- Novel trifluoromethylpyrazole acyl urea derivatives: Synthesis, crystal structure, fungicidal activity and docking study
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Thirteen novel trifluoromethylpyrazole acyl urea derivatives were designed and synthesized. In vivo fungicidal activities of these compounds were tested against Fusarium oxysporum, Corynespora mazei, Botrytis cinerea and Pseudomonas syringae respectively, particularly compounds exhibited significant control effective at 100 mg/L. More importantly, some compounds showed the good control effective at 10 mg/L. Furthermore, docking was established to study the structure-activity relationship of the title compounds. It is possible that trifluoromethylpyrazole acyl urea derivatives, which possess good control effective against Fusarium oxysporum, Corynespora mazei and Botrytis cinerea, may become novel lead compounds for the development of fungicides with further structure modification.
- Wang, Han,Zhai, Zhi-Wen,Shi, Yan-Xia,Tan, Cheng-Xia,Weng, Jian-Quan,Han, Liang,Li, Bao-Ju,Liu, Xing-Hai
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- Synthesis and antifungal activity of the derivatives of novel pyrazole carboxamide and isoxazolol pyrazole carboxylate
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A series of pyrazole carboxamide and isoxazolol pyrazole carboxylate derivatives were designed and synthesized in this study. The structures of the compounds were elucidated based on spectral data (infrared, proton nuclear magnetic resonance and mass spectroscopy). Then, all of the compounds were bioassayed in vitro against four types of phytopathogenic fungi (Alternaria porri, Marssonina coronaria, Cercospora petroselini and Rhizoctonia solani ) using the mycelium growth inhibition method. The results showed that some of the synthesized pyrazole carboxamides displayed notable antifungal activity. The isoxazole pyrazole carboxylate 7ai exhibited significant antifungal activity against R. solani, with an EC50 value of 0.37 μg/mL. Nonetheless, this value was lower than that of the commercial fungicide, carbendazol.
- Sun, Jialong,Zhou, Yuanming
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- Expedient discovery for novel antifungal leads targeting succinate dehydrogenase: Pyrazole-4-formylhydrazide derivatives bearing a diphenyl ether fragment
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The pyrazole-4-carboxamide scaffold containing a flexible amide chain has emerged as the molecular skeleton of highly efficient agricultural fungicides targeting succinate dehydrogenase (SDH). Based on the above vital structural features of succinate dehydrogenase inhibitors (SDHI), three types of novel pyrazole-4-formylhydrazine derivatives bearing a diphenyl ether moiety were rationally conceived under the guidance of a virtual docking comparison between bioactive molecules and SDH. Consistent with the virtual verification results of a molecular docking comparison, the in vitro antifungal bioassays indicated that the skeleton structure of title compounds should be optimized as an N′-(4-phenoxyphenyl)-1H-pyrazole-4-carbohydrazide scaffold. Strikingly, N′-(4-phenoxyphenyl)-1H-pyrazole-4-carbohydrazide derivatives 11o against Rhizoctonia solani, 11m against Fusarium graminearum, and 11g against Botrytis cinerea exhibited excellent antifungal effects, with corresponding EC50 values of 0.14, 0.27, and 0.52 μg/mL, which were obviously better than carbendazim against R. solani (0.34 μg/mL) and F. graminearum (0.57 μg/mL) as well as penthiopyrad against B. cinerea (0.83 μg/mL). The relative studies on an in vivo bioassay against R. solani, bioactive evaluation against SDH, and molecular docking were further explored to ascertain the practical value of compound 11o as a potential fungicide targeting SDH. The present work provided a non-negligible complement for the structural optimization of antifungal leads targeting SDH.
