56 results about "Isoxazole" patented technology

The invention belongs to the technical field of organic synthesis, and particularly relates to a synthesis method of an isoxazole compound under a visible light catalysis condition. The method comprises the following steps: dissolving a compound 1 in 1, 2-dichloroethane, then adding tert-butyl nitrite, tribromomethane, alkali and a photocatalyst, in an inert gas environment, irradiating with visible light and stirring at room temperature to react, after the reaction is completed, reducing pressure to remove a solvent, and then performing silica gel column purification on a crude product to obtain a product, namely the isoxazole compound. The brand-new method for preparing the isoxazole compound through visible light catalysis is developed, the conditions of high temperature and high pressure in a traditional synthesis method are avoided, energy consumption and environmental pollution are remarkably reduced, and the yield of the isoxazole compound is effectively increased by regulating and controlling reaction conditions and optimizing raw material selection and proportion.

The invention discloses a self-repairing mute tire and a preparation method thereof, and relates to the technical field of tires, the self-repairing mute tire comprises a tire body, and a self-repairing rubber layer and a mute material which are sequentially attached to the inner wall of the tire body from inside to outside; the self-repairing adhesive layer is prepared from the following components: epichlorohydrin rubber, acrylate rubber, a rosinyl phenyl phosphine oxide isoxazolyl functional polymer, 4, 4-chloroformyl phenyl ether, a catalyst, 2, 2-bis [4-(4-aminophenoxy) phenyl]-1, 1, 1, 3, 3, 3-hexafluoropropane, trithiocyanuric acid, a filler, an accelerant TMTD (Tetramethylthiuram Disulfide) and an auxiliary agent; the rosinyl phenyl phosphine oxide isoxazolyl functional polymer comprises structural units introduced through a condensation polymerization reaction of the following monomers: glycerol triabietate, bis (4-carboxyl phenyl) phenyl phosphine oxide and 3, 5-isoxazoledicarboxylic acid. The tire is remarkable in self-repairing effect, good in mute performance, sufficient in performance stability and long in service life.

The application provides a benzene [d] isoxazole compound and an application thereof. The compound has the structure shown in the following formula I. The benzene [d] isoxazole compound provided by the application can induce degradation of BET protein and / or GSPT1 protein, and has an anti-proliferation effect on cancer cells. Therefore, the compound and the composition provided by the application can be used for preparing a drug for treating or preventing tumor formation, inflammation, viral infection, cell proliferative disorder, autoimmune disease, sepsis and the like.

The present application relates to a kind of synthesis method of indole aldehyde and its derivative, after the reaction of o-nitro halogenated benzene compound and 4-isoxazole boronic acid pinacol ester, ring closure is obtained target product while reducing nitro group.The present application provides a kind of synthesis method of indole aldehyde and its derivative, which generates aldehyde group while synthesizing indole ring, compared with existing reference, the range of raw material selection is wide, route is short, synthesis operation is simple, reaction condition is mild, and environment is friendly.

The invention discloses a carbon fluoride battery electrolyte and a carbon fluoride primary battery, and belongs to the technical field of lithium metal primary batteries. The electrolyte comprises a fluorine-containing matrix solution and an isoxazole compound additive, wherein an R1 substituent group of an isoxazole compound is selected from a plurality of functional groups such as alkoxy, fluoroalkyl, carbonyl, ether group, carbamate group and the like. The electrolyte has excellent ionic conductivity at low temperature, and can effectively regulate and control the deposition morphology of a LiF passivation layer, reduce the interface impedance and inhibit the growth of lithium dendrites. A primary battery constructed based on the electrolyte shows excellent low-temperature discharge performance and cycling stability, and is suitable for a high-reliability energy storage scene.

The present invention relates to the crystal forms of methyl(2R*,4R*)-4-[[(5S)-3-(3,5-difluorophenyl)-5-vinyl-4H-isoxazole-5-carbonyl]amino]tetrahydrofuran-2-carboxylate (I) existing in the form of two stereoisomers: Methyl(2R,4R)-4-[[(5S)-3-(3,5-difluorophenyl)-5-vinyl-4H-isoxazole-5-carbonyl]-amino]tetrahydrofuran-2-carboxylate of formula (Ia) and methyl (2S,4S)-4-[[(5S)-3-(3,5-difluoro-phenyl)-5-vinyl-4H-isoxazole-5-carbonyl]amino]tetrahydrofuran-2-carboxylate of formula (Ib), to a method for preparing the crystal forms, to the use for preparing stable agrochemical formulations, and to the use in the field of agriculture for controlling harmful plants.

