelon; Muskmelon etc.); Herbage class (orchardgrass; Chinese sorghum; Thimothy grass; Clover; Alfalfa etc.); Lawn class (Korea S jielu grass; Creeping bentgrass etc.); Spices is with crop (lavender; Rosmarinus officinalis; Thymus vulgaris; Parsley; Pepper; Ginger etc.); Flowers (chrysanthemum; Rose; Carnation; Orchid etc.); Garden trees (ginkgo; Japanese cherry; Peach jaurel etc.); Forest (abies sachalinensis ( Abies sachalinensis), the fish scale dragon spruce ( Picea jezoensis), pine, Thujopsis dolabrata ( Thujopsis dolabrata), Japanese arbor-vitae (Japanese cedar), Japanese cypress (Japanese cypress) etc.) etc.
In order to control various insects, only need be directly or after water etc. suitably dilutes or is suspended in wherein with salt, garderning pesticide of the present invention, with to Pest Control or nematode effectively amount be applied to the plant that expectation can produce insect and nematode.For example; For the insect or the nematode that produce in fruit tree, cereal, the vegetables etc.; With insecticide spraying in stem or leaf portion; Perhaps absorb from root through following processing; Said processing is: seed treatment, such as medicament being immersed seed, seed dressing (dressing of seeds), Calper processing etc.; Soil treatment, such as the soil holostrome mix, seed furrow is used, bed soil mixes, nest eye (cell seedling) is handled, planting hole is handled, plant food is handled, the case of executing topdressing, paddy rice is handled (box treatment), used for ponds etc.In addition, salt, garderning pesticide can also through in the nutrient solution that is applied to nutrient solution (water plough) cultivation, utilize sootiness or trunk injection etc. use use.
Only need be directly or after water etc. suitably dilutes or is suspended in wherein with salt, garderning pesticide of the present invention, with to Pest Control effectively amount be applied to the place that expectation can produce insect.For example also can use as follows: be sprayed on storage grain pest, dwelling house insect, sanitary insect pest, injurious forest-insect etc., and to coatings such as dwelling house and building materials, sootiness, execute poison bait etc.
Method as seed treatment; Can enumerate conventional method; For example: comprise with seed impregnated in method through medicament is soaked into, comprise through seed is mixed with preparation or mix that medicine (dressing) waits and with solid preparation or liquid preparation attach to seed-coat method, comprise with stickiness carrier (for example, resin, polymkeric substance etc.) and preparation mixed be incorporated in the method for formation coating on the seed and comprise be applied near the method for seed etc. when planting simultaneously.
" seed " of above-mentioned pending seed treatment is meant the plant materials at the cultivation initial stage that is used to breed, and comprise seed and bulb, stem tuber, potato seed (seed potato), plumule, propagulum (propagule), bulb, utilize cutting propagation nourish and generate with plant materials etc.
When the method for use of embodiment of the present invention, " soil " of plant and " cultivation carrier " are meant the supporter that cultivated plant is used, and in particular for the supporter of root growth, and material is not subjected to special restriction.As long as plant can grow therein then any material all can, concrete material comprises for example soil, grow seedlings bed, water etc.Also can use sand, float stone, vermiculite, diatomite, agar, spawn, polymer material, rock silk floss, glass wool, wood chip, bark etc. as concrete material.
As to the stem of crop and leaf, or store the method that grain pest, dwelling house insect, sanitary insect pest, injurious forest-insect etc. are used; Method can be listed below: comprise suitable diluted liquid preparation of water (such as emulsion, preparation etc. can flow) or solid preparation (such as wettable powder or water dispersion granule etc.), and with the method for its sprinkling; Spray the method for pulvis; Perhaps sootiness etc.
As for being applied to soil, method for example can be listed below: comprise with dilution or undiluted liquid preparation in water be applied to plant materials plant food, grow seedlings with the method in nursery etc.; Comprise and granule is applied to the plant food of plant materials or grows seedlings with the method in nursery etc.; Comprise prior to seeding or transplant before poudrage, wettable powder, water dispersion granule, granule etc. and allow them to sneak into the whole method of soil; Comprise prior to seeding or plantation forward direction kind plant hole, seed furrow etc. are used the method etc. of wettable powder, water dispersion granule, granule etc.
In the situation of the nursery box of paddy rice, formulation can be used when for example sowing, use when afforesting, use when transplanting etc. and change according to opportunity.Can use formulations such as pulvis, water dispersion granule, granule.Also can use through sneaking in the compost (grove soil), wherein this compost can mix with pulvis, water dispersion granule, granule etc., for example, can adopt and sneak into bed soil, sneaks into earthing, sneak into compost integral body etc.Simply, compost and various preparation can be with the interbedded formation administered.
As the method that is applied to the paddy field, usually with solid preparations such as large-scale spray agent (jumbo), filling agent (pack), granule, water dispersion granules; Liquid preparation such as flowing agent, emulsion is sprayed on the waterflooding field.Perhaps, can also be when rice transplanting with appropriate formulation directly or be applied to after fertilizer mixes or inject soil.In addition, through liquid agent such as emulsion, flowing agent being applied to water-in and flowing to the current source in paddy field, thereby can in the process that supplies water, use effortlessly such as irrigation equipment etc.
To dry crop, can sow during the nursery stage, to seed, desire to be placed near the cultivation carrier plant materials etc. and handle.To desiring directly to be seeded in the plant in field, during preferably to the direct processing of seed, cultivation to the processing of the plant food of plant etc.The soil with water dilution or undiluted liquid agent of using, use that can carry out granule injects processing etc.Also be preferred processing with granule with cultivating the carrier fusion and sowing this adulterant prior to seeding.
The cultivated plant that desire is transplanted is in the processing of sowing or nursery stage, the preferably direct processing of seed, grows seedlings with liquid agent and to carry out its dispersion treatment with the soil-perfusion processing in nursery or with granule.In addition, during field planting with granule handle kind of a plant hole, near transplanting place cultivation carrier mixes with granule also is preferred processing with desiring to be positioned over.
Salt, garderning pesticide of the present invention is prepared into according to the general manner of formulation of agrochemicals usually and makes things convenient for the available form.
That is to say; With of the present invention by the pyrimidine derivatives shown in the formula (I) and optional adjuvants and suitable inert support with the suitable proportion fusion and through dissolving, disperse, suspend, mix, flood, adsorb or adhere the appropriate formulation form that is prepared into, concentrate thing, wettable powder, water dispersion granule, granule, pulvis, tablet, filling agent etc. like suspension-s, emulsifiable concentrate, solubility.
The available inert support can be solid or liquid among the present invention.As the material that can be used as solid carrier; Can exemplify soyflour; Grain flour; Wood chip; Tree bark powder; Sawdust; The powdered tobacco stem; The powdery walnut shell; Chaff; Solka-floc; The extraction leftover of vegetables; Resin (like powdered synthetic polymer etc.); Clay (kaolin for example; Wilkinite; And acid clay); Talcs (for example talcum and pyrophyllite); Ground silica or fragment (diatomite for example; Quartz sand; Mica and hard charcoal [synthetic polymolecularity silicic acid; Also be known as hydrated silica in small, broken bits or silicate hydrate; Calucium Silicate powder is contained as main ingredient in some commercially available prod]); Inorganic or mineral dust; Like gac; Powdery sulphur; Float stone; Calcination diatomite; The brick that pulverizes; Flying dust; Husky; Lime carbonate; Calcium phosphate etc.; Plastic carrier; Like Vilaterm; Polypropylene; Gather (vinylidene chloride) etc.; Chemical fertilizer (ammonium sulfate for example; Ammonium phosphate; Ammonium nitrate; Urea and ammonium chloride), and compost.These carriers can use separately or wherein two kinds or more kinds of mixture uses of conduct.
The material that can be used as liquid vehicle is selected from itself has solvability or even without this solvability but can come the material of dispersed activity composition by auxiliary agent.The representative instance that is liquid-carrier below also can use separately or the wherein mixture use of two or more of conduct: water; Alcohol (methyl alcohol for example; Ethanol; Isopropyl alcohol; Butanols and ethylene glycol); Ketone (acetone for example; Methyl ethyl ketone; Methyl iso-butyl ketone (MIBK); DIBK and cyclohexanone); Ether (ether for example; Two alkane; Cellosolve; Dipropyl ether and oxolane); Aliphatic hydrocarbon (for example kerosene and mineral oil); Aromatic hydrocarbon (benzene for example; Toluene; Dimethylbenzene; Solvent naphtha and Fluhyzon); Halogenated hydrocarbons (dichloroethanes for example; Chloroform; Carbon tetrachloride and chlorobenzene); Ester (ethyl acetate for example; The phthalic acid diisopropyl ester; Dibutyl phthalate and dioctyl phthalate); Acid amides (dimethyl formamide for example; DEF and dimethylacetylamide); Nitrile (for example acetonitrile); And dimethyl sulfoxide (DMSO).
Be the representative instance of said auxiliary agent below, it uses according to purpose and uses separately or two kinds or more kinds of being used in combination, or needn't use fully in some cases.
For emulsification, dispersion, dissolving and/or wetting compound as activeconstituents; Can use tensio-active agent, such as Voranol EP 2001, polyoxyethylene alkylaryl ether, polyoxyethylene high-grade aliphatic ester, polyoxyethylene resinate, polyoxyethylene sorbitan mono-laurate, polyoxyethylene sorbitan monoleate, alkylaryl sulphonate, naphthene sulfonic acid condensation product, sulfonated lignin and higher alcohol sulfate.
In addition; In order to stablize dispersion as the compound of activeconstituents; To can use casein, gelatin, starch, methylcellulose gum, carboxymethyl cellulose, Sudan Gum-arabic, gather (vinyl alcohol), turps, oil extracted from rice husks, wilkinite and sulfonated lignin etc. as the compound adhesion and/or the combination of activeconstituents.In order to improve the flowability of solid product, can use wax, stearate, alkyl phosphate etc.
The auxiliary agent of naphthene sulfonic acid condensation product and phosphoric acid ester polycondensate and so on can be used as the peptizing agent that can divide lively stock; Can also use silicone oil etc. as defoamer; And can use 1, the auxiliary agent of 2-benzisothiazole-3-ketone, parachlormetaxylenol, butyl p-hydroxybenzoate and so on is as sanitas.
In addition, if necessary, all right functions of use property spreading agent, active reinforcing agent (like the metabolism decomposing inhibitor, like piperonyl butoxide), frostproofer (like Ucar 35), antioxidant (like BHT), UV light absorber and other auxiliary agent.
Content as the compound of activeconstituents can change as required, can use with the ratio of in the scope of 0.01-90 weight part/100 part agriculture and garden reagent, suitably selecting as the compound of activeconstituents.For example, in pulvis, granule, emulsion or wettable powder, be 0.01-50 weight % as the appropriate level of the compound of activeconstituents.