- Chen, Min,Li, Guohua,Lu, Aimin,Qiu, Lingling,Wang, An,Wang, Xiaobin,Xue, Wei,Yang, Chunlong
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- Preparation method and application of -4- (S)-2-(1H- pyrazolecarboxamide)-P-methylbenzoate compound as well as preparation method and application thereof (by machine translation)
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The invention discloses (S)- 2 - (1 a system. H-pyrazol-4 (propyl-formamide)-based) propyl benzoate compound as well as preparation method, (S)- 2 - (1 and application thereofHThe structural formula of the-pyrazol-4-formamide)-based ethyl (I) benzoate compound is shown in a formula shown: in the specification. Substituent groups R in the (I) formula (No.No. STR3No.No., No.No. STR7No.No.No.). 1 The number of substituents on the, phenyl ring, which is a phenyl group or a substituted phenyl group, is, each independently selected from the group consisting of one, C1 - C4 or, more, C1 - C4 substituents, C1 - C3 each; of which R is independently selected from the group consisting of a halogen atom, an alkyl group, an alkyl group, an alkyl group, and a substituted phenyl group. 2 The preparation method of the novel compound with the. bactericidal activity is simple, and the compound obtained by the method, disclosed by the invention, is simple, in preparation method, 50mg/mL and the compound obtained by, the method disclosed by the invention has a good inhibition activity on. cucumber Botrytis cinerea and pathogenic bacteria such as cucumbers. (by machine translation)
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Paragraph 0080; 0083; 0084
(2020/02/14)
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- OXIDATION OF A PYRAZOLYL KETONE COMPOUND TO THE CORRESPONDING CARBOXYLIC ACID
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This invention concerns a process for the manufacture of carboxylic acids or carboxylic acid derivatives and a process for the manufacture of agrochemically and pharmaceutically active compounds comprising the process for the manufacture of carboxylic acids or their derivatives. The process for the manufacture of carboxylic acids or carboxylic acid derivatives of formula (II) comprises a step of oxidizing a compound of formula (I) in the presence of at least one compound of formula (III) R6-C(O)O-OH. (I) (II)
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Page/Page column 13
(2019/06/23)
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- Novel trifluoromethylpyrazole acyl thiourea derivatives: Synthesis, antifungal activity and docking study
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Background: In recent years, pyrazole carboxamide derivatives possessed excellent fungicidal activity. In the process of designing new fungicides, the carboxamide group was modified in order to find novel structure pyrazole carboxamide derivatives. Methods: Ten novel trifluoromethyl pyrazole acyl thiourea derivatives were designed and synthesized. In vivo fungicidal activities of these compounds were tested against Fusarium oxysporum, Corynespora mazei and Botrytis cinerea, respectively Results: Particularly compounds exhibited significant control effective at 100 mg/L. More importantly, some compounds showed the good control effective at 10 mg/L. Furthermore, docking was established to study the structure-activity relationship of the title compounds. Conclusion: It is possible that trifluoromethylpyrazole acyl thiurea derivatives, which possess good control effective against Botrytis cinerea, may become novel lead compounds for the development of fungicides with further structure modification.
- Wang, Han,Zhai, Zhi-Wen,Shi, Yan-Xia,Tan, Cheng-Xia,Weng, Jian-Quan,Han, Liang,Li, Bao-Ju,Liu, Xing-Hai
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p. 785 - 791
(2019/08/26)
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- (1H-pyrazole-4-carboxamido) ethyl benzoate compound as well as preparation method and application thereof
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The invention discloses an ethyl (1H-pyrazole-4-carboxamido) benzoate compound as well as a preparation method and application thereof. The structural formula of the (1H-pyrazole-4-carboxamido) ethylbenzoate compound is as shown in the formula (I), wherein the substituent groups R1 are phenyl or substituted phenyl, the number of substituent groups on a benzene ring of the substituted phenyl is one or more, and each substituent group is independently selected from H, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C3 halogenated alkyl or nitro; and the substituent R2 is methyl, monofluoromethyl, difluoromethyl or trifluoromethyl. The invention discloses a novel compound with bactericidal activity, which is simple in preparation method and convenient to operate, and the obtained compound has betterinhibitory activity on pathogenic bacteria such as cucumber botrytis cinerea, fusarium oxysporum, cucumber corynespora leaf spot and the like under the concentration of 50 mg/mL.
