57 results about "Pyrazolone" patented technology

The application discloses an electrolytic synthesis method of a pyrazolone compound intermediate, and the method uses a nitroso acid ester compound as raw material to obtain an electrolyte containing a hydrazine compound through electrochemical reduction; the electrolyte containing the hydrazine compound is subjected to a cyclization reaction to obtain a pyrazolone compound; the application uses a mild and efficient electrochemical reduction mode to replace a high-risk diazotization reaction to synthesize the pyrazolone compound; the electrolyte can be recycled for multiple times, and a large amount of sulfite, acid and other reagents needed in the synthesis process are avoided, and a large amount of 'three wastes' is reduced. The method has better product purity (> 95%) and yield (> 80%), the method is more green and environmental protection, no three wastes are generated, and is suitable for industrial production.

The invention relates to the technical field of pharmaceutical chemical engineering, in particular to a preparation method of a 5-fluoro-1-(2-fluorophenyl)-1H-pyrazolone [3, 4-B] pyridine-3-formonitrile crystal form, which comprises the following steps: mixing a 5-fluoro-1-(2-fluorophenyl)-1H-pyrazolone [3, 4-B] pyridine-3-formonitrile solid with isopropyl ether, and stirring for dissolving; and cooling, growing crystals, performing suction filtration, washing and drying. The preparation method of the 5-fluoro-1-(2-fluorophenyl)-1H-pyrazolone [3, 4-B] pyridine-3-formonitrile crystal form solves the problems that the original crystal form of the existing 5-fluoro-1-(2-fluorophenyl)-1H-pyrazolone [3, 4-B] pyridine-3-formonitrile is small in density, large in volume and easy to generate electrostatic effect, and the crystal form is easy to agglomerate to wrap impurities and is not beneficial to subsequent API (American Petroleum Institute) purification.

The application discloses a kind of molecularly imprinted magnetic microspheres for D-dimer high-efficiency detection and a preparation method thereof, and relates to the technical field of molecular imprinting.The method comprises the preparation of pyrazolone functional group modified magnetic nanomicrospheres, dispersing the pyrazolone functional group modified magnetic nanomicrospheres, D-dimer template molecules, functional monomers and crosslinking agent in a phosphate buffer solution, uniformly mixing, and then adding an initiator to carry out a polymerization reaction.After the polymerization reaction is completed, the D-dimer template molecules are eluted and removed, and the molecularly imprinted magnetic microspheres for D-dimer high-efficiency detection are obtained.The application utilizes the synergistic effect of salt bridge interaction and hydrogen bond interaction between arginine residues in D-dimer and pyrazolone functional groups, and successfully prepares magnetic molecularly imprinted microspheres with high recognition specificity for D-dimer.

This invention discloses a method for synthesizing nitrogen-containing heterocyclic compounds with a maleimide structural unit and a pyrazolone ring. The method includes the following steps: N-phenylmaleimide olefin and pyrazolone olefin are reacted with 4-dimethylaminopyridine in dichloromethane at a reflux temperature of dichloromethane. After the reaction, saturated brine is added to quench the reaction, followed by extraction with ethyl acetate, removal of the solvent by rotary evaporation under reduced pressure, and separation by forward silica gel column chromatography to obtain nitrogen-containing heterocyclic compounds with a maleimide structural unit and a pyrazolone ring. This invention utilizes optimal reaction conditions for substrate expansion, introducing methyl, methoxy, and chlorine atoms at the ortho, meta, and para positions on the benzene ring of N-phenylmaleimide olefin, constructing a series of nitrogen-containing heterocyclic compounds simultaneously containing a maleimide structural unit and a pyrazolone ring in yields up to 90%. The reaction method of this invention has a fast reaction rate and high yield.

The present application relates to the technical field of medicine and chemical industry, and in particular to a preparation method of a 5-fluoro-1-(2-fluorophenyl)-1H-pyrazolyl[3,4-B]pyridine-3-carbonitrile crystal form, which comprises the following steps: mixing 5-fluoro-1-(2-fluorophenyl)-1H-pyrazolyl[3,4-B]pyridine-3-carbonitrile solid with isopropyl ether, and then stirring and dissolving; cooling and crystallizing, and then drying after filtration and washing to obtain the product. The preparation method of the 5-fluoro-1-(2-fluorophenyl)-1H-pyrazolyl[3,4-B]pyridine-3-carbonitrile crystal form solves the problems of the original crystal form of 5-fluoro-1-(2-fluorophenyl)-1H-pyrazolyl[3,4-B]pyridine-3-carbonitrile, such as small density, large volume and easy electrostatic effect, and the crystal form is easy to form a group and wrap impurities, which is not conducive to subsequent API purification.

