- Aryl sulfide containing benzylamine structure and synthesis method and application thereof
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The invention belongs to the technical field of pesticides, and particularly relates to aryl sulfide containing a benzylamine structure and a synthesis method and application of the aryl sulfide. Represented by the following compounds: or an agriculturall
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Paragraph 0165-0169
(2020/11/05)
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- NOVEL BENZYLAMIDE COMPOUND, METHOD FOR PRODUCING THE SAME, AND MITICIDE
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An object of the present invention is to provide a benzylamide compound or a salt thereof that controls a mite. The present invention provides a benzylamide compound represented by Formula (1): or a salt thereof, wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 and R3 are identical or different and each represent hydrogen, halogen, cyano, nitro, C1-6 alkyl, or the like; R4 represents hydrogen, formyl, C1-6 alkyl, or the like; R5 and R6 are identical or different and each represent hydrogen, halogen, or C1-6 alkyl, or the like; R7, R8, R9, R10, and R11 are identical or different and each 5 represent hydrogen, halogen, or the like; X represents oxygen or sulfur; and n represents an integer of 0 to 2.
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Page/Page column 50
(2018/02/17)
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- NOVEL BENZYLAMIDE COMPOUND, METHOD FOR PRODUCING THE SAME, AND MITICIDE
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An object of the present invention is to provide a benzylamide compound or a salt thereof that controls a mite. The present invention provides a benzylamide compound represented by Formula (1): or a salt thereof, wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 and R3 are identical or different and each represent hydrogen, halogen, cyano, nitro, C1-6 alkyl, or the like; R4 represents hydrogen, formyl, C1-6 alkyl, or the like; R5 and R6 are identical or different and each represent hydrogen, halogen, or C1-6 alkyl, or the like; R7, R8, R9, R10, and R11 are identical or different and each represent hydrogen, halogen, or the like; X represents oxygen or sulfur; and n represents an integer of 0 to 2.
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Page/Page column 60; 61
(2018/02/28)
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- NOVEL AMIDE COMPOUND, METHOD FOR PRODUCING THE SAME, AND MITICIDE
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An object of the present invention is to provide an amide compound or a salt thereof that controls a mite. The present invention provides an amide compound represented by Formula (1) : or a salt thereof, wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 and R3 are identical or different and each represent hydrogen, halogen, cyano, nitro, C1-6 alkyl, or the like; Q represents Q-1 or Q-2: R4 represents hydrogen, C1-6 alkyl, acetyl or the like; R5 and R6 are identical or different and each represent hydrogen, halogen, or C1-6 alkyl, or the like; HET represents 5- or 6-membered heteroaryl, R7 represents C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, C3-8 cycloalkyl C1-6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryl C1-6 alkyl X represents oxygen or sulfur; and n represents an integer of 0 to 2.
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Page/Page column 79
(2018/04/14)
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- Synthesis of 2-methylbenzoxazoles directly from: N -phenylacetamides catalyzed by palladium acetate
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A method to synthesize 2-methylbenzoxazoles directly from N-phenylacetamides catalyzed by Pd(OAc)2 in the presence of K2S2O8 and TfOH has been developed. The desired products were obtained in moderate to excellent yields. This approach provides a facile procedure to prepare benzoxazoles with available substrates. It is found that TfOH is the key factor for this cyclization reaction. A plausible mechanism of the reaction is proposed according to the control reactions and the literature.
- Wang, Biying,Jiang, Chengfei,Qian, Jiasheng,Zhang, Shuwei,Jia, Xiaodong,Yuan, Yu
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p. 101 - 107
(2017/12/27)
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- Amide-assisted radical strategy: Metal-free direct fluorination of arenes in aqueous media
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A metal- and initiator-free direct fluorination of arenes with the assistance of an amide group is developed. This reaction proceeded under simple aqueous conditions with good functional group tolerance and ortho-para selectivity, and is highly practical because it could be readily scaled up to a multigram-scale. At this stage, an exclusive mechanism could not be proposed, and several possibilities have been discussed. The possibility of the amide-assisted radical chain mechanism has been supported by experimental and computational investigations as well as a seminal work.
