cas 864731-61-3, 4-[(5R)-5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]-2-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]benzamide

Articles about 864731-61-3Total 18 be found

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PROCESS FOR PREPARATION OF ISOXAZOLINE SUBSTITUTED BENZAMIDE COMPOUND
The invention relates to process for the preparation of isoxazoline-substituted benzamide compound and intermediates thereof. The invention also relates to process for the preparation of Fluralaner and intermediates thereof.
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(2022/03/14)

Synthetic method of fluralana
According to the method, 2-methyl-5-bromobenzoic acid is adopted as a raw material, and Suzuki coupling reaction, condensation reaction, dehydration cyclization reaction and amide condensation reaction are performed to finally obtain the fluralan. According to the synthesis method, the reaction cost is reduced, the yield is improved, and the reaction period is shortened.
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(2022/04/15)

Synthesis of fluralaner
The invention relates to synthesis of fluralaner, and the key step of synthesis relates to preparation of the fluralaner through reaction of 4-(5-(3, 5-dichlorophenyl)-5-(trifluoromethyl)-4, 5-dihydroisoxazole-3-yl)-2-methyl-benzonitrile and 2-amino-N-(2, 2, 2-trifluoroethyl) acetamide under the action of Zn(OTf)2/hydroxylamine hydrochloride.
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(2021/10/20)

Fluorine thramine intermediate and method for preparing flumbine by using same
The invention discloses a fluororesonide intermediate and a method for preparing the same, and a fluororesonide intermediate -5. Routes include the use of m-xylene as starting materials, halogenation. Oxidation reaction The intermediate -5 is further obtained by hydroximation, cyanolation, hydrolysis reaction or cyanation, oximation, and hydrolysis reaction. As some examples of the present invention, synthetic routes were increased 2 steps from 5 steps in the prior art, but surprisingly high overall yields were obtained and the purity of intermediate -5 was significantly increased. , The starting material of the intermediate -5 is prepared from high 4 - bromo -2 - methylbenzoic acid to low-priced m-xylene, so that the cost of the intermediate -5 is greatly reduced. , The reaction condition is mild, the synthesis difficulty is low, and the environment is more environmentally friendly.
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(2021/12/07)

Method for preparing fluralana intermediate, prepared intermediate and application of fluralana intermediate
A method for preparing a fluralana intermediate, provided by the invention, comprises the following steps: carrying out nucleophilic addition reaction on 1-(3, 5-dichlorophenyl)-2, 2, 2-trifluoroethanone, carrying out acidolysis, reacting with a Grignard reagent, carrying out oxidation, carrying out oxidation cyclization reaction, reacting with hydroxyl(toluenesulfonyloxy)benzene iodide, and reacting with a trimethoxyphosphorus solution to finally generate the fluralan. In the preparation process, a catalyst and dimethoxy zinc are not needed, ultralow-temperature reaction conditions of -78 DEG C are not needed, operation is easy and convenient, meanwhile, reagents such as ozone and dimethyl sulfide which are harmful to the environment are replaced, and the method is more environmentally friendly. The invention also provides the intermediate for preparing the fluralan.
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(2021/10/05)

PROCESS FOR PURIFICATION OF FLURALANER
The present invention relates to a process for purification of Fluralaner of formula (I). The present invention further relates to a process for purification of Fluralaner of formula (I) with purity more than 99%, in simple, economic and commercially viable manner.
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Paragraph 7; 8

(2021/06/04)

Preparation method of isoxazoline insecticide
The invention relates to a preparation method of an isoxazoline insecticide, which relates to the technical field of chemical industry, and comprises the following steps: 1) coupling reaction: mixingan intermediate 1 with nitromethane in a solvent, adding a palladium catalyst and a ligand to carry out catalytic coupling, reacting, and separating and purifying to obtain an intermediate 2; 2) cyclization reaction: mixing the intermediate 2 and an intermediate 3, adding the mixture into a mixed solution of a dehydrating agent and alkali, carrying out full cyclization reaction, and purifying to obtain an intermediate 4; and 3) condensation reaction: mixing the intermediate 4 and an intermediate 5, adding a condensing agent, carrying out full condensation reaction, and carrying out separationand purification to obtain an isoxazoline compound 6. The method has the advantages of short reaction route, accessible raw materials, fewer three wastes and high purity of the purified product, and is suitable for industrial production.
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Paragraph 0020; 0024; 0025; 0026