The disclosure relates to compounds of formula I, which are formyl peptide 2 (FPR2) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.

The present invention relates to the field of pyrazolones synthesis. To address the problem that synthesizing pyrazolones using carbonylation reactions requires expensive transition metal catalysts and highly toxic carbon monoxide, a method for synthesizing pyrazolones using carbon dioxide is provided. The reaction formula is as follows: Compound II reacts with carbon dioxide in an organic solvent under a carbon dioxide atmosphere in the presence of a base to obtain a pyrazolones structure. The present invention utilizes carbon dioxide to synthesize pyrazolones in an environmentally friendly and efficient manner.

The invention relates to a solid water-dispersible pharmaceutical composition for use in the treatment of a disease, said treatment comprising dispersing said pharmaceutical composition into an aqueous liquid to produce an enteraliy administrable liquid containing at least 0.5 gram of said pharmaceutical composition and at least 0.3 g / 1 of edaravone, followed by enteral administration of said enteraliy administrable liquid to a human patient in an amount to provide a dose of 30-300 mg of edaravone, said pharmaceutical composition comprising: 2-50 weight % of 3-methyl-l-phenyl-2-pyrazolin-5-one (edaravone); and 3-50 weight % of a water-soluble alkalizing agent. This solid composition containing edaravone can be easily dispersed in an aqueous liquid to prepare an aqueous solution of edaravone that can be ingested by a patient. The solid composition of the invention provides the advantage that when the composition is introduced into water the edaravone dissolves very rapidly and the enteraliy administrable liquid thus obtained has a high oral bioavailability.

The present application belongs to the technical field of rubbers, and particularly relates to a rubber composition and a preparation method therefor, and an OTR engineering tire using same. The rubber composition disclosed in the present application comprises (in parts by mass) 100 parts of a diene rubber, 0-1.5 parts of a tetrazine compound, 0.2-1.5 parts of a pyrazolone compound, 0-30 parts of a liquid rubber, 20-100 parts of a reinforcing filler, 0-5 parts of a silane coupling agent, 2-10 parts of a vulcanization activator, and a vulcanization accelerator, a vulcanizing agent, an antioxidant, a resin and a plasticizer. Moreover, the ratios of the tetrazine compound and the liquid rubber are not zero at the same time. The present application can significantly reduce the heat generated by the OTR engineering tire, and can also improve the damage resistance of the tire.

The invention discloses a method for synthesizing a chiral pyrazolone imine derivative based on an asymmetric aza-Henry reaction catalyzed by an organic catalyst, which comprises the following steps: placing a pyrazolone imine compound and a nitroalkane compound in a solvent, adding the organic catalyst, and reacting at-78-60 DEG C while stirring to prepare the target product chiral pyrazolone imine derivative. Or placing the pyrazolone imine compound and brominated nitromethane in a solvent, then adding an organic catalyst, carrying out a stirring reaction at-78 to 60 DEG C to prepare a chiral pyrazolone imine derivative, and further carrying out debromination to obtain the target product, namely the chiral pyrazolone imine compound. The asymmetric aza-Henry reaction of the pyrazolone imine compound and the nitroalkane compound or the bromo-nitromethane is successfully realized on the basis of the small organic molecule catalyst, and the asymmetric aza-Henry reaction has the advantages of low catalyst consumption, high reaction rate (the fastest reaction rate is 0.5 h), high enantioselectivity (the highest reaction rate reaches 96% ee), good universality of reaction substrates and the like.

The application discloses a 1-aryl-5-pyrazolone compound and a pharmaceutical composition and application thereof. The compound has a structure selected from any one of the following structures, and also comprises a tautomer, a pharmaceutically acceptable salt or a mixture thereof: the compound can effectively inhibit COX-2 and effectively scavenge free radicals at a micromolar concentration level, can reduce cardiovascular and digestive tract side effects caused by NSAID-induced free radical production, and can also play a better treatment effect on chronic inflammatory diseases with pain through the synergistic effect of antioxidation stress and anti-inflammatory analgesia.