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- METHOD FOR THE PREPARATION OF 3-FLUOROALKYL-1-METHYLPYRAZOL-4-CARBOXYLIC ACID
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The present invention relates to method for the preparation of 3-fluoroalkyl-1-methylpyrazol-4-carboxylic acid, wherein it comprises the following steps: step 1, fluoroacetyl fluoride derivative shown in Formula I undergoes condensation with dimethylamino vinyl methyl ketone, as a result, 3-dimethylamino methylene-fluoro-2,4-pentanedione derivative shown in Formula II is formed; step 2, ring closing reaction takes place between said 3-dimethylamino methylene-fluoro-2,4-pentanedione shown in Formula II and methylhydrazine, in this way, 3-fluoroalkyl-1-methyl-4-acetyl pyrazol derivative shown in Formula III is obtained; step 3, the said 3-fluoroalkyl-1-methyl-4-acetyl pyrazol derivative shown in Formula III is oxidized in the presence of alkali, and then acidified, in this way, 3-fluoroalkyl-1-methylpyrazol-4-carboxylic acid shown in Formula IV is formed. Preparing method of present invention, wherein the required preparing route is simple, the raw material cost is low, the resulting yield of each step is high, and it is suitable for industrialization.
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- 1-methyl-3-trifluoromethyl-1H-pyrazol-4-amide derivative as well as preparation method and application thereof
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The invention discloses a 1-methyl-3-trifluoromethyl-1H-pyrazol-4-amide derivative as well as a preparation method and application thereof. Ethyl trifluoroacetoacetate and triethyl orthoformate are subjected to reflux in acetic anhydride; then, the materials are added into methyl hydrazine to prepare ethyl 1-methyl-3-trifluoromethyl-1H-pyrazol-4-formate; the ethyl 1-methyl-3-trifluoromethyl-1H-pyrazol-4-formate is hydrolyzed; then, hydrochloric acid is added to prepare 1-methyl-3-trifluoromethyl-1H-pyrazol-4-carboxylic acid; after the 1-methyl-3-trifluoromethyl-1H-pyrazol-4-carboxylic acid reacts with thionyl chloride, methylene dichloride is added for dilution; alkarylamine and triethylamine are added for preparing the 1-methyl-3-trifluoromethyl-1H-pyrazol-4-amide derivative. The preparation method is simple; the operation is convenient; the obtained compound has the best inhibition activity on peanut cercospora arachidicola and sclerotinia sclerotiorum at 50ppm; the inhibition rate respectively reaches 96 percent and 100 percent; the inhibition rate on the physalospora piricola is high; the inhibition rate is not less than 10 percent higher than the control medicine bacterium inhibition rate; the foundation is laid for new pesticide invention and development.
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Paragraph 0024; 0032; 0035-0036
(2018/06/15)
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- Application of 1-methyl-3-trifluoromethyl-1H-pyrazole-4-amide derivative in preparation of herbicides
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The invention discloses application of a 1-methyl-3-trifluoromethyl-1H-pyrazole-4-amide derivative in preparation of herbicides. The seeds of lettuce and agrostis are taken as the test objects, beforebiological determination, a 5-10% Chlorox solution is employed for surface sterilization on the seeds for 10min, and then the deionized water of a Millipore system is utilized for flushing thoroughly, air drying is carried out in a sterile environment, and during sample treatment, all samples adopt acetone as the solvent to prepare a solution with a concentration of 1mM, and then biological determination is carried out to conclude that the compound tested in the invention shows good inhibition on lettuce and agrostis. The compound provided by the invention is a new compound with herbicidal activity, and provides the basis for the research and development of new pesticides.
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Paragraph 0013; 0016; 0017
(2018/11/22)
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- Preparation method of 3-fluoroalkyl-1-methylpyrazol-4-carboxylic acid
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The invention relates to a preparation method of 3-fluoroalkyl-1-methylpyrazol-4-carboxylic acid. The method comprises the following steps: step 1, making a fluoroacetyl halide derivative shown in the formula I and dimethylamino vinyl methyl ketone to undergo a condensation reaction to generate a 3-dimethylamino methylene-1,1-difluoro-2,4-pentanedione derivative shown in the formula II; step 2, reacting the 3-dimethylamino methylene-1,1-difluoro-2,4-pentanedione derivative shown in the formula II with methylhydrazine for a ring-closing reaction to generate a 3-fluoroalkyl-1-methyl-4-acetyl pyrazole derivative shown in the formula III; and step 3, oxidizing the 3-fluoroalkyl-1-methyl-4-acetyl pyrazole derivative shown in the formula III in an alkaline condition, and performing acidification to generate 3-fluoroalkyl-1-methylpyrazol-4-carboxylic acid. The preparation method is short in reaction route, low in raw material cost, high in reaction yield of each step, and suitable for industrial production.