The amount of application of agent for controlling noxious insect pests of the present invention, especially salt, garderning pesticide changes with various factors, trend, weather, envrionment conditions, formulation, the application process that occurs like the growth conditions of purpose, the insect that will control, plant, insect, uses place and time of application.It can restrain to the scope of 1kg (with regard to regard to the compound of activeconstituents)/10 ares at 0.001g to 10 kg, preferred 0.01 according to purpose and suitably select.
Can mixing with other salt, garderning pesticide, miticide, nematocides, mycocide, biological pesticide etc. of agent for controlling noxious insect pests of the present invention, especially salt, garderning pesticide used with the scope of widening the may command disease and insect and time cycle of effectively using or minimizing dosage.In addition, salt, garderning pesticide of the present invention can mix use with weedicide, plant-growth regulator, fertilizer etc. according to application scenarios.
As other salt, garderning pesticide that is used for above-mentioned purpose; Miticide and nematocides; Can exemplify following salt, garderning pesticide; Miticide and nematocides are like Nialate (Ethion); Trichlorphon (Trichlorfon); Acephatemet (Methamidophos); Acephate (Acephate); SD-1750 (Dichlorvos); Phosdrin (Mevinphos); Monocrotophos (Monocrotophos); Malathion (Malathion); Rogor (Dimethoate); Peace fruit (Formothion); Mecarbam (Mecarbam); Vamidothion (Vamidothion); Thiometon (Thiometon); Thiodemeton (Disulfoton); Thiometan (Oxydeprofos); Naled (Naled); Parathion-methyl (Methyl parathion); Fenitrothion 95 (Fenitrothion); Cynock (Cyanophos); Kayaphos (Propaphos); Tiguvon (Fenthion); Toyodan (Prothiofos); Profenofos (Profenofos); Isofenphos (Isofenphos); Temephos (Temephos); Tsidial (Phenthoate); Dimethylvinphos (Dimethylvinphos); Zaprawa enolofos (Chlorfenvinphos); Tetrachlorvinphos (Tetrachlorvinphos); Volaton (Phoxim);
Figure 375473DEST_PATH_IMAGE005
Azoles phosphorus (Isoxathion); Pyraclofos (Pyraclofos); Methidathion (Methidathion); Chlorpyrifos 94 (Chlorpyrifos); Chlorpyrifos_methyl (Chlorpyrifos-methyl); Pyridaphenthione (Pyridaphenthion); Diazinon (Diazinon); Pririmiphos_methyl (Pirimiphos-methyl); Phosalone (Phosalone); R-1504 (Phosmet); Dioxabenzofos (Dioxabenzofos); Resitox (Quinalphos); Terbufos (Terbufos); Ethoprophos (Ethoprophos); Cadusafos (Cadusafos); Nematode spirit (Mesulfenfos); DPS (NK-0795); Phosphorus worm prestige (Phosphocarb); Fenamiphos (Fenamiphos); Different amine pine (Isamidofos); Lythidathion (Fosthiazate); Isazofos (Isazofos); Ethoprop (Ethoprophos); Tiguvon (Fenthion); Fosthietan (Fostietane); Dichlofenthion (Dichlofenthion); Ethyl pyrazinyl phosphorothioate (Thionazin); Sulprofos (Sulprofos); Fensulfothion (Fensulfothion); Nellite (Diamidafos); Pyrethrin (Pyrethrin); Esbiothrin (Allethrin); The alkynes third chrysanthemum ester (Prallethrin); Resmethrin (Resmethrin); Permethrin (Permethrin); Tefluthrin (Tefluthrin); Bi Fenning (Bifenthrin); Fenvalerate (Fenpropathrin); Cypermethrin (Cypermethrin); Alphacypermethrin (α-Cypermethrin); Cyfloxylate (Cyhalothrin); Smart betacyfluthrin (λ-Cyhalothrin); Deltamethrin (Deltamethrin); Acrinathrin (Acrinathrin); Fenvalerate (Fenvalerate); Efficient fenvalerate (Esfenvalerate); Cycloprothrin (Cycloprothrin); Ether chrysanthemum ester (Etofenprox); Halfenprox (Halfenprox); Salifluofen (Silafluofen); Flucythrinate (Flucythrinate); Fluorine amine fenvalerate (Fluvalinate); Methomyl (Methomyl); Oxamyl (Oxamyl); The two prestige (Thiodicarb) of sulphur; Aldicarb (Aldicarb); Alanycarb (Alanycarb); Cartap (Cartap); Meta-tolyl-N-methylcarbamate (MTMC) (Metolcarb); Xylylcarb (Xylylcarb); Propoxur (Propoxur); Fenoxycarb (Fenoxycarb); Fenobucarb (Fenobucarb); Benzene worm prestige (Ethiophencarb); Fenothiocarb (Fenothiocarb); Bifenazate (Bifenazate); Fenobucarb (Fenobucarb); Carbaryl (Carbaryl); Aphox (Pirimicarb); Carbofuran (Carbofuran); Carbosulfan (Carbosulfan); Furathiocarb (Furathiocarb); Benfuracarb (Benfuracarb); Aldoxycarb (Aldoxycarb); Methamidophos (Diafenthiuron); Diflubenzuron (Diflubenzuron); Fluorobenzene urea (Teflubenzuron); Fluorine bell urea (Hexaflumuron); Napropamide (Novaluron); Chlorine fragrant new (Lufenuron); Flufenoxuron (Flufenoxuron); UC 62644 (Chlorfluazuron); Fenbutatin oxide (Fenbutatin oxide); Tin tricyclohexylhydroxide (Tricyclohexyltin hydroxide); Sodium oleate; Potassium oleate; Methoprene (Methoprene); Hydroprene (Hydroprene); Niagara 9044 (Binapacryl); Amitraz (Amitraz); Kelthane (Dicofol); Kai Ersheng (Kelthane); G-23922 (Chlorobenzilate); Bromopropylate (Bromopropylate); Tetradifon (Tetradifon); Bensultap (Bensultap); Benzoximate (Benzoximate); Worm hydrazides (Tebufenozide); Methoxyfenozide (Methoxyfenozide); Pyridalyl (Pyridalyl); Ring worm hydrazides (Chromafenozide); Alkynes mite special (Propargite); Mite quinone (Acequinocyl) goes out; 5a,6,9,9a-hexahydro-6,9-methano-2,4 (Endosulfan); Dioxathion (Diofenolan); Bromothalonil (Chlorfenapyr); Azoles mite ester (Fenpyroximate); Azoles insect amide (Tolfenpyrad); Fluorine worm nitrile (Fipronil); Tebufenpyrad (Tebufenpyrad); Triaxamate (Triazamate); Second mite azoles (Etoxazole); Hexythiazox (Hexythiazox); Nicotine sulfate (Nicotine sulfate); Ti304 (Nitenpyram); Acetamiprid (Acetamiprid); Thiophene worm quinoline (Thiacloprid); Provado (Imidacloprid); Thiophene worm piperazine (Thiamethoxam); Thiophene worm amine (Clothianidin); MTI-446 (Dinotefuran); Fluazinam (Fluazinam); Pyrrole propyl ether (Pyriproxyfen); Hydramethylnon Bait (Hydramethylnon); Pyrimidifen (Pyrimidifen); Reach leech ketone (Pyridaben); Fly eradication amine (Cyromazine); TPIC (isocyanuric acid three propyl ester); Pyrrole aphid ketone (Pymetrozine); Four mite piperazines (Clofentezine); Buprofezin (Buprofezin); Thiocyclam (Thiocyclam); Fenazaquin (Fenazaquin); Chinomethionate (Chinomethionate); Indenes worm prestige (Indoxacarb); Mitecidin C (Polynactin complexes); More visit rhzomorph (Milbemectin); Avrmectin (Abamectin); Emaricin (Emamectin-benzoate); Pleocidin (Spinosad); BT (bacillus thuringiensis ( Bacillus thuringiensis)), nimbin (Azadirachtin), fish rise ketone (Rotenone), hydroxypropylated starch (Hydroxypropyl starch), R-12564 (Levamisole hydrochloride), metamsodium (Metam-sodium), morantel tartrate (Morantel tartrate), dazomet (Dazomet), trichlamide (Trichlamide), pasteurellaceae handle bacterium ( Pasteuria penetrans), knurl catch genus monacrosporium ( Monacrosporium- Phymatophagum) etc.
With the same purpose as agricultural and horticultural use of fungicides, as can be exemplified agricultural and horticultural fungicides, such as sulfur, lime sulfur (Lime? Sulfur), basic copper sulfate (Copper? Sulfate? Basic), Iprobenfos (Iprobenfos), edifenphos (Edifenphos), methyl Tolclofos (Tolclofos-methyl), thiram (Thiram), on behalf of Senfu America zinc? (Polycarbamate), Zineb (Zineb), Dyson Manganese (Maneb), mancozeb (Mancozeb), Propineb (Propineb), thiophanate (Thiophanate), thiophanate-methyl (Thiophanate? methyl), benomyl (Benomyl), amine acetate Iminoctadine Salt (Iminoctadine? acetate), biguanide Trioctylamine alkylbenzene sulfonate (Iminocutadine? albecylate), destroy embroidered amine (Mepronil), fluorine-amide (Flutolanil), Pencycuron (Pencycuron), furosemide bacteria topiramate amine (Furametpyr), thiophene amine fluoride bacteria (Thifluzamide), metalaxyl (Metalaxyl),
Figure 759181DEST_PATH_IMAGE005
Cream Spirit (Oxadixyl), cyclopropane acid bacteria amine (Carpropamid), antibacterial Ling (Dichlofluanid), flusulfamide (Flusulfamide), chlorothalonil (Chlorothalonil) , Kresoxim (Kresoxim-methyl), cyano bacteria amine (Fenoxanil),
Figure 889948DEST_PATH_IMAGE005
mold Ling (Hymexazol), soil benomyl (Etridiazole), chlorofluorocarbons sclerotia Lee (Fluoroimide), procymidone (Procymidone), vinclozolin (Vinclozolin), iprodione (Iprodione), triadimefon (Triadimefon), triflumizole (Triflumizole),? Bitertanol (Bitertanol), triflumizole (Triflumizole), ipconazole (Ipconazole), fluorine itraconazole (Fluconazole), propiconazole (Propiconazole), diphenyl itraconazole (Difenoconazole), myclobutanil (Myclobutanil), PTFE ether azole (Tetraconazole), Hexaconazole (Hexaconazole), tebuconazole (Tebuconazole), acyl acetazolamide (Imibenconazole), prochloraz (Prochloraz), pefurazoate (Pefurazoate), Cyproconazole (Cyproconazole), Isoprothiolane (Isoprothiolane), fenarimol (Fenarimol), pyrimethanil (Pyrimethanil), mepanipyrim (Mepanipyrim), piperidine spot oxime (Pyrifenox), fluazinam (Fluazinam), triforine (Triforine), da cycloheximide (Diclomezine), azoxystrobin (Azoxystrobin), trifloxystrobin (trifloxystrobin)?, oxime ether bacteria amine (orysastrobin)?, thiadiazines (Thiadiazine), captan (Captan), thiophene acid bacteria amine (Tiadinil), allyl isothiazole (Probenazole), activated ester (Acibenzolar-S-methyl? (CGA -245,704)), tetrachlorophthalide (Fthalide), Tricyclazole (Tricyclazole), pyroquilon (Pyroquilon), Chinomethionate (Chinomethionat), oxolinic acid (Oxolinic? acid), dithianon (Dithianon)? , Cyazofamid (cyazofamid), thiophene acid bacteria amine (Tiadinil), double-cypermethrin bacteria amine (diclocymet), kasugamycin (Kasugamycin), Jinggangmycin (Validamycin), polymyxin (Polyoxin), blasticidin (Blasticidin), Streptomycin (Streptomycin), etc.