The invention relates to the technical field of pesticides. The structural formula of an isoxazole persulfate compound is shown as a formula (I). The invention particularly relates to a synthesis method of a persulfide compound containing isoxazole and prevention and control of the persulfide compound on agricultural and forestry diseases, weeds and weeds. The method is mild in reaction condition and high in practicability and conforms to the modern green chemistry concept. Meanwhile, the compound has a good control effect on agricultural and forestry diseases, weeds and weeds, and the chemical structure and the application effect of the compound are not disclosed in existing reports related to sterilization, insecticide and herbicides.

The application provides an application of isoxazole 9 (ISX-9) in promoting mesenchymal stem cell osteogenic differentiation and bone injury regeneration repair. ISX-9 is a small molecule compound, and has the characteristics of easy to obtain, controllable structure and low cost. The in vitro experiment of the application shows that ISX-9 has the ability to induce mesenchymal stem cell osteogenic differentiation and promote the formation of mineralized nodules; the in vivo experiment shows that the hydrogel wrapped with ISX-9 can promote the regeneration repair of mouse skull defects, indicating that ISX-9 has good osteogenic induction and is a potential bone regeneration repair drug. Therefore, ISX-9 can promote mesenchymal stem cell osteogenic differentiation and be applied to bone tissue regeneration repair. The application also provides a direct action target and action mechanism of ISX-9 in promoting osteogenic differentiation. The application further provides a new drug sustained release delivery system of ISX-9, which is helpful for the application from theoretical research to clinical application.

The present invention relates to a novel isoxazole compound as a TM4SF5 specific inhibitor and a use thereof, and more specifically, to a novel isoxazole compound, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the same, in which the compound can inhibit the expression, protein-protein binding or signal transduction activity of a TM4SF5 protein, and can inhibit the TM4SF5 protein. Or the immune checkpoint function is inhibited by activating the killing efficacy of T and NK immune cells or regulating the distribution of the T and NK immune cells. Specifically, the isoxazole compound provided by the invention is a TM4SF5 specific isoxazole compound, and can inhibit immune checkpoints of NK cells, so that the isoxazole compound has the advantage of being used as an inhibitor of liver diseases or liver cancer.

The present disclosure provides compounds represented by Formula I:and pharmaceutically acceptable salts, solvates, e.g., hydrates, and prodrugs thereof, wherein X and n are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat diseases and conditions, e.g., cancer, wherein inhibition of HDAC provides a benefit.

The invention provides a method for analyzing an anti-eczema effect target spot of traumatology based on network pharmacology. The method comprises the following steps: firstly, screening out seven representative active components through a SwisSADME platform, predicting by integrating SwisTarget Prediction, SEA and ChEMBL databases to obtain 367 drug targets, and analyzing to obtain 82 intersection targets; a PPI network is constructed based on an STRING database, and 10 core targets such as IL6, TNF and EGFR are screened out through topology analysis. GO / KEGG enrichment analysis reveals that the GO / KEGG is significantly enriched in the processes of IL-17 signal pathway, epidermal barrier repair and the like. Molecular docking verification proves that isofraxidin, scopoletin and verbenin are strongly combined with EGFR (epidermal growth factor receptor) targets. According to the method, a multi-component-multi-target-multi-channel synergistic eczema treatment mechanism of traumatology is systematically analyzed, and a theoretical basis is provided for preparation optimization.

The invention relates to the technical field of organic chemistry, and particularly discloses an isoxazole amide derivative with a structure shown in a general formula III as well as a preparation method and application of the isoxazole amide derivative. The isoxazole amide derivative disclosed by the invention shows remarkable antibacterial activity on staphylococcus aureus, escherichia coli, methicillin-resistant staphylococcus aureus (MRSA) and fluoroquinolone-resistant escherichia coli (FREC), the activity of part of compounds is superior to that of gentamicin, and the isoxazole amide derivative has broad-spectrum antibacterial potential and can be used for preparing medicines for treating related bacterial infections.

Described herein are detecting methods for conformational disease, aging and proteinopathies, by measuring the presence of b-isox-precipitates and the levels of b-isox-captured proteins in biofluids of healthy individuals and patients. Research identified additional biomarkers, which made it possible to detect, diagnose or treat, a human disease in a human subject by, with or without adding an isoxazole to an obtained biofluid sample, detecting the biomarker. Use of b-iso and / or biomarkers for diagnosing the disease are made possible.