(2021/03/11)

PROCESS FOR PREPARING FLURALANER
The invention relates to an improved process for the synthesis of Fluralaner in an efficient and economical way.
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Paragraph 0074-0082

(2021/06/26)

Synthetic method of isoxazoline anthelmintic
The invention belongs to the technical field of chemical drug synthesis, and particularly relates to a synthesis method of an isoxazoline anthelmintic. The method is characterized in that the isoxazoline anthelmintic is fluralaner, and the method includes
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Paragraph 0032; 0039-0048; 0049-0066

(2020/10/04)

PROCESS FOR PREPARATION OF OPTICALLY ENRICHED ALDOL COMPOUNDS
The present invention relates to a process for preparing benzylic amidesof formula (I) wherein the variables are as defined in the specification, and the shown enantiomer has at least 50 % ee; by condensation of a ketone o formula (II) with an acetyl compound of formula (III) in the presence of a catalystof formula (IV) wherein the variables are as defined in the specification.
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(2020/05/28)

Preparation method of isoxazoline insectifuge
The invention belongs to the technical field of chemical drug synthesis, and particularly relates to a preparation method of an isoxazoline insectifuge. The preparation method is characterized in thatthe isoxazoline insectifuge is fluralaner; an intermediate I is sequentially subjected to an amidation condensation reaction, a substitution reaction and a ring closing reaction in the same reactioncontainer; and after the reactions are finished, a reaction product is poured into water, stirring and filtering are conducted to obtain a solid, and the obtained solid is recrystallized to obtain theisoxazoline insectifuge. The method has the beneficial effects that the method uses a solvent and one-pot method to synthesize fluralaner, technological operation of a synthesis process is reduced, treatment time and reaction time are shortened, product yield is improved, and the method is suitable for large-scale production.
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Paragraph 0032; 0039-0043; 0049-0063

(2020/09/30)

Preparation method of oxazoline insecticide
The invention discloses a preparation method of an oxazoline insecticide. The method comprises the steps that a first compound shown in description is used as a starting raw material; through oximation and amide condensation, a second compound shown in the description is obtained; further, through NXS substitution, elimination and cyclization, the oxazoline insecticide is obtained. The method hasthe advantages that the intermediate purification difficulty is lowered; meanwhile, the product purification difficulty is also lowered, so that the product quality and yield are improved; the productcompetitiveness is finally improved.
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(2019/06/30)

Absolute configuration assignment of (+)-fluralaner using vibrational circular dichroism
The absolute configurations of the separated enantiomers of fluralaner, a racemic animal health product used to prevent fleas and ticks, have been assigned using vibrational circular dichroism (VCD). The crystallographic structure of the active enantiomer (+)-fluralaner has previously been shown to have the (S) configuration using small molecule crystallography. We sought a faster analytical method to determine the absolute configuration of the separated enantiomers. When comparing the measured IR (infrared) and VCD spectra, it is apparent that the amide carbonyl groups appear in the IR but are nearly absent in the VCD. Computational work to calculate the VCD and IR using in vacuo models, implicit solvation, and explicitly solvated complexes has implicated conformational averaging of the carbonyl VCD intensities.
Kong, John,Joyce, Leo A.,Liu, Jinchu,Jarrell, Tiffany M.,Culberson, J. Chris,Sherer, Edward C.
p. 854 - 864
(2017/11/20)

INSECTICIDAL, MITICIDAL, NEMATICIDAL, MOLLUSCICIDAL, MICROBICIDAL, OR BACTERICIDAL COMPOSITION AND METHOD FOR CONTROLLING PEST
The present invention provides a novel insecticidal, miticidal, nematicidal, microbicidal, or bactericidal composition and a novel pest control method. An insecticide, miticide, nematicide, molluscicide, disinfectant, or bactericide composition containing
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Paragraph 0247