Similarly, as herbicides include herbicides such as the following: glyphosate (Glyphosate), grass phosphinothioyl (Sulfosate), glyphosate (Glufosinate), bialaphos (Bialaphos), suppression grass phosphorus (Butamifos) , E Caodan (Esprocarb), prosulfocarb (Prosulfocarb), grasses Dan (Benthiocarb), barnyardgrass Dan (Pyributicarb), Asulam (Asulam), linuron (Linuron), Daimuron (Dymron), iso Long (Isouron), Bensulfuron (Bensulfuron? methyl), Cyclosulfamuron (Cyclosulfamuron), ethyl ether (Cinosulfuron), topiramate ethyl (Pyrazosulfuron? ethyl), ethyl tetrazole (Azimsulfuron) , zolpidem ethyl (Imazosulfuron), thiophene metolachlor (Thenylchlor), alachlor (Alachlor), metolachlor (Pretilachlor), barnyardgrass amine (Clomeprop), Ethyl benzene metolachlor (Etobenzanid), benzoth acyl alachlor (Mefenacet), flufenacet (flufenacet), tetrazole acid metolachlor (fentrazamide), pendimethalin (Pendimethalin), carboxymethyl nitrofen (Bifenox), acifluorfen (Acifluorfen), milk Fluorine diclofop (Lactfen), Cyhalofop (Cyhalofop-butyl), iodobenzonitrile (Ioxynil), bromine butyrylcholinesterase metolachlor (Bromobutide), grasses off (Alloxydim), sethoxydim (Sethoxydim), Diuron amine (Napropamide), indanofan (Indanofan), Pyrazolate (Pyrazolate), topiramate grass ketone (Benzofenap), topiramate grass ether (Pyraflufen-ethyl), imidazole hydrochloride (Imazapyr), methanesulfonic alachlor (Sulfentrazone), azole alachlor (Cafenstrole), cyclopentyl
Figure 799184DEST_PATH_IMAGE005
Grass ketone (Bentoxazon),
Figure 48900DEST_PATH_IMAGE005
Grass ketone (oxadiazon), paraquat (Paraquat), diquat (Diquat), ethyl ether grass (Pyriminobac), simazine (Simazine), atrazine (Atrazine), isoamyl net (Dimethametryn), triazine amine fluoride grass (Triaziflam), furosemide grass yellow (Benfuresate), fluthiacet methyl (Fluthiacet-methyl), quizalofop (Quizalofop-ethyl), bentazone ( Bentazone),
Figure 34174DEST_PATH_IMAGE005
metribuzin (oxaziclomefone), azole piperidine grass ketone (azafenidin), bicyclic Sulcotrione (benzobicyclon), calcium peroxide.
As for biological pesticide; Through salt, garderning pesticide of the present invention and following material are mixed use can expect obtain with more than identical effect, said material for example: the virus formulation that waits acquisition by NPV (NPV), granulosis virus(GV) (GV), plasmotype polyhedron disease virus (CPV), entomopoxvirus (EPV); As the microbial pesticide of sterilant or nematocides, as knurl catch genus monacrosporium ( Monacrosporium phymatophagum), steinernema Stahli line worm ( Steinernema carpocapsae), Steinernema kushidai, the thorn pasteurellosis bacillus ( Pasteuria penetrans) etc.; As the microbial pesticide of mycocide, as lignin wood mould ( Trichoderma lignorum), agrobacterium radiobacter ( Agrobacterium radiobactor), non-pathogenic carrot soft rot Erwinia ( Erwinia carotovora), Bacillus subtilus ( Bacillus subtilis) etc.; With as the biological pesticide of weedicide such as xanthomonas campestris ( XIanthomonas campestris) etc.
In addition, agriculture and garden of the present invention is with the reagent use that can combine with biological pesticide, and said biological pesticide comprises natural enemy, as parasitic wasp (Encarsia formosa ( Encarsia formosa)), parasitic wasp (the A Bula chalcid fly ( Aphidius colemani)), cecidomyiia ( Aphidoletes aphidimyza), parasitic wasp (the fly Ji chalcid fly of diving ( Diglyphus isaea)), the parasitic mite class (from jaw cocoon honeybee ( Dacnusa sibirica)), predacious mites (Chilean little phytoseiid mite ( Phytoseiulus persimilis)), predatism stinkbug class (the East Asia minute pirate bugs ( Orius sauteri)) etc.; Microbial pesticide, as muscardine ( Beauveria brongniartii) etc.; And pheromone; Like (Z)-10-tetradecene yl acetate, (E; Z)-4,10-14 carbon dialkylene acetic ester, (Z)-8-dodecylene yl acetate, (Z)-11-tetradecene yl acetate, (Z)-13-eicosylene-10-ketone, (Z)-8-dodecylene yl acetate, (Z)-11-tetradecene yl acetate, (Z)-13-eicosylene-10-ketone, 14-methyl isophthalic acid-vaccenic acid etc.
Embodiment
Following example representative embodiment of the present invention, these embodiment also are not interpreted as restrictive.
Embodiment 1
(1-1) manufacturing of 2-chloro-4-(4-tert-butyl-phenyl)-5-methoxy pyrimidine
Figure 281615DEST_PATH_IMAGE022
With 4-tert.-butylbenzene ylboronic acid (3.98 g, 0.022 mol), yellow soda ash (7.00 g, 0.066 mol), 2,4-two chloro-5-methoxy pyrimidines (4.0 g, 0.022 mol) and tetrakis triphenylphosphine palladium (2.54 g, 0.0022 mol) join in the mixed solvent of acetonitrile (60 mL) and water (40 mL).The reaction vessel argon replaces, and this mixture reacted 3 hr under reflux.This mixture is cooled to room temperature, and injects water.Wash with methyl tertiary butyl ether this mixture of extraction and with saturated brine.Use the anhydrous magnesium sulfate drying organic layer, distillation removes and desolvates.Residue with the silica gel column chromatography purifying so that target product (4.33 g) to be provided,
Yield: 71%
Rerum natura: fusing point m.p.=77-79 ℃.
(1-2) preparation of 4-(4-tert-butyl-phenyl)-5-methoxy pyrimidine (compound N o. 1-53)
Figure 352340DEST_PATH_IMAGE023
Sodium acetate (2.57 g, 0.031 mol), 5% palladium carbon (1.44 g) and 2-chloro-4-(4-tert-butyl-phenyl)-5-methoxy pyrimidine (4.33 g, 0.016 mol) are joined in the ethanol (100 mL), react 3 hr down in atmosphere of hydrogen (3.0 atm).Remove solid through diatomite filtration, and concentrating under reduced pressure filtrating.In residue, add saturated sodium bicarbonate aqueous solution, and use the ethyl acetate extraction mixture.Use the anhydrous magnesium sulfate drying organic layer, and distillation is except that desolvating.Residue with the silica gel column chromatography purifying so that target product (4.00 g) to be provided,
Yield: quantitatively (quant.)
Rerum natura: refractive index n D=1.5689 (26.6 ℃).
The preparation of embodiment 2. 4-(4-tert-butyl-phenyl)-5-hydroxy pyrimidine (compound N o. 1-1)
4-(4-tert-butyl-phenyl)-5-methoxy pyrimidine (1.40 g, 5.78 mmol) and lithium iodide (2.48 g, 18.5 mmol) are joined in the 2 (6 mL) reaction 8 hr under reflux.This mixture is cooled to room temperature, and injects 3N hydrochloric acid (30 ml).With this mixture ethyl acetate extraction.Use the anhydrous magnesium sulfate drying organic layer, and distillation is except that desolvating.Residue with the silica gel column chromatography purifying so that target product (0.73 g) to be provided,
Yield: 55%
Rerum natura: fusing point m.p.=104-106 ℃.
The preparation of embodiment 3. 4-(4-tert-butyl-phenyl)-5-positive propoxy pyrimidine (compound N o. 1-86)
Figure 435407DEST_PATH_IMAGE025
4-(4-tert-butyl-phenyl)-5-hydroxy pyrimidine (0.37 g, 1.62 mmol), n-propyl alcohol (0.18 g, 2.43 mmol) and triphenylphosphine (0.64 g, 2.43 mmol) are joined in the tetrahydrofuran (THF) (5 mL), and in this solution, drip diethyl azodiformate (1.06 g, 2.43 mmol).Then, this mixture is at room temperature reacted 2 hr.Concentrating under reduced pressure reaction soln, residue with the silica gel column chromatography purifying so that target product (0.27 g) to be provided,
Yield: 62%
Rerum natura: refractive index n D=1.5618 (25.5 ℃).
The preparation of embodiment 4. 4-(3-nitro-4-neo-pentyl phenyl)-5-methoxy pyrimidine (compound N o. 1-34)
The acid mixture of the preparation concentrated nitric acid (0.99 g, 9.6 mmol) and the vitriol oil (1.48 g, 15.0 mmol), and be cooled to 0 ℃.4-(4-neo-pentyl phenyl)-5-methoxy pyrimidine (1.75 g, 6.8 mmol) is dissolved in the vitriol oil (2 ml), and this mixture is cooled to 0 ℃.With this concentrated sulfuric acid solution so that interior temperature is no more than 5 ℃ mode slowly is added drop-wise in the acid mixture of prepared beforehand.After dropping, this mixture heating up to room temperature, and is further stirred 2 hr.Reaction mixture is injected in the frozen water, and,, uses the dried over mgso organic layer with sodium bicarbonate aqueous solution and saturated brine washing with this mixture of ethyl acetate extraction.Distillation removes desolvates, residue with the silica gel column chromatography purifying so that target product (1.93 g) to be provided,
Yield: 94%
Rerum natura: refractive index n D=1.5549 (26.1 ℃).