- Liang, Deqiang,Li, Yanni,Gao, Shulin,Li, Renlun,Li, Xiangguang,Wang, Baoling,Yang, Hai
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supporting information
p. 3344 - 3349
(2017/07/28)
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- Regioselective and efficient bromination of anilides on water using HBr and Selectfluor
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A metal-, additive-, and Br2-free highly regioselective bromination of anilides using HBr and Selectfluor is presented. This reaction proceeded under mild conditions with high efficiency and good functional group tolerance, and water served as the solvent. In general, with substrates bearing no para-substituent, para-mono-bromination occurred exclusively, while ortho-mono-brominated anilides were the only products when para-positions were blocked. The incorporation of a stronger orienting group might result in a reversed regioselectivity, and the reaction was sensitive to steric hindrance.
- Liang, Deqiang,Li, Xiangguang,Wang, Chaowu,Dong, Qishan,Wang, Baoling,Wang, Hai
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p. 5390 - 5394
(2016/11/11)
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- INSECTICIDAL ACTIVE MIXTURES COMPRISING ARYLQUINAZOLINONE COMPOUNDS
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Pesticidal active mixtures comprising arylquinazolinone compounds The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I) wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one active compound II selected from a group M comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, allosteric nicotinic acetylcholine receptor activitaors, chloride channel activators, juvenile hormone mimics, homopteran feeding blockers, mit grow inhibitors, inhibitors of mitochondrial bATP synthase, uncouplers of the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, ecdyson receptor agonists, octamin receptor agonists, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis, ryanodine receptor modulators and other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating and controlling insects, arachnids or nematodes in and on plants, and for protecting such plants being infested with pests, especially also for protecting plant proparagation material, such as seeds.
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Page/Page column 51
(2013/03/28)
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- USE OF PESTICIDAL ACTIVE 3-ARYLQUINAZOLIN-4-ONE DERIVATIVES IN SOIL APPLICATION METHODS
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PF72171 60 Abstract Use of pesticidal active 3-arylquinazolin-4-one derivatives in soil application methods The present invention relates to agricultural methods and the use of 3-arylquinazolin-4-5 one derivatives of formula (I) N N O S(O) n R 1 R 3 R 2 (R 4 ) k (I) wherein R1, R2, R3, R4, k and n are defined in the description in soil application methods.10 The compounds of the formula (I) are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection. 15
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Page/Page column 45
(2013/03/28)
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- AGRICULTURAL MIXTURES COMPRISING ARYLQUINAZOLINONE COMPOUNDS
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The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I): wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.
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Page/Page column 60
(2013/03/28)
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- 3-ARYLQUINAZOLIN-4-ONE COMPOUNDS FOR COMBATING INVERTEBRATE PESTS
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The present invention relates to the 3-arylquinazolin-4-one compounds of the formula (I) and the salts thereof, formula (I) wherein n is O, 1 or 2; X is O, S or N-R4; Y1 is N or CH; Y2 is N or C-R5; R1/sup
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Page/Page column 70
(2010/09/18)
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- Octahydropyrrolo[3,4-C]pyrrole derivatives
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The present invention relates to octahydropyrrolo[3,4-c]pyrrole derivatives of formula (I): and to processes for the preparation thereof, compositions containing the same and the uses thereof.
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Page/Page column 13
(2010/11/08)
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- A highly effective nonpolar isostere of deoxyguanosine: synthesis, structure, stacking, and base pairing.