The application discloses application of an amino isoxazole compound in preventing and treating Ralstonia solanacearum, and belongs to the technical field of plant bacterial wilt prevention and treatment; the amino isoxazole compound is 5,6-dihydro-4H-cyclopenta[c]isoxazol-3-amine; it is found for the first time that 5,6-dihydro-4H-cyclopenta[c]isoxazol-3-amine has strong inhibitory activity on Ralstonia solanacearum; experiments show that the MIC of 5,6-dihydro-4H-cyclopenta[c]isoxazol-3-amine on Ralstonia solanacearum is 6 mu g / mL at 24 h, is equivalent to that of benzio carb, and can be used for preventing and treating plant bacterial wilt, thereby providing a new candidate compound for development of a bactericide for Ralstonia solanacearum.

The application discloses a kind of diazomethyl isoxazole energetic compounds and synthesis method thereof, its structural formula is as shown in formula (I).The application also provides the synthesis method of the compound.The energetic compound disclosed in the application is liquid at room temperature, the thermal decomposition temperature is 204 DEG C, the heat of formation is 739.64 kJ / mol, and it has good application potential in energetic plasticizer.

The invention provides a preparation method of an isoxazole-oxadiazole compound, which comprises the following steps: reacting 4-chloro-2-fluoro-3-vinylbenzoic acid with tert-butyloxycarboryl hydrazine in the presence of a condensing agent and a catalyst, then removing a protecting group under an acidic condition to obtain an intermediate 4-chloro-2-fluoro-3-vinylbenzoyl hydrazine, and then reacting with N, N-dimethylformamide to obtain the isoxazole-oxadiazole compound. The method comprises the following steps: cyclizing N, N '-carbonyldiimidazole in the presence of alkali, carrying out an O-alkylation reaction with an alkylation reagent R1-X in the presence of alkali, and carrying out an olefin dihydroxylation-sodium periodate oxidation cleavage reaction in the presence of an oxidant and a catalyst; reacting with hydroxylamine in the presence of alkali, and finally carrying out 1, 3-dipolar cycloaddition reaction with an acrylate compound in the presence of alkali and an oxidizing agent. The method is carried out at room temperature, has the advantages of mild conditions, simplicity in operation and the like, is wider in application range compared with a traditional synthesis method, and has important synthesis application value.

The invention relates to the field of crop protection, more specifically to the use of methyl (2R*,4R*)-4- [[(5S)-3-(3,5-difluorophenyl)-5-vinyl-4H-isoxazole-5-carbonyl]amino]tetrahydrofuran-2-carboxylate (I) and / or a salt thereof for control of undesired vegetation at a cultivation site for dicotyledonous crop plants through an application prior to the emergence of the dicotyledonous crop plants.

The invention relates to the technical field of material preparation, in particular to an isoxazole-containing bridged pyrazolopyran quinoline derivative and a synthesis method thereof. The isoxazole bridged pyrazolopyranoquinoline derivative is efficiently prepared by taking pyrazolone as a carbon attack point or an oxidation attack point and a 2-((halogenated quinoline-3-yl) vinyl) isoxazole compound through a base catalysis series cyclization reaction, and has the characteristics of easily available raw materials, simplicity and convenience in operation, high atom economy and the like, and meanwhile, the isoxazole bridged pyrazolopyranoquinoline derivative can be used for preparing the pyrazolopyranoquinoline derivative. The isoxazole bridged pyrazolopyranoquinoline derivative prepared by the invention combines two known dominant structures with biological activity, namely isoxazole and pyrazolopyranoquinoline, and is expected to generate a synergistic effect, so that the isoxazole bridged pyrazolopyranoquinoline derivative has important application prospect and implementation value in drug research and development.

The application relates to the technical field of pesticide chemistry, and discloses a phenyl isoxazole derivative containing a triazole ring as well as a preparation method and application thereof. The phenyl isoxazole derivative containing the triazole ring has the structural formula: The phenyl isoxazole derivative containing the triazole ring provided by the application has good insecticidal activity on agricultural pests such as Plutella xylostella, Spodoptera frugiperda, Helicoverpa armigera, Ostrinia nubilalis, and aphids when the concentration is 50 mu g / mL. Therefore, the phenyl isoxazole derivative containing the triazole ring provided by the application can be applied to the prevention and control of agricultural pests as an active pesticide ingredient.