The preparation of embodiment 5. 4-(3-amino-4-neo-pentyl phenyl)-5-methoxy pyrimidine (compound N o. 1-33)
Figure 208508DEST_PATH_IMAGE027
4-(3-nitro-4-neo-pentyl phenyl)-5-methoxy pyrimidine (1.93 g, 6.4 mmol) and iron powder (1.07 g, 19.2 mmol) are added in the mixed solvent of ethyl acetate (30 ml), AcOH (10 ml) and water (10 ml), and make this mixture in argon atmosphere, reflux under the reaction 3 hr.After the cooling,,, use the dried over mgso organic layer with sodium bicarbonate aqueous solution and saturated brine washing with this mixture ethyl acetate extraction.Distillation removes desolvates, residue with the silica gel column chromatography purifying so that target product (1.48 g) to be provided,
Yield: 85%
Rerum natura: refractive index n D=1.5778 (26.1 ℃).
The preparation of embodiment 6. 4-(3-chloro-4-neo-pentyl phenyl)-5-methoxy pyrimidine (compound N o. 1-29)
Figure 3288DEST_PATH_IMAGE028
With 4-(3-amino-4-neo-pentyl phenyl)-5-methoxy pyrimidine (650 mg, 2.04 mmol) and CuCl 2(387 mg, 2.88 mmol) are dissolved in the acetonitrile (10 ml), and this mixture is cooled to 0 ℃.In this solution,, temperature slowly drips t-BuONO (nitrous acid tertiary butyl ester) (371 mg, 3.60 mmol) so that being no more than 5 ℃ mode.This mixture slowly is heated to room temperature, and 2 hr then reflux.After the cooling, this mixture is passed through diatomite filtration.Filtrating is used ethyl acetate extraction, with sodium bicarbonate aqueous solution and saturated brine washing, uses the dried over mgso organic layer.Distillation removes desolvates, residue with the silica gel column chromatography purifying so that target product (194 mg) to be provided,
Yield: 28%
Rerum natura: fusing point m.p.=41-43 ℃.
Embodiment 7.
(7-1) preparation of 4-isobutyl-phenacyl bromide
Figure 697575DEST_PATH_IMAGE029
4-isobutyl acetophenone (5.0 g, 28.4 mmol) is added in the acetate (15 ml), with this mixture heating up to 70 ℃.Dripping bromine in this solution (4.8 g, 29.8 mmol) makes this mixture at room temperature react 30 min.Make this reaction soln be cooled to room temperature, and carry out concentrating under reduced pressure, so that target product (7.8 g) to be provided,
Yield: quantitatively
Rerum natura: 1H-NMR (CDCl 3/ TMS, δ value ppm) 7.90 (2H, m), 7.26 (2H, d), 4.44 (2H, s), 2.55 (2H, d), 1.91 (1H, m), 0.91 (6H, d)
(7-2) preparation of 4-isobutyl phenenyl methylthiomethyl ketone
Figure 536087DEST_PATH_IMAGE030
(20 g, 42.6 mmol) join in the Virahol (30 ml) with the sodium methyl mercaptide aqueous solution.At room temperature in this solution, add 4-isobutyl-phenacyl bromide (7.2 g, 28.4 mmol), this mixture is reacted 2 hr under uniform temp.In this reaction soln, add ethyl acetate, with this mixture water and saturated brine washing.Use the anhydrous magnesium sulfate drying organic layer, and carry out concentrating under reduced pressure, so that target product (5.7 g) to be provided.This product is purified and directly be used for next reaction,
Yield: 91%
Rerum natura: 1H-NMR (CDCl 3/ TMS, δ value ppm) 7.90 (2H, d), 7.24 (2H, d), 3.75 (2H, s), 2.53 (2H, d), 2.15 (3H, s), 1.91 (1H, m), 0.91 (6H, d)
(7-3) preparation of 3-(dimethylamino)-1-(4 '-isobutyl phenenyl)-2-(methylthio group) third-2-alkene-1-ketone
Figure 581403DEST_PATH_IMAGE031
In dimethylformamide dimethyl acetal (1.6 g, 13.5 mmol), add 4-isobutyl phenenyl methylmercaptoethyl ketone (2.0 g, 9.0 mmol), then this mixture is reacted 5.5 hr under reflux.This mixture is cooled to room temperature, and carries out concentrating under reduced pressure, so that target product (2.5 g) to be provided.This product is purified and directly be used for next reaction,
Yield: quantitatively
Rerum natura: 1H-NMR (CDCl 3/ TMS, δ value ppm) 7.42 (2H, d), 7.13 (2H, d), 3.28 (6H, s), 2.49 (2H, d), 2.13 (3H, s), 0.90 (6H, d)
(7-4) preparation of 4-(4-isobutyl phenenyl)-5-methylthiopyrimidine (compound N o. 2-9)
Figure 976612DEST_PATH_IMAGE032
Sodium ethylate (0.92 g, 13.5 mmol) is added in the ethanol (10 ml), this mixture is cooled to 0 ℃.In this solution, add amitraz hydrochloride (1.2 g, 11.7 mmol) and 3-(dimethylamino)-1-(4 '-isobutyl phenenyl)-2-(methylthio group) third-2-alkene-1-ketone, this mixture was at room temperature reacted 3 days.The concentrating under reduced pressure reaction soln, and add ethyl acetate.This mixture with saturated aqueous sodium carbonate and saturated brine washing, use the anhydrous magnesium sulfate drying organic layer, and distillation is except that desolvating.Residue with the silica gel column chromatography purifying so that target product (0.72 g) to be provided,
Yield: 31%
Rerum natura: refractive index n D=1.5189 (24.5 ℃).
The preparation of embodiment 8. 4-(4-isobutyl phenenyl)-5-methyl sulfinyl pyrimidine (compound N o. 2-10)
Figure 463088DEST_PATH_IMAGE033
5-methylthio group-4-(4-isobutyl phenenyl) pyrimidine (0.2 g, 0.8 mmol) is dissolved in the chloroform (5 ml), and this solution is cooled to 0 ℃.In this solution, add metachloroperbenzoic acid (0.2 g, 0.9 mmol), this mixture is reacted 2 hr under uniform temp.Ethyl acetate is joined in the reaction soln, and this mixture is washed with saturated aqueous sodium carbonate and saturated brine.Use the anhydrous magnesium sulfate drying organic layer, and distillation is except that desolvating.Residue with the silica gel column chromatography purifying so that target product (0.16 g) to be provided.
Yield: 76%
Rerum natura: refractive index n D=1.4911 (23.3 ℃).
Embodiment 9.
(9-1) preparation of 4-isobutyl phenenyl methyl sulphonyl methyl ketone
Figure 551130DEST_PATH_IMAGE034
(1.8 g, 8.1 mmol) are dissolved in the chloroform (5 ml) with 4-isobutyl phenenyl methylthiomethyl ketone, and this solution is cooled to 0 ℃.In this solution, add metachloroperbenzoic acid (4.3 g, 20.3 mmol), then this mixture is at room temperature reacted 2 hr.In reaction soln, add ethyl acetate, and this mixture is washed with saturated aqueous sodium carbonate and saturated brine.Use the anhydrous magnesium sulfate drying organic layer, and distillation is except that desolvating.Residue with the silica gel column chromatography purifying so that target product (1.5 g) to be provided,
Yield: 73%
Rerum natura: 1H-NMR (CDCl 3/ TMS, δ value ppm) 7.92 (2H, d), 7.29 (2H, d), 4.58 (2H, s), 3.22 (3H, s), 2.55 (2H, d), 1.91 (1H, m), 0.91 (6H, d)
(9-2) preparation of 3-(dimethylamino)-1-(4 '-isobutyl phenenyl)-2-(methyl sulphonyl) third-2-alkene-1-ketone
Figure 818163DEST_PATH_IMAGE035
In dimethylformamide dimethyl acetal (1.1 g, 8.9 mmol), add 4-isobutyl phenenyl methyl sulphonyl methyl ketone (1.5 g, 5.9 mmol), then this mixture is reacted 3.5 hr under reflux.The concentrating under reduced pressure reaction soln is to provide target product (1.8 g).This product is purified and directly be used for next reaction,
Yield: quantitatively
Rerum natura: 1H-NMR (CDCl 3/ TMS, δ value ppm) 7.73 (2H, d), 7.21 (2H, d), 3.19 (6H, s), 2.52 (2H, d), 2.29 (3H, s), 1.91 (1H, m), 0.90 (6H, d)
(9-3) preparation of 4-(4-isobutyl phenenyl)-5-sulfonyloxy methyl yl pyrimidines (compound N o. 2-11)
(0.61 g, 8.9 mmol) are dissolved in the ethanol (10 ml) with sodium ethylate, and this mixture is cooled to 0 ℃.In this solution, add ethanol (5 ml) solution of amitraz hydrochloride (0.8 g, 7.7 mmol) and 3-(dimethylamino)-1-(4 '-isobutyl phenenyl)-2-(methyl sulphonyl) third-2-alkene-1-ketone (1.8 g, 5.9 mmol), then this mixture is reacted 2 hr under reflux.This reaction soln is cooled to room temperature, and distillation is except that desolvating.In residue, add ethyl acetate, and this mixture is washed with saturated sodium bicarbonate aqueous solution and saturated brine.Use the anhydrous magnesium sulfate drying organic layer, and distillation is except that desolvating.Residue with the silica gel column chromatography purifying so that target product (0.92 g) to be provided,
Yield: 54%
Rerum natura: fusing point m.p.=57-58 ℃.
Below describe representative formulation example of the present invention and Test Example, but they should not be construed as the scope of the present invention that limits.
Term " part " used in the instance is meant weight part.
Formulation example 1
10 parts of compounds of the present invention
70 parts of xylenes
10 parts of N-Methyl pyrrolidone
10 parts in the mixture of polyoxyethylene nonylplenyl ether and alkyl benzene calcium sulfonate
With mentioned component effectively dissolving mix and make missible oil.
Formulation example 2
3 parts of compounds of the present invention
82 parts in clay powder
15 parts of diatomite powders
Mentioned component is mixed and pulverizes and make pulvis.
Formulation example 3
5 parts of compounds of the present invention
90 parts of the mix powders of wilkinite and clay
5 parts of calcium lignin sulphonates
Mentioned component is mixed, and gained mixture and an amount of water is mixing, then granulation and dry and make granule.
Formulation example 4
20 parts of compounds of the present invention
75 parts in the mixture of kaolin and synthetic high dispersive silicic acid
5 parts in the mixture of polyoxyethylene nonylplenyl ether and alkyl benzene calcium sulfonate
Mentioned component is mixed and pulverizes and make wettable powder.
Test Example 1.