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Paragraph 0084; 0085
(2017/08/28)
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- Containing 1 - methyl - 3 - trifluoromethyl - 1 H - pyrazole structure of acyl thiourea compound and its preparation method and application (by machine translation)
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The invention discloses a containing 1 - methyl - 3 - trifluoromethyl - 1 H - pyrazole acyl thiourea compound and its preparation method and application. It first of all in order to trifluoro acetyl ethyl acetate and ethyl trimethyl orthoformate and methyl hydrazine as raw material synthesis 1 - methyl - (trifluoromethyl) - 1 H - pyrazole - 4 - carboxylic acid, the latter acid radical chloride to obtain 1 - methyl - (trifluoromethyl) - 1 H - pyrazole - 4 - formyl chloride, potassium cyanide and subsequently and sulfur substituted aniline reaction to obtain the final product (I). Its raw material is simple and easy, simple preparation method, after treatment is convenient, high product yield, but the compound as having anti-fungal activity, in particular against cucumber, cucumber bacterial angle the blood, cucumber gray mold and cucumber leafspot has good sterilization effect, to provide the basis for a new pesticide research. (by machine translation)
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- Acyl urea compound containing 1-methyl-3-trifluoromethyl-1H-pyrazole structure and preparation method and application thereof
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The invention discloses an acyl urea compound containing a 1-methyl-3-trifluoromethyl-1H-pyrazole structure and a preparation method and application thereof. The preparation method comprises the following steps: firstly using ethyl trifluoroacetoacetate, triethyl orthoformate and methylhydrazine as raw materials to synthesize 1-methyl-(trifluoromethyl)-1H-pyrazole-4-formic acid, performing the amidation to obtain 1-methyl-(trifluoromethyl)-1H-pyrazole-4-formamide, and reacting with oxalyl chloride and substituted anilines to obtain a final product (I). The raw materials are simple and are easily obtained, the preparation method is simple, the aftertreatment is convenient, and the product yield is high. The compound has the antifungal activity, and has the good sterilizing effect in allusion to cucumber fusarium wilt, cucumber bacterial angular leaf spot, cucumber gray mold and cucumber target leaf spot especially. The foundation is provided for new pesticide research and development.
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- Trifluoromethyl-containing pyrazolecarboxamide compounds as well as preparation method and application thereof
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The invention discloses trifluoromethyl-containing pyrazolecarboxamide compounds as well as a preparation method and application thereof. The compounds are N-substituted-(1-methyl-3-trifluoromethyl-1H-pyrazole-4-yl) amide compounds and are also novel compounds with nematicidal activity. The compounds are particularly used for preventing and controlling meloidogyne incognita and the like and provide a basis for researching and developing novel pesticides.
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- Preparation method for polyfluoromethylpyrazole compound, and intermediate of compound and preparation method thereof
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The invention discloses a preparation method for a polyfluoromethylpyrazole compound, and an intermediate of the compound and a preparation method thereof. The invention provides a preparation method for a compound 1 as defined in the specification. The preparation method comprises a step of subjecting a compound 2 as defined in the specification and methylhydrazine to a ring-closure reaction in an organic solvent so as to obtain the compound 1, wherein R is a C1-4 alkyl group, R is a methyl or ethyl group and x is 2 or 3. The preparation method provided by the invention uses cheap and easily available raw materials and is mild in reaction conditions, safe to operate, environment friendly, low in production cost, high in reaction conversion rate, low in the content of isomer in by-products, high in reaction yield and product purity and suitable for industrial production.