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We describe the preparation and structure of the deoxyribonucleoside of 4-fluoro-6-methylbenzimidazole, abbreviated dH (8), which acts as a close shape mimic of the nucleoside deoxyguanosine. The nucleoside is prepared from 2-fluoro-4-methylaniline in seven steps. The X-ray crystal structure reveals a (-sc) glycosidic orientation, an S conformation for the deoxyribose moiety, and quite close shape mimicry of guanine by the substituted benzimidazole. Conformational studies by (1)H NMR and (1)H-(1)H ROESY experiments reveal an S-type conformation and an anti glycosidic orientation in solution (D(2)O), essentially the same as that of deoxyguanosine. Base-stacking studies in a "dangling end" context reveal that the benzimidazole base mimic stacks more strongly than all four natural bases, and more strongly than its counterpart guanine by 1.1 kcal/mol. Base-pairing studies in a 12mer DNA duplex show that, like other nonpolar nucleoside isosteres, H is destabilizing and nonselective when paired opposite natural bases. However, when paired opposite another nonpolar isostere, difluorotoluene (F), a mimic of thymine, the pair exhibits stability approaching that of its natural analogue, a G-T (wobble) base pair. The nucleoside analogue dH will be useful in studies of protein-DNA interactions, and the H-F base pair will serve as a structurally and thermodynamically close mimic of G-T in studies of DNA mismatch repair enzymes.
- O'Neill, Bryan M,Ratto, Jessica E,Good, Kristi L,Tahmassebi, Deborah C,Helquist, Sandra A,Morales, Juan C,Kool, Eric T
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p. 5869 - 5875
(2007/10/03)
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- Substituent modulation of mild fluorination of aromatic molecules with caesium fluoroxysulphate
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Functionalization of mono- and di-substituted benzene derivative with CsSO4F has been modulated by substituents on the benzene ring. α-Hydroxyalkylbenzenes, with a deactivated ring, were oxidized to phenones, while fluorodealkylation was achieved in high yield when electron-donating groups were present in a para position. Electron-withdrawing substituents favoured chain fluorofunctionalization in alkylbenzenes, while ring fluorination was found exclusively in acylamino-derivatized alkylbenzenes; fluoro-addition products were formed in the case of p-alkoxy-substituted alkylbenzene derivatives.
- Stavber, Stojan,Planinsek, Zdenka,Kosir, Iztok,Zupan, Marko
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p. 409 - 412
(2007/10/02)
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- A Novel Electrophilic Fluorination of Activated Aromatic Rings Using Acetyl Hypofluorite, Suitable also for Introducing (18)F into Benzene Nuclei
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Acetyl hypofluorite (1) is a new compound that serves as a novel electrophilic fluorinating agent.It is special in the sense that, while it is very reactive, it is still a milder reagent than other fluoroxy compounds such as CF3OF or CF3COOF.It is synthesized directly from elemental fluorine and is used without any isolation or purification.The hypofluorite 1 reacts efficiently and selectively with activated aromatic rings,particularly phenol and aniline derivatives after suitable protection of the hydroxyl and the amino groups.The net result of the reaction is partly according to classical aromatic electrophilic substitution.Unlike such a substitution, however, the electrophilic fluorine atom of 1 substitutes mainly an ortho hydrogen and only occasionally small amounts of p-fluoro derivatives are found.Evidence supports the mechanism for this aromatic fluorination as being mainly an addition-elimination one.In many cases the electrophilic aromatic fluorinations can replace the classical 60-year-old Balz-Schiemann method, which until today is probably the most used procedure.Since aromatic fluorination with 1 is a very fast reaction and since 1 is produced directly from elemental fluorine, this is probably one of the best ways for introduction of the short-living radioisotope (18)F into activated aromatic rings.This will greatly encourage the synthesis of compounds suitable for use in the rapidly developing field of positron emitting transaxial tomography, which in itself depends on the efficient and easy supply of compounds possessing positron emitting isotopes.
- Lerman, Ori,Yitzhak, Tor,Hebel, David,Rozen, Shlomo
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p. 806 - 813
(2007/10/02)
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