To black peach aphid ( Myzus persicae) prevention effect
In each plastic tub of diameter 8 cm and height 8 cm, plant Chinese cabbage (Chinese cabbage) plant, and black peach aphid is bred on this plant, add up the number of parasites in each basin then.With of the present invention by formula (I) expression each pyrimidine derivatives or its salt is scattered in the water and dilute with water to obtain 500 ppm liquid chemicals.Spray stem and the leaf of potted plant Chinese cabbage plant with this liquid chemical, and air-dry, then this basin is stored in the greenhouse.After sprinkling the 6th day, add up the number of black peach aphid parasitic on each Chinese cabbage plant and calculate the prevention effect degree, thereby judge insecticidal effect based on standard as follows with equation,
Prevention effect=100-(T * Ca)/(Ta * C) } * 100
Ta: the number of parasites in the treatment group before sprinkling
T: the number of parasites in the treatment group after sprinkling
Ca: the number of parasites in the untreated fish group before sprinkling
C: the number of parasites in the untreated fish group after sprinkling
A prevention effect 100%
B prevention effect 99%-90%
C prevention effect 89%-80%
D prevention effect 79%-50%.
Test Example 2.
To brown paddy plant hopper ( Nilaparvata lugens) insecticidal effect
With of the present invention by formula (I) expression each substituted pyrimidine derivatives or its salt is scattered in the water and dilute with water to obtain 500 ppm liquid chemicals.Rice seedlings (kind: Japan fine (Nihonbare)) are immersed in this liquid chemical 30 seconds and air-dry, then with each rice shoot as in the glass developmental tube, inoculate with the tritonymph of 10 brown paddy plant hoppers, with this developmental tube tampon jam-pack.After inoculation 8 days, add up the number of the dead worm and the worm that lives.Calculate mortality ratio with equation, and judge prevention effect according to standard as follows.
Figure 607314DEST_PATH_IMAGE037
Identical in criterion and the Test Example 1.
As a result of, in the pyrimidine derivatives by formula (I) expression of the present invention, the compound of following compounds number demonstrates horizontal D or above insecticidal effect to black peach aphid:
Compound number 1-2; 1-3; 1-6; 1-7; 1-8; 1-9; 1-10; 1-11; 1-13; 1-14; 1-15; 1-17; 1-18; 1-20; 1-22; 1-25; 1-26; 1-27; 1-29; 1-30; 1-31; 1-33; 1-34; 1-36; 1-38; 1-41; 1-42; 1-44; 1-46; 1-48; 1-49; 1-50; 1-51; 1-52; 1-53; 1-55; 1-58; 1-59; 1-60; 1-61; 1-63; 1-64; 1-66; 1-70; 1-72; 1-74; 1-76; 1-77; 1-78; 1-79; 1-80; 1-84; 1-86; 1-98; 1-110; 1-122; 1-134; 1-146; 1-148; 1-149; 1-152; 1-153; 1-156; 1-157; 1-158; 1-161; 1-162; 1-177; 1-178; 1-179; 1-180; 1-181; 1-184; 1-185; 1-186; 1-187; 1-188; 1-191; 1-192; 1-193; 1-194; 1-195; 1-196; 1-198; 1-199; 1-200; 1-202; 1-207; 1-209; 1-210; 1-211; 1-213; 1-215; 1-216; 1-217; 1-219; 1-224; 1-225; 1-226; 1-229; 1-230; 1-231; 1-232; 1-233; 1-234; 1-235; 1-236; 1-237; 1-238; 1-239; 1-241; 1-244; 1-245; 1-246; 1-247; 1-249; 1-250; 1-251; 1-252; 1-253; 1-255; 1-256; 1-258; 1-259; 1-260; 1-261; 1-262; 1-264; 1-265; 1-266; 1-267; 1-268; 1-269; 1-270; 1-272; 1-275; 1-276; 1-278; 1-280; 1-281; 1-282; 1-284; 1-285; 1-287; 1-289; 1-290; 1-291; 1-292; 1-293; 1-294; 1-295; 1-296; 1-297; 1-298; 1-299; 1-300; 1-303; 1-305; 1-306; 1-308; 1-309; 1-310; 1-311; 1-312; 1-313; 1-317; 1-318; 1-320; 1-321; 1-324; 1-327; 1-328; 1-330; 1-333; 1-335; 1-336; 1-341; 1-344; 1-350; 1-355; 1-356; 1-357; 1-360; 1-361; 1-362; 1-364; 1-367; 1-368; 1-370; 1-371; 1-372; 1-373; 1-376; 1-377; 1-378; 1-379; 1-380; 1-381; 1-382; 1-384; 1-387; 1-388; 1-390; 1-391; 1-392; 1-396; 1-397; 1-399; 1-401; 1-402; 1-403; 1-404; 1-408; 1-409; 1-411; 1-412; 1-413; 1-414; 1-415; 1-417; 1-418; 1-419; 1-420; 1-421; 1-422; 1-423; 1-424; 1-425; 1-426; 1-427; 1-428; 1-429; 1-431; 1-433; 1-434; 1-437; 1-439; 1-441; 1-443; 1-444; 1-445; 1-446; 1-447; 1-449; 1-451; 1-453; 1-454; 1-455; 1-456; 1-457; 1-458; 1-460; 1-464; 1-465; 1-466; 1-469; 1-470; 1-471; 1-472; 1-475; 1-476; 1-477; 1-478; 1-480; 1-481; 1-482; 1-483; 1-485; 1-486; 1-487; 1-488; 1-489; 1-490; 1-494; 1-495; 1-496; 1-497;
2-5,2-7,2-9,2-10,2-13,2-15,2-16,2-17,2-19,2-20,2-21,2-23,2-25,2-27,2-29,2-33,2-37,2-41,2-45,2-47,2-49,2-57,2-59,2-60,2-61,2-62,2-64,2-65,2-66,2-67,2-68,2-69,2-70,2-71,2-80,2-81,3-1,3-2,3-3,3-4,3-5,3-7,3-9,3-10,3-11,3-12 and 4-4
Especially the compound exhibits of following compounds number goes out the excellent pesticidal effect of horizontal A:
Compound number 1-3; 1-11; 1-14; 1-25; 1-26; 1-27; 1-29; 1-30; 1-34; 1-36; 1-38; 1-41; 1-42; 1-44; 1-49; 1-50; 1-51; 1-52; 1-53; 1-55; 1-58; 1-61; 1-64; 1-66; 1-74; 1-76; 1-78; 1-79; 1-80; 1-86; 1-134; 1-149; 1-156; 1-161; 1-178; 1-179; 1-180; 1-181; 1-186; 1-191; 1-193; 1-200; 1-216; 1-226; 1-229; 1-230; 1-234; 1-235; 1-244; 1-250; 1-258; 1-260; 1-261; 1-266; 1-267; 1-268; 1-269; 1-275; 1-278; 1-280; 1-290; 1-293; 1-298; 1-306; 1-310; 1-320; 1-328; 1-360; 1-368; 1-372; 1-373; 1-377; 1-379; 1-380; 1-384; 1-387; 1-388; 1-390; 1-391; 1-392; 1-403; 1-415; 1-417; 1-423; 1-424; 1-425; 1-426; 1-427; 1-428; 1-431; 1-439; 1-441; 1-446; 1-447; 1-455; 1-457; 1-458; 1-469; 1-470; 1-472; 1-477; 1-481; 1-485; 1-486; 1-495; 2-5; 2-9; 2-15; 2-20; 2-25; 2-27; 2-33; 2-45; 2-49; 2-59; 2-61; 2-65; 2-66; 2-67; 2-81; 3-5 and 4-4.
In addition, the compound of following compounds number demonstrates the excellent pesticidal effect of horizontal A to brown paddy plant hopper:
Compound number 1-1; 1-2; 1-3; 1-4; 1-5; 1-6; 1-7; 1-8; 1-10; 1-11; 1-13; 1-14; 1-15; 1-18; 1-20; 1-23; 1-24; 1-25; 1-26; 1-27; 1-29; 1-30; 1-31; 1-34; 1-36; 1-38; 1-41; 1-42; 1-44; 1-46; 1-47; 1-48; 1-49; 1-50; 1-51; 1-52; 1-53; 1-55; 1-58; 1-59; 1-60; 1-61; 1-62; 1-63; 1-64; 1-66; 1-70; 1-72; 1-74; 1-76; 1-77; 1-78; 1-79; 1-80; 1-82; 1-84; 1-86; 1-98; 1-106; 1-108; 1-110; 1-122; 1-134; 1-146; 1-149; 1-150; 1-156; 1-158; 1-159; 1-161; 1-162; 1-177; 1-178; 1-179; 1-180; 1-181; 1-184; 1-185; 1-186; 1-187; 1-188; 1-191; 1-192; 1-193; 1-196; 1-199; 1-200; 1-201; 1-202; 1-203; 1-205; 1-206; 1-207; 1-208; 1-209; 1-210; 1-211; 1-212; 1-213; 1-215; 1-216; 1-217; 1-219; 1-221; 1-222; 1-224; 1-225; 1-226; 1-227; 1-229; 1-230; 1-231; 1-232; 1-233; 1-234; 1-235; 1-236; 1-238; 1-239; 1-240; 1-241; 1-244; 1-245; 1-246; 1-247; 1-250; 1-251; 1-252; 1-253; 1-254; 1-255; 1-256; 1-257; 1-258; 1-259; 1-260; 1-261; 1-262; 1-264; 1-265; 1-266; 1-267; 1-268; 1-269; 1-270; 1-272; 1-273; 1-274; 1-275; 1-276; 1-277; 1-278; 1-279; 1-280; 1-281; 1-282; 1-286; 1-288; 1-289; 1-290; 1-291; 1-292; 1-293; 1-294; 1-295; 1-296; 1-297; 1-298; 1-299; 1-300; 1-301; 1-302; 1-303; 1-304; 1-306; 1-308; 1-309; 1-310; 1-311; 1-312; 1-313; 1-314; 1-315; 1-317; 1-319; 1-320; 1-321; 1-323; 1-324; 1-327; 1-328; 1-330; 1-333; 1-334; 1-335; 1-336; 1-339; 1-340; 1-341; 1-344; 1-345; 1-347; 1-349; 1-350; 1-351; 1-352; 1-354; 1-355; 1-356; 1-357; 1-358; 1-359; 1-360; 1-361; 1-362; 1-363; 1-364; 1-365; 1-366; 1-368; 1-369; 1-370; 1-372; 1-373; 1-374; 1-376; 1-377; 1-378; 1-379; 1-380; 1-381; 1-384; 1-385; 1-386; 1-387; 1-388; 1-389; 1-390; 1-391; 1-394; 1-395; 1-396; 1-397; 1-399; 1-400; 1-401; 1-402; 1-403; 1-404; 1-412; 1-413; 1-415; 1-416; 1-417; 1-418; 1-419; 1-420; 1-421; 1-422; 1-423; 1-424; 1-425; 1-426; 1-427; 1-428; 1-429; 1-431; 1-433; 1-434; 1-435; 1-436; 1-437; 1-438; 1-439; 1-440; 1-441; 1-442; 1-443; 1-444; 1-445; 1-446; 1-447; 1-448; 1-449; 1-453; 1-455; 1-456; 1-457; 1-458; 1-460; 1-462; 1-463; 1-464; 1-465; 1-466; 1-467; 1-468; 1-472; 1-473; 1-474; 1-475; 1-476; 1-477; 1-478; 1-479; 1-480; 1-481; 1-485; 1-486; 1-488; 1-490; 1-494; 1-495; 1-496; 1-497;
2-7,2-9,2-10,2-13,2-15,2-17,2-19,2-20,2-21,2-23,2-25,2-27,2-29,2-33,2-37,2-41,2-45,2-47,2-49,2-57,2-59,2-60,2-61,2-62,2-64,2-65,2-66,2-67,2-68,2-69,2-70,2-71,2-81,3-1,3-2,3-3,3-4,3-5,3-6,3-9,3-10,3-11,3-12 and 4-4.
