34 results about "Pyrazolone" patented technology

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.

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 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 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 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 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.

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 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.

The present application belongs to the technical field of wastewater treatment, and particularly relates to a purification treatment process for pyrazolone production wastewater. The present application, in view of the characteristics of high COD, high total nitrogen, high salt and difficult biodegradation of the pyrazolone production wastewater, constructs a whole-process collaborative process of targeted pretreatment-resource recovery-mild detoxification-depth purification, efficiently recovers acetonitrile through composite extraction and pervaporation membrane separation, catalyzes alkaline hydrolysis through a magnesium-aluminum composite catalyst, mildly degrades heterocyclic compounds through ring-opening, and improves biodegradability. Photocatalysis and Fenton-like are combined to continuously generate hydroxyl radicals, deeply oxidize and mineralize refractory organic matter, modify the biological carbon to adsorb residual small molecules and chroma, and reduce the residual metal ion and secondary pollution risk. The oxidation-adsorption coupling strategy combines the strong degradation ability of advanced oxidation and the adsorption purification function of biological carbon, realizes the beneficial improvement of treatment efficiency, ensures that the wastewater meets the discharge standard, recovers resources to reduce costs, and has both environmental and economic benefits.

The invention discloses a pyrazolone compound, a pharmaceutical composition containing the pyrazolone compound and application of the pyrazolone compound and the pharmaceutical composition. The pyrazolone compound is a compound shown in a general formula I or a tautomer, a raceme, a meso-raceme, an enantiomer, a diastereoisomer and pharmaceutically acceptable salt of the compound. The pyrazolone compound provided by the invention can inhibit a Z-type nucleic acid binding protein 1 (ZBP1) signal channel, and has an application prospect in treatment of diseases related to ZBP1 protein functions.

The application discloses a method for preparing a hydroxylamine aqueous solution by a hydroxylamine salt neutralization method, and belongs to the technical field of hydroxylamine aqueous solution preparation. Specifically, a hydroxylamine salt is added into a reaction container, and is dissolved in a proper amount of deionized water; stirring is started under normal pressure; an alkali solution is added dropwise to perform a neutralization reaction; after the neutralization reaction is completed, the reaction solution is reduced-pressure filtered; a proper amount of a stabilizer is added into the filtrate; and then, reduced-pressure distillation is performed; and a distillate is the hydroxylamine aqueous solution. In the method, a pyrazolone type stabilizer is adopted, a mercapto imidazole sodium propyl sulfonate is introduced as a chelating agent, and a piperazine functional group is introduced, so that the stabilizing effect of the stabilizer can be effectively increased.

The invention relates to the technical field of yellow pigment processing, in particular to a sun-proof yellow pigment preparation process and a product thereof, and the process comprises the following steps: under the protection of nitrogen, preparing a diazonium solution from polyvinylpyrrolidone, hydrochloric acid, dichloroaniline and sodium nitrite; preparing a coupling solution from sodium hydroxide, phenyl methyl pyrazolone and hexadecyl trimethyl ammonium bromide; mixing the modified titanium dioxide with sodium dodecyl benzene sulfonate, rosin soap and ethylene diamine tetraacetic acid, carrying out four-stage pH regulation and gradient heating, finally adding the modified titanium dioxide, and carrying out heat preservation, filter pressing and drying. On the premise of not changing the traditional azo core reaction, the sun-proof grade of the pigment is improved to 7-8 grade from 4-5 grade through assistant synergy and crystal form regulation and control, and the pigment has high tinting strength, excellent dispersity and batch stability, is suitable for building exterior wall coatings, automobile plastic ornaments and high-end light-color ink, and thoroughly solves the problem of outdoor yellow color fading.

The invention discloses application of a trifluoromethylthio-substituted pyrazolone compound in preparation of a medicine for treating lung cancer, and belongs to the technical field of medicines. According to the trifluoromethylthio-substituted pyrazolone compound disclosed by the invention, Ar is an aromatic substituent or an aromatic heterocyclic substituent, can effectively inhibit proliferation of human non-small cell lung cancer cells (A549), and can be used for preparing anti-lung cancer drugs.