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Paragraph 0215; 0216; 0217
(2017/06/30)
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- Use of a Traceless Activating and Directing Group for the Construction of Trifluoromethylpyrazoles: One-Pot Transformation of Nitroolefins and Trifluorodiazoethane
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We disclose an efficient one-pot transformation of trifluorodiazoethane and higher perfluorinated homologues with various nitroolefins. This method takes advantage of the nitro group as a traceless activating and directing group (TADG) that is released in the aromatization step to produce 4-substituted 3-perfluoroalkyl pyrazoles with complete regioselectivity. The potential of this method is further demonstrated by the synthesis of penthiopyrad.
- Chen, Zhen,Zheng, Yan,Ma, Jun-An
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supporting information
p. 4569 - 4574
(2017/04/11)
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- Method of manufacturing pyrazolecarboxylic compd.
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PROBLEM TO BE SOLVED: To provide 1,3-disubstituted pyrazole-4-carboxylic acid obtained by reducing the content of isomers from 1,3-disubstituted pyrazole-4-carboxylic acid containing 1,5-disubstituted pyrazole-4-carboxylic acid (the isomer). SOLUTION: The production method of 1,3-disubstituted pyrazole-4-carboxylic acid comprises: preparing an aqueous solution including 1,3-disubstituted pyrazole-4-carboxylate, 1,5-disubstituted pyrazole-4-carboxylate and an organic solvent; and making the pH of this aqueous solution to the pH range where the 1,3-disubstituted pyrazole-4-carboxylic acid precipitates. COPYRIGHT: (C)2013,JPOandINPIT
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Paragraph 0041
(2016/12/26)
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- Synthesis and antifungal activity of n-(substituted pyridinyl)- 1-methyl(phenyl)-3-(trifluoromethyl)-1h-pyrazole-4- carboxamide derivatives
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A series of N-(substituted pyridinyl)-1-methyl(phenyl)-3-trifluoromethyl- 1Hpyrazole- 4-carboxamide derivatives were synthesized. All target compounds were characterized by spectral data (1H-NMR, 13C-NMR, IR, MS) and elemental analysis and were bioassayed in vitro against three kinds of phytopathogenic fungi (Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica). The results showed that some of the synthesized N-(substituted pyridinyl)-1-methyl-3- trifluoromethyl-1H-pyrazole-4-carboxamides exhibited moderate antifungal activities, among which compounds 6a, 6b and 6c displayed more than 50% inhibition activities against G. zeae at 100 μg/mL, which was better than that of the commercial fungicides carboxin and boscalid.
- Wu, Zhibing,Hu, Deyu,Kuang, Jiqing,Cai, Hua,Wu, Shixi,Xue, Wei
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p. 14205 - 14218
(2013/02/26)
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- Method for the Production of Halogen-Substituted 2-(aminomethylidene)-3-oxobutyric Acid Esters
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The present invention relates to a process for preparing 2-(aminomethylidene)-4,4-dihalo-3-oxobutyric esters of the formula (I), wherein R1, R2, R3 are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl, and/or R2 together with R3 and the nitrogen atom to which the two radicals are attached are a heterocyclic radical, in which a corresponding 3-aminoacrylic ester is reacted with a halogen-substituted acetyl fluoride in the presence of at least one alkali or alkaline earth metal fluoride; and the further conversion of halogen-substituted 2-(aminomethylidene)-3-oxobutyric esters of the formula (I) to halomethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.
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(2011/04/14)
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- METHOD FOR PRODUCING FLUORINE-CONTAINING ACYLACETIC ACID DERIVATIVE, METHOD FOR PRODUCING FLUORINE-CONTAINING PYRAZOLECARBOXYLIC ACID ESTER DERIVATIVE, AND METHOD FOR PRODUCING FLUORINE-CONTAINING PYRAZOLECARBOXYLIC ACID DERIVATIVE
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A halogenating agent is added to a mixture including a base, a fluoroalkylcarboxylic acid derivative and an acrylate derivative to produce a fluoroaclyacetic acid derivative represented by the following Formula (3): wherein Rf represents a fluorine containing alkyl group, R1 and R2 represent a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, an arylalkyl grou p or an acyl group, or together represent an atomic group that forms a 5- or 6-memb ered ring containing a nitrogen atom to which R1 and R2 are bonded; R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or an arylalkyl g roup; and R4 represents an alkyl group, a cycloalkyl group, an aryl group, or an aryl alkyl group.