The application is based on the patent application No. 309125/2008 of japanese publication, and its content all is contained among this paper.
Though the present invention representes with reference to its preferred specific embodiments and illustrates, it will be appreciated by those skilled in the art that into, under the situation that does not break away from the category of the present invention that appended claims contains, can carry out the change of various forms and details.Patent, the open case of patent or other publication pointed or that quote are incorporated among this paper with way of reference with it in full among all this paper.

Claims (7)

1. by pyrimidine derivatives or its salt of general formula (I) expression,
Figure 639691DEST_PATH_IMAGE001
Wherein, R 1Be
(a1) hydrogen atom;
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a22) aryl (C 1-C 6) alkyl;
(a23) has 1~5 identical or different substituent aryl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Hydrogen atom, (C can identical or different and respectively do for oneself 1-C 6) alkyl, (C 3-C 6) cycloalkyl, (C 2-C 6) thiazolinyl, (C 2-C 6) alkynyl, (C 3-C 6) cycloalkyl (C 1-C 6) alkyl, halo (C 1-C 6) alkyl, halo (C 3-C 6) cycloalkyl, halo (C 2-C 6) thiazolinyl, halo (C 2-C 6) alkynyl, halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl, phenyl, or phenyl (C 1-C 6) alkyl, perhaps R 3And R 4Can bonding and form and contain a nitrogen-atoms and then optional 1 or 2 identical or different heteroatomic 5~8 yuan nitrogen heterocyclic ring that is selected from Sauerstoffatom, sulphur atom and the nitrogen-atoms that contains;
(a24) cyanic acid (C 1-C 6) alkyl;
(a25) nitro (C 1-C 6) alkyl;
(a26) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a27) (R 3) OC (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a28) (R 3) O 2C (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a29) R 3(R 4) NCO (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a32) aryl sulfonyl;
(a33) have 1~5 identical or different substituent aryl sulfonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a34) aryl carbonyl;
(a35) have 1~5 identical or different substituent aryl carbonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a36) arylthio (C 1-C 6) alkyl;
(a37) has 1~5 identical or different substituent arylthio (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a38) aryl sulfinyl (C 1-C 6) alkyl;
(a39) has 1~5 identical or different substituent aryl sulfinyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a40) aryl sulfonyl (C 1-C 6) alkyl;
(a41) has 1~5 identical or different substituent aryl sulfonyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a42) aryl carbonyl oxygen (C 1-C 6) alkyl;
(a43) has 1~5 identical or different substituent aryl carbonyl oxygen (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a44) (C 1-C 6) alkyl-carbonyl;
(a45) (C 1-C 6) alkoxy carbonyl;
(a46) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a47) R 3(R 4) N ketonic oxygen (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a50) (C 1-C 6) alkoxy carbonyl oxygen (C 1-C 6) alkyl;
(a51) (C 1-C 6) alkyl (C 1-C 6) alkylsulfonyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo group;
(a54) heterocycle (C 1-C 6) alkyl;
(a55) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo group; Or
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different,
A is-O-,-S-,-SO-or-SO 2-,
R 2Can be identical or different, and each is naturally
(b1) halogen atom;
(b2) hydroxyl;
(b3) cyanic acid;
(b4) nitro;
(b5) N (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b6) N (R 3) CO (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b7) N (R 3) SO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b8) N (R 3) CO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b9) CO (R 3) group, wherein R 3Like above-mentioned definition;
(b10) CO 2(R 3) group, wherein R 3Like above-mentioned definition;
(b11) CON (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b12) C (R 3)=NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b13) (C 1-C 12) alkyl;
(b14) (C 2-C 12) thiazolinyl;
(b15) (C 2-C 12) alkynyl;
(b16) (C 3-C 12) cycloalkyl;
(b17) halo (C 1-C 12) alkyl;
(b18) halo (C 2-C 12) thiazolinyl;
(b19) halo (C 2-C 12) alkynyl;
(b20) halo (C 3-C 12) cycloalkyl;
(b21) three (C 1-C 12) the alkyl silyl, wherein said alkyl can be identical or different;
(b22) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b23) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b24) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b25) (C 3-C 12) cycloalkyl (C 3-C 12) cycloalkyl;
(b26) (C 1-C 12) alkoxyl group;
(b27) (C 2-C 12) alkene oxygen base;
(b28) (C 2-C 12) alkynyloxy group;
(b29) (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b30) halo (C 1-C 12) alkoxyl group;
(b31) halo (C 2-C 12) alkene oxygen base;
(b32) halo (C 2-C 12) alkynyloxy group;
(b33) halo (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b34) (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b35) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b36) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(b37) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b38) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b39) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b40) sulfydryl;
(b41) (C 1-C 12) alkylthio;
(b42) (C 2-C 12) alkenylthio group;
(b43) (C 2-C 12) the alkynes sulfenyl;
(b44) (C 3-C 12) the cycloalkyl sulfenyl;
(b45) halo (C 1-C 12) alkylthio;
(b46) halo (C 2-C 12) alkenylthio group;
(b47) halo (C 2-C 12) the alkynes sulfenyl;
(b48) halo (C 3-C 12) the cycloalkyl sulfenyl;
(b49) (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b50) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b51) (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b52) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b53) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b54) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b55) (C 1-C 12) the alkyl sulfinyl;
(b56) (C 2-C 12) the thiazolinyl sulfinyl;
(b57) (C 2-C 12) the alkynyl sulfinyl;
(b58) (C 3-C 12) the cycloalkyl sulfinyl;
(b59) halo (C 1-C 12) the alkyl sulfinyl;
(b60) halo (C 2-C 12) the thiazolinyl sulfinyl;
(b61) halo (C 2-C 12) the alkynyl sulfinyl;
(b62) halo (C 3-C 12) the cycloalkyl sulfinyl;
(b63) (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b64) halo (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b65) (C 1-C 12) alkyl sulphonyl;
(b66) (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b67) (C 2-C 12) the alkynyl alkylsulfonyl;
(b68) (C 3-C 12) the naphthene sulfamide base;
(b69) halo (C 1-C 12) alkyl sulphonyl;
(b70) halo (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b71) halo (C 2-C 12) the alkynyl alkylsulfonyl;
(b72) halo (C 3-C 12) the naphthene sulfamide base;
(b73) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b74) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b75) aryl;
(b76) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b77) aryl (C 1-C 6) alkyl;
(b78) has 1~5 identical or different substituent aryl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b79) aryloxy;
(b80) have 1~5 identical or different substituent aryloxy, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b81) aryloxy (C 1-C 6) alkyl;
(b82) has 1~5 identical or different substituent aryloxy (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b83) arylthio;
(b84) have 1~5 identical or different substituent arylthio, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b85) pyridyl oxygen base;
(b86) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl oxygen base in alkyl, (d) cyanic acid and (e) nitro;
(b87) pyridyl sulfenyl;
(b88) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl sulfenyl in alkyl, (d) cyanic acid and (e) nitro;
(b89) halo (C 1-C 6) alkylenedioxy group;
(b90) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b91) (C 3-C 8) alkylidene group;
(b92) (C 1-C 6) alkyl (C 3-C 8) alkylidene group;
(b93) three (C 1-C 12) the alkyl silyloxy, wherein said alkyl can be identical or different;
(b94) three (C 1-C 12) alkyl silyl (C 1-C 6) alkoxyl group, wherein said alkyl can be identical or different;
(b95) two (C 1-C 12) halogenated alkyl (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b96) two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b97) two (C 1-C 12) the alkyl hydroxy silyl, wherein said alkyl can be identical or different;
(b98) two (C 1-C 12) the alkyl hydrogen silyl, wherein said alkyl can be identical or different;
(b99) two (C 1-C 12) the alkyl phenyl silyl, wherein said alkyl can be identical or different;
(b100) (C 1-C 6) alkylthio (C 1-C 6) alkoxyl group;
(b101) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkoxyl group;
(b102) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkoxyl group;
(b103) (C 1-C 6) alkoxy carbonyl (C 1-C 6) alkoxyl group;
(b104) (C 1-C 6) alkyl-carbonyl (C 1-C 6) alkoxyl group;
(b105) cyanic acid (C 1-C 6) alkoxyl group;
(b106) aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation;
(b107) has 1~5 identical or different substituent aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation, and said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b108) hydroxyl (C 1-C 6) alkyl;
(b109) (C 1-C 6) alkylthio (C 1-C 6) alkyl-carbonyl;
(b110) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(b111) three (C 1-C 12) alkyl silyl (C 1-C 6) alkylthio, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b112) three (C 1-C 12) alkyl silyl (C 1-C 6) the alkyl sulfinyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b113) three (C 1-C 12) alkyl silyl (C 1-C 6) alkyl sulphonyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b114) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(b115) heterocyclic radical;
(b116) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b117) heterocyclic oxy group except that pyridyl oxygen base;
(b118) have 1~5 identical or different substituent heterocyclic oxy group except that pyridyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b119) the heterocycle sulfenyl except that the pyridyl sulfenyl;
(b120) have 1~5 identical or different substituent heterocycle sulfenyl except that the pyridyl sulfenyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b121) heterocycle sulfinyl;
(b122) have 1~5 identical or different substituent heterocycle sulfinyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b123) heterocycle alkylsulfonyl;
(b124) have 1~5 identical or different substituent heterocycle alkylsulfonyl, said substituting group is selected from: (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b125) heterocycle (C 1-C 6) alkyl oxy;
(b126) have 1~5 identical or different substituent Heterocyclylalkyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b127) (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b128) halo (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b129) group that is expressed from the next:
Figure 494514DEST_PATH_IMAGE002
R wherein 3And R 4Like above-mentioned definition and R 5Be hydrogen atom, (C 1-C 6) alkyl, (C 3-C 6) cycloalkyl, (C 2-C 6) thiazolinyl, (C 2-C 6) alkynyl, (C 3-C 6) cycloalkyl (C 1-C 6) alkyl, halo (C 1-C 6) alkyl, halo (C 3-C 6) cycloalkyl, halo (C 2-C 6) thiazolinyl, halo (C 2-C 6) alkynyl, halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl, phenyl, or phenyl (C 1-C 6) alkyl;
(b130) 4,4,5,5-tetramethyl--1,2,3-dioxane pentaborane-2-base;
(b131) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(b132) two (C 1-C 12) the alkyl benzyl silyl, wherein said alkyl can be identical or different;
(b133) heterocycle (C 1-C 6) alkyl; Or
(b134) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group, perhaps
R 2Can with adjacent R on the aromatic nucleus 2Form (b135) condensed ring or dicyclo together, this condensed ring or dicyclo are optional to have identical or different one or more substituting groups, and said substituting group is selected from: (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) alkyl, (d) (C 1-C 6) alkoxyl group, (e) halo (C 1-C 6) alkoxyl group, (f) (C 1-C 6) alkylthio, (g) halo (C 1-C 6) alkylthio, (h) (C 1-C 6) alkyl sulfinyl, (i) halo (C 1-C 6) alkyl sulfinyl, (j) (C 1-C 6) alkyl sulphonyl and (k) halo (C 1-C 6) alkyl sulphonyl,
M is 0 or 1 integer, and n is 0~4 integer, and
X be optional oxidized nitrogen-atoms or-CH-.