(2017/06/07)

METHOD FOR CATALYTIC ASYMMETRIC SYNTHESIS OF OPTICALLY ACTIVE ISOXAZOLINE COMPOUND, AND OPTICALLY ACTIVE ISOXAZOLINE COMPOUND
There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
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Paragraph 0236; 0237; 0238; 0252

(2014/12/09)

PROCESS FOR PRODUCTION OF ISOXAZOLINE-SUBSTITUTED BENZOIC ACID AMIDE COMPOUND
[Problem] To provide a production method of an isoxazoline-substituted benzoic acid amide compound. [means for solving the problem] A production method of an isoxazoline-substituted benzoic acid amide compound of Formula (1) where X is a halogen atom, Cs
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Page/Page column 27

(2011/04/25)

The antiparasitic isoxazoline A1443 is a potent blocker of insect ligand-gated chloride channels
A structurally unique isoxazoline class compound, A1443, exhibits antiparasitic activity against cat fleas and dog ticks comparable to that of the commercial ectoparasiticide fipronil. This isoxazoline compound inhibits specific binding of the γ-aminobutyric acid (GABA) receptor channel blocker [3H]4′-ethynyl-4-n-propylbicycloorthobenzoate (EBOB) to housefly-head membranes, with an IC50 value of 455 pM. In contrast, the IC50 value in rat-brain membranes is >10 μM. To study the mode of action of this isoxazoline, we utilized MdGBCl and MdGluCl cDNAs, which encode the subunits of housefly GABA- and glutamate-gated chloride channels, respectively. Two-electrode voltage clamp electrophysiology was used to confirm that A1443 blocks GABA- and glutamate-induced chloride currents in Xenopus oocytes expressing MdGBCl or MdGluCl channels, with IC50 values of 5.32 and 79.9 nM, respectively. Blockade by A1443 was observed in A2′S-MdGBCl and S2′A-MdGluCl mutant channels at levels similar to those of the respective wild-types, and houseflies expressing A2′S-MdGBCl channels were as susceptible to A1443 as standard houseflies. These findings indicate that A1443 is a novel and specific blocker of insect ligand-gated chloride channels.
Ozoe, Yoshihisa,Asahi, Miho,Ozoe, Fumiyo,Nakahira, Kunimitsu,Mita, Takeshi
experimental part
p. 744 - 749
(2011/03/22)

ISOXAZOLINE-SUBSTITUTED BENZAMIDE COMPOUND AND NOXIOUS ORGANISM CONTROL AGENT
An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A 1 , A 2 and A 3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., X is halogen atom, C 1 -C 6 haloalkyl, etc., Y ia halogen atm, C 1 -C 6 alkyl, etc., R 1 is C 1 -C 12 alkyl arbitrarily substituted with R 16 , C 3 -C 12 alkenyl, arbitrarily substituted with R 16 is oxygen atom or sulfur atom, -N(R 20 )R 19 , etc., R 2 is hydrogen atom, C 1 -C 4 alkoxy C 1 -C 6 alkyl, etc., R 3 is C 1 -C 6 haloalkyl, etc., R 16 is halogen atom, cyano, phenyl substituted with (Z) p1 , D-1 to D-60, E-1 to E-49, etc., R 19 is phenyl, phenyl substituted with (Z) p1 , etc., R 20 is hydrogen atom, C 1 -C 6 alkyl, etc., Z is halogen atom, nitro, C 1 -C 4 alkoxy, etc., D-1 to D-60 are 5- or 6-membered aromatic heterocyclic rings, E-1 to E-49 are 5- or 6-membered saturated heterocyclic rings, m is an integer of 0 to 5, n is an integer of 0 to 4, p1 is an integer of 1 to 5. The pesticide containing these compounds.
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Page/Page column 251

(2008/06/13)