The invention relates to the technical field of pesticide chemistry, and discloses an isoxazoline derivative containing a triazole thioether structure and preparation and application of the isoxazoline derivative, three active fragments of isoxazole, triazole and thioether are innovatively subjected to structural splicing synthesis, and the preparation process is clear in step, mild in reaction condition, excellent in intermediate yield and easy to industrially amplify. The insecticidal activity of the derivative on major agricultural pests such as plutella xylostella, spodoptera frugiperda and ostrinia nubilalis reaches 100%, the activity of the derivative is equivalent to that of fluxazole amide, the derivative can prevent and treat various pests such as cotton bollworm, aphid and rice planthopper, and the derivative is not applied in the field, has no drug resistance of the pests, has the advantages of broad spectrum, high efficiency, difficult generation of drug resistance and the like, can be used for preparing insecticides, and has wide application prospects. A brand new solution is provided for green prevention and control of agricultural pests.

The application relates to an extraction method for purifying 3-phenyl-5-vinyl-4H-isoxazole-5-carboxylic acids of formulae (Ia) and / or (Ib), in particular those which are contaminated with by-products of a preceding elimination reaction.

The present disclosure provides compounds represented by Formula I:and pharmaceutically acceptable salts, solvates, e.g., hydrates, and prodrugs thereof, wherein X and n are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat diseases and conditions, e.g., cancer, wherein inhibition of HDAC provides a benefit.

The present invention relates to a novel process for preparing methyl 4-[[3-(3,5-difluorophenyl)-5-vinyl- 4H-isoxazole-5-carbonyl]amino]tetrahydrofuran-2-carboxylate of formula (I) in all its stereoisomeric forms, mixtures thereof and agrochemical acceptable salts thereof.

The application discloses a kind of inhibitors of targeting 5-HTT / HDAC double target and preparation method and application thereof.The application is based on the principle of rational drug design, and synthesizes novel small-molecule compounds with 5-HTT and HDAC inhibitory activity, multi-targets with potential antidepressant activity.The inhibitors of targeting 5-HTT / HDAC double target have both 5-HTT inhibitor effect and HDAC inhibitory effect, and are a kind of multi-target fluoxetine derivatives with 5-HTT and HDAC synergistically realizing antidepressant.The compound of the application is superior to fluoxetine compound in design strategy, introduces isoxazoles structure that can improve antidepressant activity, improves antidepressant activity, and has good improvement on the shortcomings of long treatment time and large side effects of currently used antidepressant compounds.

The present disclosure relates to a herbicidal composition and in particular, a granular composition comprising at least one N-phenyltriazolinone herbicide, at least one isoxazole herbicide, at least one triazinone herbicide and at least one agrochemically acceptable excipient. The present disclosure also relates to a method for controlling weeds using the herbicidal composition thereof.

The invention discloses a 4-trifluoromethyl isoxazole compound and an electrochemical synthesis method and application, and belongs to the field of organic synthesis. The structural formula of the 4-trifluoromethyl isoxazole compound is shown in the specification; wherein R1 is one of methyl, methoxyl, a chlorine atom and a bromine atom; r2 is one of methyl, methoxyl, a chlorine atom and a bromine atom; r1 and R2 independently exist; the condition that R1 and R2 independently exist comprises that only R1 exists, only R2 exists, and neither R1 nor R2 exists. The 4-trifluoromethyl isoxazole compound prepared by the invention solves the problems of narrow reaction substrate application range, expensive reagents, complex reaction substrate synthesis, low yield and harsh reaction conditions in the traditional preparation process of the 4-trifluoromethyl isoxazole compound, has better inhibitory activity, and can be applied to preparation of antitumor drugs.

The invention provides an isoxazole biphenyl compound with CBP BRD and BRD4 BD2 inhibitory activity as well as a preparation method and application of the isoxazole biphenyl compound, and also provides an isoxazole biphenyl compound with CBP BRD and BRD4 BD2 inhibitory activity or a pharmaceutically acceptable salt of the isoxazole biphenyl compound, and the isoxazole biphenyl compound has a structural formula shown as a general formula (I) and a general formula (II). The invention also provides application of the isoxazole biphenyl compound or the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the isoxazole biphenyl compound in preparation of drugs for preventing or treating cancers, inflammations and metabolic diseases related to CBP and BRD4. The invention has the following technical effects: a novel molecule is designed and synthesized, and the structure is optimized, so that a compound with specific inhibitory activity on two targets of CBP BRD and BRD4 BD2 at the same time is obtained. The invention further provides a synthesis method of the compound, and the target compound can be efficiently prepared.

Compound of formula (l): wherein R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphoriylaminoalkyl or N-hydroxycarboximidamide group, process for its preparation and pharmaceutical composition containing it for use as a modulator of the AMPA (a-amino-3 hydroxy-5 -methyl-4-isoxazole-propionfc acid) receptor.

Compounds of the formula Iare provided. These compounds can inhibit c-Kit kinase and can be employed for the treatment of cancer.