2. pyrimidine derivatives according to claim 1 or its salt,
Wherein A, R 2, definition in m, n and X such as the claim 1, and
R 1Be
(a1) hydrogen atom;
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a22) aryl (C 1-C 6) alkyl;
(a23) has 1~5 identical or different substituent aryl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like definition in the claim 1;
(a24) cyanic acid (C 1-C 6) alkyl;
(a25) nitro (C 1-C 6) alkyl;
(a26) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a27) (R 3) OC (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a28) (R 3) O 2C (C 1-C 6) alkyl, wherein R 3Like above-mentioned definition;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a32) aryl sulfonyl;
(a33) have 1~5 identical or different substituent aryl sulfonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a34) aryl carbonyl;
(a35) have 1~5 identical or different substituent aryl carbonyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a36) arylthio (C 1-C 6) alkyl;
(a37) has 1~5 identical or different substituent arylthio (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a38) aryl sulfinyl (C 1-C 6) alkyl;
(a39) has 1~5 identical or different substituent aryl sulfinyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a40) aryl sulfonyl (C 1-C 6) alkyl;
(a41) has 1~5 identical or different substituent aryl sulfonyl (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl and (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a44) (C 1-C 6) alkyl-carbonyl;
(a45) (C 1-C 6) alkoxy carbonyl;
(a46) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition;
(a47) R 3(R 4) N ketonic oxygen (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a50) (C 1-C 6) alkoxy carbonyl oxygen (C 1-C 6) alkyl;
(a51) (C 1-C 6) alkyl (C 1-C 6) alkylsulfonyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo group;
(a54) heterocycle (C 1-C 6) alkyl;
(a55) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo group; Or
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different.
3. pyrimidine derivatives according to claim 1 and 2 or its salt,
Wherein definition in m, n and X such as the claim 1,
R 1Be
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like definition and (t) phenoxy group in the claim 1;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a50) (C 1-C 6) alkoxy carbonyl oxygen (C 1-C 6) alkyl;
(a51) (C 1-C 6) alkyl (C 1-C 6) alkylsulfonyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo group; Or
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different,
A is-O-or-S-, and
R 2Can be identical or different, and each is naturally
(b1) halogen atom;
(b2) hydroxyl;
(b3) cyanic acid;
(b4) nitro;
(b5) N (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b6) N (R 3) CO (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b7) N (R 3) SO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b8) N (R 3) CO 2(R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b9) CO (R 3) group, wherein R 3Like above-mentioned definition;
(b10) CO 2(R 3) group, wherein R 3Like above-mentioned definition;
(b11) CON (R 3) (R 4) group, wherein R 3And R 4Like above-mentioned definition;
(b12) C (R 3)=NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b13) (C 1-C 12) alkyl;
(b14) (C 2-C 12) thiazolinyl;
(b15) (C 2-C 12) alkynyl;
(b16) (C 3-C 12) cycloalkyl;
(b17) halo (C 1-C 12) alkyl;
(b18) halo (C 2-C 12) thiazolinyl;
(b19) halo (C 2-C 12) alkynyl;
(b20) halo (C 3-C 12) cycloalkyl;
(b21) three (C 1-C 12) the alkyl silyl, wherein said alkyl can be identical or different;
(b22) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b23) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b24) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b25) (C 3-C 12) cycloalkyl (C 3-C 12) cycloalkyl;
(b26) (C 1-C 12) alkoxyl group;
(b27) (C 2-C 12) alkene oxygen base;
(b28) (C 2-C 12) alkynyloxy group;
(b29) (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b30) halo (C 1-C 12) alkoxyl group;
(b31) halo (C 2-C 12) alkene oxygen base;
(b32) halo (C 2-C 12) alkynyloxy group;
(b33) halo (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b34) (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b35) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b36) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(b37) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b38) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b39) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b41) (C 1-C 12) alkylthio;
(b42) (C 2-C 12) alkenylthio group;
(b43) (C 2-C 12) the alkynes sulfenyl;
(b44) (C 3-C 12) the cycloalkyl sulfenyl;
(b45) halo (C 1-C 12) alkylthio;
(b46) halo (C 2-C 12) alkenylthio group;
(b47) halo (C 2-C 12) the alkynes sulfenyl;
(b48) halo (C 3-C 12) the cycloalkyl sulfenyl;
(b49) (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b50) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b51) (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b52) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b53) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b54) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b55) (C 1-C 12) the alkyl sulfinyl;
(b56) (C 2-C 12) the thiazolinyl sulfinyl;
(b57) (C 2-C 12) the alkynyl sulfinyl;
(b58) (C 3-C 12) the cycloalkyl sulfinyl;
(b59) halo (C 1-C 12) the alkyl sulfinyl;
(b60) halo (C 2-C 12) the thiazolinyl sulfinyl;
(b61) halo (C 2-C 12) the alkynyl sulfinyl;
(b62) halo (C 3-C 12) the cycloalkyl sulfinyl;
(b63) (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b64) halo (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b65) (C 1-C 12) alkyl sulphonyl;
(b66) (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b67) (C 2-C 12) the alkynyl alkylsulfonyl;
(b68) (C 3-C 12) the naphthene sulfamide base;
(b69) halo (C 1-C 12) alkyl sulphonyl;
(b70) halo (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b71) halo (C 2-C 12) the alkynyl alkylsulfonyl;
(b72) halo (C 3-C 12) the naphthene sulfamide base;
(b73) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b74) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b75) aryl;
(b76) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b79) aryloxy;
(b80) have 1~5 identical or different substituent aryloxy, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b81) aryloxy (C 1-C 6) alkyl;
(b82) has 1~5 identical or different substituent aryloxy (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b83) arylthio;
(b84) have 1~5 identical or different substituent arylthio, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b85) pyridyl oxygen base;
(b86) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl oxygen base in alkyl, (d) cyanic acid and (e) nitro;
(b87) pyridyl sulfenyl;
(b88) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl sulfenyl in alkyl, (d) cyanic acid and (e) nitro;
(b89) halo (C 1-C 6) alkylenedioxy group;
(b90) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b91) (C 3-C 8) alkylidene group;
(b92) (C 1-C 6) alkyl (C 3-C 8) alkylidene group;
(b93) three (C 1-C 12) the alkyl silyloxy, wherein said alkyl can be identical or different;
(b94) three (C 1-C 12) alkyl silyl (C 1-C 6) alkoxyl group, wherein said alkyl can be identical or different;
(b95) two (C 1-C 12) halogenated alkyl (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b96) two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b97) two (C 1-C 12) the alkyl hydroxy silyl, wherein said alkyl can be identical or different;
(b98) two (C 1-C 12) the alkyl hydrogen silyl, wherein said alkyl can be identical or different;
(b99) two (C 1-C 12) the alkyl phenyl silyl, wherein said alkyl can be identical or different;
(b100) (C 1-C 6) alkylthio (C 1-C 6) alkoxyl group;
(b101) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkoxyl group;
(b102) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkoxyl group;
(b103) (C 1-C 6) alkoxy carbonyl (C 1-C 6) alkoxyl group;
(b104) (C 1-C 6) alkyl-carbonyl (C 1-C 6) alkoxyl group;
(b105) cyanic acid (C 1-C 6) alkoxyl group;
(b106) aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation;
(b107) has 1~5 identical or different substituent aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation, and said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b108) hydroxyl (C 1-C 6) alkyl;
(b109) (C 1-C 6) alkylthio (C 1-C 6) alkyl-carbonyl;
(b110) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(b111) three (C 1-C 12) alkyl silyl (C 1-C 6) alkylthio, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b112) three (C 1-C 12) alkyl silyl (C 1-C 6) the alkyl sulfinyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b113) three (C 1-C 12) alkyl silyl (C 1-C 6) alkyl sulphonyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b114) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(b115) heterocyclic radical;
(b116) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b117) heterocyclic oxy group except that pyridyl oxygen base;
(b118) have 1~5 identical or different substituent heterocyclic oxy group except that pyridyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b119) the heterocycle sulfenyl except that the pyridyl sulfenyl;
(b120) have 1~5 identical or different substituent heterocycle sulfenyl except that the pyridyl sulfenyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b125) heterocycle (C 1-C 6) alkyl oxy;
(b126) have 1~5 identical or different substituent Heterocyclylalkyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b127) (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b128) halo (C 1-C 12) alkyl (C 3-C 12) cycloalkyl;
(b129) group that is expressed from the next:
R wherein 3, R 4And R 5Like definition in the claim 1;
(b130) 4,4,5,5-tetramethyl--1,2,3-dioxane pentaborane-2-base;
(b131) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(b132) two (C 1-C 12) the alkyl benzyl silyl, wherein said alkyl can be identical or different;
(b133) heterocycle (C 1-C 6) alkyl; Or
(b134) have 1~5 identical or different substituent Heterocyclylalkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group, perhaps
R 2Can with adjacent R on the aromatic nucleus 2Form (b135) condensed ring or dicyclo together, this condensed ring or dicyclo are optional to have identical or different one or more substituting groups, and said substituting group is selected from: (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) alkyl, (d) (C 1-C 6) alkoxyl group, (e) halo (C 1-C 6) alkoxyl group, (f) (C 1-C 6) alkylthio, (g) halo (C 1-C 6) alkylthio, (h) (C 1-C 6) alkyl sulfinyl, (i) halo (C 1-C 6) alkyl sulfinyl, (j) (C 1-C 6) alkyl sulphonyl and (k) halo (C 1-C 6) alkyl sulphonyl.