The invention discloses a novel deuterium-containing pyrazolone compound as well as a pharmaceutical composition and application thereof, the novel deuterium-containing pyrazolone compound is shown as a formula (I) and / or a formula (II), and the definition of each substituent is shown in the specification. The compound can be used for preparing medicines for preventing or treating neurodegenerative diseases and cardiovascular and cerebrovascular diseases.

The present application belongs to the technical field of rubber, and particularly relates to a rubber composition and a preparation method therefor, and a truck tire using same. The rubber composition comprises, in parts by mass: 100 parts of diene rubber, 0.2-1.5 parts of a hydrazide compound, 0.2-1.5 parts of a pyrazolone compound, 0-30 parts of liquid rubber, 20-120 parts of a reinforcing filler, 0-10 parts of a silane coupling agent, 2-10 parts of a vulcanization activator, a vulcanization accelerator, a vulcanizing agent, an antioxidant, a resin and a plasticizer. The present application can significantly reduce the heat generation of the tire while improving its cut resistance and tear resistance, thereby enhancing the damage resistance of the truck tire.

The invention discloses an energetic compound based on pyrazolo [1, 5-a] pyrimidine and a synthesis method of the energetic compound. The synthesis method comprises the following steps: (1) reacting 2-oxime ethyl cyanoacetate, potassium permanganate and potassium hydroxide to prepare potassium salt of 2-cyano-2-nitroethyl acetate; (2) enabling the potassium salt of the 2-cyano-2-nitroethyl acetate to react with hydrazine hydrate, so as to prepare 5-amino-4-nitro-1, 2-dihydro-3-pyrazolone; and (3) carrying out a reaction on the 5-amino-4-nitro-1, 2-dihydro-3-pyrazolone, potassium permanganate and potassium hydroxide, so as to prepare the potassium salt of the 5-hydroxy-3, 6-dinitropyrazolo [1, 5-a] pyrimidine-2, 7 (1H, 4H)-diketone. The synthesis process is mild in condition and high in safety, the raw materials are easy to prepare, the product yield is high, and the synthesized energetic compound has good detonation performance and low sensitivity and has potential application value in the field of energetic materials.

The invention discloses a synthesis method of a diaryl quaternary carbon pyrazolone compound with a chiral center, and belongs to the field of organic synthesis. The method comprises the following steps: (1) at room temperature, taking ether as a solvent, adding silver oxide and substituted N-phenyl-3-(2-hydroxyphenyl) indole-2-ketone, and reacting for 6-12 hours; (2) performing column chromatography purification on the product to obtain an intermediate, taking a polar solvent or halogenated alkane as a solvent, adding alkali and substituted hydrazone, and reacting at 0-40 DEG C for 1-30 minutes; and (3) adding methyl iodide to continuously react for 1-12 hours to obtain the diaryl quaternary carbon pyrazolone compound with the chiral center as shown in the formula (I). According to the present invention, N-phenyl-3-(2-hydroxyphenyl) indole-2-one or a derivative thereof and substituted hydrazone are adopted as reactants to synthesize the diaryl quaternary carbon pyrazolone compound having the chiral center through the alkali start-up reaction, and the method has advantages of wide substrate universality, simple operation, mild condition and medium to excellent yield. (I)

The invention belongs to the technical field of wastewater treatment, and particularly relates to a purification treatment process for pyrazolone production wastewater. Aiming at the characteristics of high COD (Chemical Oxygen Demand), high total nitrogen, high salt and difficulty in biochemical degradation of the pyrazolone production wastewater, a whole-flow synergistic process of targeted pretreatment, resource recovery, mild detoxification and deep purification is constructed, acetonitrile is efficiently recovered through composite extraction and pervaporation membrane separation, and alkali thermal hydrolysis is catalyzed by a magnesium-aluminum composite catalyst; the heterocyclic compound is mildly subjected to ring opening degradation, and the biodegradability is improved. Photocatalysis and Fenton-like are combined to continuously generate hydroxyl free radicals, degradation-resistant organic matters are deeply oxidized and mineralized, the modified charcoal adsorbs residual small molecules and chromaticity, and metal ion residues and secondary pollution risks are reduced. According to the oxidation-adsorption coupling strategy, the strong degradation capacity of advanced oxidation and the adsorption purification function of biochar are fused, beneficial improvement of the treatment efficiency is achieved, it is ensured that wastewater reaches the standard and is discharged, meanwhile, resources are recycled, the cost is reduced, and environmental and economic benefits are achieved.