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.

This invention relates to the field of organic synthesis technology, and in particular to a method for preparing N,S-acetal compounds based on a transition metal catalytic system. The method uses a chiral complex formed by a chiral binaphthyl-imidazoline tridentate ligand and a transition metal as a catalyst to catalyze asymmetric nucleophilic addition reactions of thiols, thiophenols, and pyrazolinone imine compounds. This method solves the problems of the scarcity of chiral transition metal complexes and the harsh reaction conditions of some catalytic systems in existing asymmetric nucleophilic addition reactions of thiols to imines. Simultaneously, the method yields chiral N,S-acetal compounds with high yields and excellent enantioselectivity.

The application discloses a method for preparing a trifluoromethyl-containing pyrazolone compound under visible light irradiation, which prepares the trifluoromethyl-containing pyrazolone compound through a free radical addition / cyclization cascade reaction. Under visible light irradiation, the reaction generates CF3 free radicals through an electron donor-acceptor (EDA) complex formed by Togni reagent II and an organic base, without an external photocatalyst. The method can convert various N-methyl acryl hydrazides into target products with good to excellent yield. The method is simple in operation, easy to scale up, and has high functional group tolerance, and provides a sustainable synthesis path for the synthesis of functional heterocyclic compounds.

This invention aims to provide a method for preparing bis(4-pyrazolone)methane compounds. The preparation method is as follows: a mixture of compound A and compound B is added to an organic mixed solvent, heated under reflux at a certain temperature for 4-6 hours, then filtered while hot. The filtrate is allowed to evaporate the solvent naturally at room temperature to obtain the final target product C. R1, R2, R3, R4, and R5 are any one of alkyl, aryl, heterocyclic, or hydrogen atoms, respectively. The method for preparing bis(4-pyrazolone)methane compounds provided by this invention requires fewer raw materials, has simpler synthesis steps, milder reaction conditions, and higher yield than traditional methods. These compounds have the ability to improve the growth rate of edible fungi mycelia and activate the activity of mycelial succinate dehydrogenase, and can be used as potential growth regulators for edible fungi.

This invention discloses a method for synthesizing a standard sample for detecting tartrazine intermediates as shown in structural formula 1, characterized by the following reaction formula 1. This patent provides a method for preparing a standard sample for detecting the content of tartrazine intermediates, the structure of which is shown in structural formula 1, enabling rapid and accurate quantitative detection of 1-(4'-sulfonylphenyl)-3-carboxylic acid methyl ester-5-pyrazolone monosodium salt in tartrazine.

The present application belongs to the field of tire manufacturing, and particularly relates to a tire sidewall rubber composition and a preparation method and application thereof. The tire sidewall rubber composition is composed of the following raw materials in parts by mass: natural rubber 10-100 parts by mass, butadiene rubber 10-100 parts by mass, carbon black 30-80 parts by mass, zinc oxide 1-15 parts by mass, rubber oil 3-15 parts by mass, fatty acid compound 1-5 parts by mass, protective wax 1-4 parts by mass, antioxidant 0.5-4 parts by mass, sulfur powder 1-8 parts by mass, accelerator 0.5-3 parts by mass, anti-scorching agent 0.05-0.5 parts by mass, pyrazolone heterocyclic compound 0.3-3 parts by mass, and phenolic compound 0.5-5 parts by mass. The pyrazolone heterocyclic compound and the phenolic compound synergize with the traditional antioxidant, make up for the deficiency of the traditional antioxidant, and significantly improve the comprehensive performance of the entire rubber composite material, thereby effectively prolonging the service life of the tire sidewall. The tire manufactured by using the rubber composition has excellent durability and use safety.

Disclosed are a pyrazolone-fused pyrimidine compound, a preparation method for same and applications thereof. Provided in the present invention is the pyrazolone-fused pyrimidine compound as represented by formula (II). The compound has improved inhibitory activity with respect to WEE1 kinase.

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