4. according to each pyrimidine derivatives or its salt in the claim 1~3,
Wherein definition in m, n and X such as the claim 1,
R 1Be
(a2) (C 1-C 6) alkyl;
(a3) (C 3-C 6) cycloalkyl;
(a4) (C 2-C 6) thiazolinyl;
(a5) (C 2-C 6) alkynyl;
(a6) halo (C 1-C 6) alkyl;
(a7) halo (C 3-C 6) cycloalkyl;
(a8) halo (C 2-C 6) thiazolinyl;
(a9) halo (C 2-C 6) alkynyl;
(a10) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a11) (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a12) (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a13) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a14) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a15) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a16) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkyl;
(a17) halo (C 1-C 6) alkylthio (C 1-C 6) alkyl;
(a18) halo (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkyl;
(a19) halo (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkyl;
(a20) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a21) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkyl;
(a30) aryl;
(a31) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) phenoxy group;
(a48) three (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(a49) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(a52) heterocyclic radical;
(a53) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition and (t) oxo group; Or
(a56) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different,
A is-O-or-S-, and
R 2Can be identical or different, and each is naturally
(b1) halogen atom;
(b4) nitro;
(b13) (C 1-C 12) alkyl;
(b14) (C 2-C 12) thiazolinyl;
(b15) (C 2-C 12) alkynyl;
(b16) (C 3-C 12) cycloalkyl;
(b17) halo (C 1-C 12) alkyl;
(b18) halo (C 2-C 12) thiazolinyl;
(b19) halo (C 2-C 12) alkynyl;
(b20) halo (C 3-C 12) cycloalkyl;
(b21) three (C 1-C 12) the alkyl silyl, wherein said alkyl can be identical or different;
(b22) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b23) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b24) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl;
(b25) (C 3-C 12) cycloalkyl (C 3-C 12) cycloalkyl;
(b26) (C 1-C 12) alkoxyl group;
(b27) (C 2-C 12) alkene oxygen base;
(b28) (C 2-C 12) alkynyloxy group;
(b29) (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b30) halo (C 1-C 12) alkoxyl group;
(b31) halo (C 2-C 12) alkene oxygen base;
(b32) halo (C 2-C 12) alkynyloxy group;
(b33) halo (C 3-C 12) cycloalkyl oxy, wherein said cycloalkyl can condense with phenyl ring;
(b34) (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b35) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkoxyl group;
(b36) (C 1-C 6) alkoxyl group (C 1-C 6) alkyl;
(b37) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b38) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b39) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkoxyl group;
(b41) (C 1-C 12) alkylthio;
(b42) (C 2-C 12) alkenylthio group;
(b43) (C 2-C 12) the alkynes sulfenyl;
(b44) (C 3-C 12) the cycloalkyl sulfenyl;
(b45) halo (C 1-C 12) alkylthio;
(b46) halo (C 2-C 12) alkenylthio group;
(b47) halo (C 2-C 12) the alkynes sulfenyl;
(b48) halo (C 3-C 12) the cycloalkyl sulfenyl;
(b49) (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b50) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkylthio;
(b51) (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b52) halo (C 1-C 6) alkoxyl group (C 1-C 6) alkylthio;
(b53) (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b54) halo (C 1-C 6) halogenated alkoxy (C 1-C 6) alkylthio;
(b55) (C 1-C 12) the alkyl sulfinyl;
(b56) (C 2-C 12) the thiazolinyl sulfinyl;
(b57) (C 2-C 12) the alkynyl sulfinyl;
(b58) (C 3-C 12) the cycloalkyl sulfinyl;
(b59) halo (C 1-C 12) the alkyl sulfinyl;
(b60) halo (C 2-C 12) the thiazolinyl sulfinyl;
(b61) halo (C 2-C 12) the alkynyl sulfinyl;
(b62) halo (C 3-C 12) the cycloalkyl sulfinyl;
(b63) (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b64) halo (C 3-C 12) cycloalkyl (C 1-C 12) the alkyl sulfinyl;
(b65) (C 1-C 12) alkyl sulphonyl;
(b66) (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b67) (C 2-C 12) the alkynyl alkylsulfonyl;
(b68) (C 3-C 12) the naphthene sulfamide base;
(b69) halo (C 1-C 12) alkyl sulphonyl;
(b70) halo (C 2-C 12) the thiazolinyl alkylsulfonyl;
(b71) halo (C 2-C 12) the alkynyl alkylsulfonyl;
(b72) halo (C 3-C 12) the naphthene sulfamide base;
(b73) (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b74) halo (C 3-C 12) cycloalkyl (C 1-C 12) alkyl sulphonyl;
(b75) aryl;
(b76) have 1~5 identical or different substituent aryl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b79) aryloxy;
(b80) have 1~5 identical or different substituent aryloxy, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b81) aryloxy (C 1-C 6) alkyl;
(b82) has 1~5 identical or different substituent aryloxy (C 1-C 6) alkyl, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 1-C 6) alkyl sulfinyl, (s) halo (C 1-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b83) arylthio;
(b84) have 1~5 identical or different substituent arylthio, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b85) pyridyl oxygen base;
(b86) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl oxygen base in alkyl, (d) cyanic acid and (e) nitro;
(b87) pyridyl sulfenyl;
(b88) have identical or different being selected from (a) halogen atom, (b) (C 1-C 6) alkyl, (c) halo (C 1-C 6) 1~4 substituent pyridyl sulfenyl in alkyl, (d) cyanic acid and (e) nitro;
(b89) halo (C 1-C 6) alkylenedioxy group;
(b90) (C 1-C 6) alkoxyl group (C 1-C 6) alkoxyl group;
(b93) three (C 1-C 12) the alkyl silyloxy, wherein said alkyl can be identical or different;
(b94) three (C 1-C 12) alkyl silyl (C 1-C 6) alkoxyl group, wherein said alkyl can be identical or different;
(b95) two (C 1-C 12) halogenated alkyl (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b96) two (C 1-C 12) alkyl (C 1-C 6) alkylthio (C 1-C 6) the alkyl silyl, wherein said alkyl can be identical or different;
(b99) two (C 1-C 12) the alkyl phenyl silyl, wherein said alkyl can be identical or different;
(b100) (C 1-C 6) alkylthio (C 1-C 6) alkoxyl group;
(b101) (C 1-C 6) alkyl sulfinyl (C 1-C 6) alkoxyl group;
(b102) (C 1-C 6) alkyl sulphonyl (C 1-C 6) alkoxyl group;
(b106) aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation;
(b107) has 1~5 identical or different substituent aryl (C 1-C 6) alkoxyl group, wherein said alkoxyl group part can be by halogenation, and said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) (C 1-C 6) alkyl, (e) halo (C 1-C 6) alkyl, (f) (C 1-C 6) alkoxyl group, (g) halo (C 1-C 6) alkoxyl group, (h) (C 2-C 6) alkene oxygen base, (i) halo (C 2-C 6) alkene oxygen base, (j) (C 2-C 6) alkynyloxy group, (k) halo (C 2-C 6) alkynyloxy group, (l) (C 3-C 6) cycloalkyl oxy, (m) halo (C 3-C 6) cycloalkyl oxy, (n) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (o) halo (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (p) (C 1-C 6) alkylthio, (q) halo (C 1-C 6) alkylthio, (r) (C 2-C 6) alkyl sulfinyl, (s) halo (C 2-C 6) alkyl sulfinyl, (t) (C 1-C 6) alkyl sulphonyl, (u) halo (C 1-C 6) alkyl sulphonyl, (v) N (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition, (w) N (R 3) COR 4Group, wherein R 3And R 4Like above-mentioned definition, (x) N (R 3) CO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (y) N (R 3) SO 2R 4Group, wherein R 3And R 4Like above-mentioned definition, (z) COR 3Group, wherein R 3Like above-mentioned definition, (aa) CO 2R 3Group, wherein R 3Like above-mentioned definition, (bb) CON (R 3) R 4Group, wherein R 3And R 4Like above-mentioned definition and (cc) C (R 3) NOR 4Group, wherein R 3And R 4Like above-mentioned definition;
(b111) three (C 1-C 12) alkyl silyl (C 1-C 6) alkylthio, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b112) three (C 1-C 12) alkyl silyl (C 1-C 6) the alkyl sulfinyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b113) three (C 1-C 12) alkyl silyl (C 1-C 6) alkyl sulphonyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different;
(b114) R 3(R 4) N (C 1-C 6) alkyl, wherein R 3And R 4Like above-mentioned definition;
(b115) heterocyclic radical;
(b116) have 1~5 identical or different substituent heterocyclic radical, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like definition, (t) (C in the claim 1 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b117) heterocyclic oxy group except that pyridyl oxygen base;
(b118) have 1~5 identical or different substituent heterocyclic oxy group except that pyridyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b125) heterocycle (C 1-C 6) alkyl oxy;
(b126) have 1~5 identical or different substituent Heterocyclylalkyl oxygen base, said substituting group is selected from: (a) halogen atom, (b) cyanic acid, (c) nitro, (d) formyl radical, (e) (C 1-C 6) alkyl, (f) halo (C 1-C 6) alkyl, (g) (C 1-C 6) alkoxyl group, (h) halo (C 1-C 6) alkoxyl group, (i) (C 3-C 6) cycloalkyl (C 1-C 6) alkoxyl group, (j) (C 1-C 6) alkylthio, (k) halo (C 1-C 6) alkylthio, (l) (C 1-C 6) alkyl sulfinyl, (m) halo (C 1-C 6) alkyl sulfinyl, (n) (C 1-C 6) alkyl sulphonyl, (o) halo (C 1-C 6) alkyl sulphonyl, (p) (C 1-C 6) alkyl-carbonyl, (q) carboxyl, (r) (C 1-C 6) alkoxy carbonyl, (s) R 3(R 4) N carbonyl, wherein R 3And R 4Like above-mentioned definition, (t) (C 2-C 6) alkynyl, (u) three (C 1-C 6) alkyl silyl (C 1-C 6) alkyl, wherein said three (C 1-C 6) alkyl in the alkyl silyl can be identical or different, (v) three (C 1-C 6) alkyl silyl (C 2-C 6) alkynyl, wherein said alkyl can be identical or different and (w) oxo group;
(b127) (C 1-C 12) alkyl (C 3-C 12) cycloalkyl; Or
(b128) halo (C 1-C 12) alkyl (C 3-C 12) cycloalkyl.
5. salt, garderning pesticide, its pyrimidine derivatives or its salt that contains in the with good grounds claim 1~4 each is as the effective constituent salt, garderning pesticide.
6. the method for use of salt, garderning pesticide, this method comprise that the effective constituent of using according to the salt, garderning pesticide of claim 5 handles plant or soil.
According to each pyrimidine derivatives or its salt in the claim 1~4 as the application of salt, garderning pesticide.
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