The present invention provides pyrazolone-fused pyrimidine compounds as shown in formula (II), which have excellent inhibitory activity against WEE1 kinase. [Formula 1] TIFF2022538901000260.tif41170

The application relates to a method for synthesizing dihydropyrrolo[2,3-c]pyrazole analogs. Specifically, under the catalysis of a transition metal and a bidentate ligand, dihydropyrrolo[2,3-c]pyrazole analogs can be obtained in high selectivity by using the bidentate ligand synergy, taking pyrazolinone as raw material and reacting with 1,3-alkyne under the action of triethylenediamine. The application uses cheap and commercially available 1,3-alkyne and easily obtained pyrazolinone, and a series of heterocyclic compounds with potential medicinal value are obtained in high selectivity under simple and mild conditions.

The invention discloses pyrazolo-pyranol compounds as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis and pharmacy. The invention provides a method for efficiently constructing a pyrazolo-pyranol skeleton by taking an electron-deficient peroxide as an amphiphilic reagent and carrying out an alkali-promoted Michael addition / cyclization / ring-opening reaction on the electron-deficient peroxide and pyrazolone or a derivative thereof. The preparation method comprises the following specific steps: dissolving substituted pyrazolone or a derivative II thereof and an amphiphilic electroreagent electron-deficient peroxide III in an organic solvent according to a molar ratio of 1: (0.5-3), adding a basic catalyst into a reaction system, reacting for 10-20 hours in a temperature range of 0-90 DEG C, and separating and purifying through silica gel column chromatography after the reaction is completed to obtain a target product pyrano [2, 3-b] pyrazolone derivative. The present invention relates to a compound (I) of [1, 2, 3-c] pyrazole-5-ol or a derivative The technical problems of limited raw material range, single product type, undefined application and the like in the prior art are solved, and an efficient, cheap and green new way is provided for synthesis and application of the pyrazolo-pyranol compound. The pyrano [2, 3-c] pyrazole-5-alcohol prepared by the method or the derivative thereof shows excellent inhibition on HeLa cells, and has good anti-tumor application potential.

The invention discloses a preparation method of a 1-substituted aryl-3-pyrazole alcohol compound, which is characterized in that in the presence of inorganic acid, sodium nitrite is used as an oxidant, and a 1-substituted aryl-3-pyrazolone compound is subjected to an oxidation reaction to obtain the 1-substituted aryl-3-pyrazole alcohol compound. The oxidation reagent adopted by the invention is safer, and safety accidents caused by high activity of the oxidizing agent are essentially avoided; the reaction system is obviously different from the existing alkaline system, the produced product has few impurities and higher content, and industrial large-scale production is facilitated.

Pyrazolone compounds, pharmaceutical compositions comprising the same, and methods of using the same are disclosed herein. The disclosed compounds may be used for treatment of neurodegenerative diseases and / or disorders, such as Alzheimer's disease.

The invention discloses a method for preparing a trifluoromethyl pyrazolone compound through visible light induction. According to the method, the trifluoromethyl pyrazolone compound is prepared through a free radical addition / cyclization cascade reaction. Under the irradiation of a visible light source, CF3 free radicals are generated through an electron donor-acceptor (EDA) compound formed by a Togni reagent II and organic alkali, and an external photocatalyst is not needed. According to the method, various N-methacrylhydrazide can be converted into target products, and the yield is good to excellent. The method is simple and convenient to operate and easy to amplify, has high functional group tolerance, and provides a sustainable synthesis path for synthesis of the functionalized heterocyclic compound.

The invention discloses a pyrazolone phenazine nitrogen-containing heterocyclic compound, a luminescent composition and an organic electroluminescent element, and relates to the technical field of organic photoelectric materials and elements. The pyrazolone phenazine nitrogen-containing heterocyclic compound is a compound with a molecular structure general formula (1), is a nitrogen-containing heterocyclic compound taking pyrazolone phenazine as a skeleton, has the characteristics of high performance and narrow emission spectrum, and can be applied to preparation of organic electroluminescent elements or lighting elements.