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Page/Page column 21-22
(2011/01/11)
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- FLUORINE-CONTAINING PYRAZOLECARBONITRILE DERIVATIVE AND METHOD FOR PRODUCING THE SAME, AND FLUORINE-CONTAINING PYRAZOLECARBOXYLIC ACID DERIVATIVE OBTAINED BY USING THE FLUORINE-CONTAINING PYRAZOLECARBONITRILE DERIVATIVE AND METHOD FOR PRODUCING THE SAME
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The present invention provides a fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same, and a fluorine-containing pyrazolecarboxylic acid derivative obtained by using the fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same. A fluorine-containing acyacrylonitrile derivative prepared from a fluoroacyl derivative and an aminoacrylonitrile derivative, is reacted with a hydrazine derivative to produce a fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1). In Formula (1), Rf represents an alkyl group having 1 to 6 carbon atoms and substituted with at least one fluorine atom; R1 represents an alkyl group having 1 to 6 carbon atoms and R2 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like. The fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1) is reacted with water to produce a fluorine-containing pyrazolecarboxylic acid derivative.
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(2009/12/23)
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- Switchable reactivity: The site-selective functionalization of trifluoromethyl-substituted pyrazoles
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Modern organometallic methods enable the regioflexible conversion of simple heterocyclic starting materials into families of isomers and congeners. Depending on the choice of the reagent, 1-methyl-5-(trifluoromethyl)pyrazole (1) undergoes deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Similarly, 1-phenyl-5-(trifluoromethyl)pyrazole (5) and 3-methyl-l-phenyl-5-(trifluoromethyl)pyrazole (8) are selectively attacked by lithium diisopropylamide at the heterocyclic 4-position and by butyllithium concomitantly at the 4-position and the ortho position of the phenyl ring. In contrast, metalation of 1-methyl-3-(trifluoromethyl)pyrazole (2) occurs only at the 5-position, whatever the organometallic or metal amide base. Further sites become accessible to functionalization if bromine is introduced into the heterocyclic or aromatic ring. This has been demonstrated with 4-bromo-1-methyl-5-(trifluoromethyl)pyrazole (3), 4-bromo-l-methyl-3-(trifluoromethyl)pyrazole (4), 4-bromo-1-methyl-5-(trifluoromethyl)pyrazole (7) and 1-(2-bromophenyl)-5-(trifluoromethyl)pyrazole (6). Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002.
- Schlosser, Manfred,Volle, Jean-Noel,Leroux, Frederic,Schenk, Kurt
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p. 2913 - 2920
(2007/10/03)
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- Carboxanilides, their preparation and compositions containing them for controlling harmful fungi
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Carboxanilides of the formula I where the substituents have the following meanings: R is substituted or unsubstituted alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxy or phenyl; A is one of the radicals A1 to A5 STR1 where R1 is hydrogen or alkyl; R2 is halogen or alkyl; R3 is alkyl or haloalkyl; n is 1 or 2, methods of manufacturing them, and agents containing them and their use for controlling harmful fungi.
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- FACILE SYNTHETIC METHODS FOR 3- AND 5-TRIFLUOROMETHYL-4-TRIFLUOROACETYLPYRAZOLES AND THEIR CONVERSION INTO PYRAZOLE-4-CARBOXYLIC ACIDS
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3- and 5-Trifluoromethyl-4-trifluoroacetylpyrazoles (4 and 5) were easily synthesized in excellent yields by reaction of β,β-bis(trifluoroacetyl)vinyl ethers 1, sulfides 2, and -amines 3 with hydrazines.Hydrolysis of these compounds (4 and 5) with aqueous potassium hydroxide gave the corresponding pyrazole-4-carboxylic acids (6 and 7) in high yields.
- Okada, Etsuji,Masuda, Ryoichi,Hojo, Masaru
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p. 791 - 798
(2007/10/02)
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