A synergistically effective herbicide composition comprising as component (A) an herbicidally active amount of pyridate and as component (B) at least one 4-HPPD inhibitor selected from the group comprising triketones, pyrazolones, isoxazoles and other 4-HPPD inhibitors, wherein a weight ratio of components (A) and (B) is in a range up to 1000:1. And a kit comprising pyridate and at least one 4-HPPD inhibitor and a use of a herbicide composition according to the invention in an amount effective for controlling one or more types of unwanted vegetation by applying the herbicide composition to the unwanted vegetation and / or a habitat thereof.

The utility model discloses a pyrazolone production wastewater treatment device, which belongs to the technical field of wastewater treatment and comprises a tank body, the top of the tank body is fixedly connected with an L-shaped connecting block, the L-shaped connecting block is fixedly connected with a servo motor, the top of the tank body is provided with a transmission mechanism, the L-shaped connecting block is provided with a pesticide spreading mechanism, and the pesticide spreading mechanism is provided with a pesticide spraying mechanism. And the top of the tank body is fixedly connected with a chemical feeding port. By arranging the conveying mechanism and the medicine spreading mechanism, uniform dispersion of medicine is realized, the conveying mechanism can control the medicine spreading speed and medicine quantity, and the medicine spreading mechanism can uniformly spread the medicine around by utilizing centrifugal force, so that waste is avoided, the medicine is more uniformly distributed, and the stability and the reliability of wastewater treatment are enhanced; by arranging the transmission mechanism, linkage of the multiple mechanisms is achieved, an operator only needs to control one servo motor, the operation states of the multiple mechanisms can be adjusted at the same time, the operation process is simplified, and the operation difficulty is reduced.

The application discloses application of a phenylpropionic acid compound in detection of monosaccharide composition of traditional Chinese medicine polysaccharide. The phenylpropionic acid compound has a structure as shown in formula (I). The application provides a new application of the phenylpropionic acid compound, and preliminary realization of quality control research on traditional Chinese medicine preknowing polysaccharide. Compared with a method for detecting monosaccharide composition of traditional Chinese medicine polysaccharide by using 1-phenyl-3-methyl-5-pyrazolone as a pre-column derivatization reagent, the application has the following advantages: 1. Derivatization of aldehyde sugar and ketose can be simultaneously realized; 2. The reaction temperature is more moderate, and the safety of the reaction is greatly improved; 3. The detection wavelength of HPLC-UV is improved from 245 nm to 274 nm, interference is reduced, and sensitivity is improved; and 4. The pre-column derivatization reagent is low in cost and easy to obtain.

A dye kit comprises: a) a colorant composition, comprising a1) at least one oxidative dye; b) a developer composition, comprising b1) at least one oxidant; and c) a retardant composition, comprising c1) at least one pyrazolone compound, and c2) at least one solvent capable of dissolving or dispensing the pyrazolonecompound; wherein the retardant composition is placed in a container separate from the colorant composition and the developer composition.

The invention discloses a pyrazolone compound as well as a preparation method and application thereof. The compound has a structural formula as shown in a formula I, wherein X is selected from N or O; r1 is selected from thienyl, naphthyl, phenyl or phenyl substituted by at least one of C1-6 alkyl, C1-6 alkoxy and halogen; r2 is selected from alkyl of C1-6, phenyl or phenyl substituted by alkoxy of C1-6; r3 is selected from H and alkyl of C1-6; and R4 is selected from phenyl or phenyl substituted by at least one of C1-6 alkyl, C1-6 alkoxy and halogen. The invention provides a series of pyrazolone compounds with novel structures, and the compounds can protect nematodes and reduce damage of formaldehyde to the nematodes, so that the survival rate of the nematodes is improved. The compound can be used for preparing medicines for treating and / or preventing Parkinson's disease, senile dementia or formaldehyde poisoning.

Disclosed are a new deuterium-containing pyrazolone compound, and a pharmaceutical composition and the use thereof. The new deuterium-containing pyrazolone compound is as represented by formula (I) and / or formula (II), wherein the definition of each substituent is detailed in the description. The compound can be used in the preparation of a drug for preventing or treating neurodegenerative diseases and cardiovascular and cerebrovascular diseases.

Provided are a class of fused-cyclic pyrazolone formamide compounds and a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided is a compound having the structure as shown in formula (I) (with each group defined in the description). The compound can be used as an AXL inhibitor in the preparation of a pharmaceutical composition for treating tumors.