209 results about "Propanamide" patented technology

Stable and bioavailable formulations and dosage forms comprising a dispersion (e.g., spray-dried dispersion) of solid amorphous 6-(cyclopropancamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide (Formula (I): BMS-986165) in a solid polymer matrix are provided for the treatment of auto-immune and auto-inflammatory diseases such as an inflammatory bowel disease (IBD) and psoriasis.

The present invention belongs to the technical field of petroleum fracturing production enhancement and modification, and specifically discloses a fracturing fluid pre-fluid for optimizing the size of in-situ autogenous proppant and its application, which is used to solve the problem of small particle size of proppant particles generated by hydrothermal reaction of formation minerals. The fracturing fluid pre-fluid is suitable for calcium-rich reservoirs and is composed of clean water, phosphate, pH regulator and Ca 2+ The chelating agent composition comprises 1 to 10 parts by weight of phosphate relative to 100 parts by weight of clean water, a volume molar concentration of the pH regulator is 1 to 5 mol / L, and Ca 2+ The molar concentration of the chelating agent is 0.001~1mol / L; the pH regulator is urea, ammonia, propionamide, etc. 2+ The chelating agent is EDTA, glutamic acid, etc. The present invention increases the average particle size of proppant particles generated by hydrothermal reaction of formation minerals, thereby improving the supporting effect thereof in micro-fractures of the formation.

This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4 -yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.

The invention belongs to the technical field of petroleum fracturing yield increase transformation, and particularly discloses fracturing fluid prepad fluid for optimizing the size of an in-situ authigenic proppant and application of the fracturing fluid prepad fluid, which are used for solving the problem of small particle size of proppant particles generated by a formation mineral hydrothermal reaction in the prior art. The fracturing fluid prepad fluid is suitable for a calcium-rich reservoir and is composed of clear water, phosphate, a pH regulator and a Ca < 2 + > chelating agent, relative to 100 parts by weight of clear water, the content of the phosphate is 1-10 parts by weight, the volume molar concentration of the pH regulator is 1-5 mol / L, and the volume molar concentration of the Ca < 2 + > chelating agent is 0.001-1 mol / L; the pH regulator is urea, ammonia water, propanamide and the like, and the Ca < 2 + > chelating agent is EDTA (Ethylene Diamine Tetraacetic Acid), glutamic acid and the like. The average particle size of the proppant particles generated by the formation mineral hydrothermal reaction is increased, and the supporting effect of the proppant particles in formation microfractures is improved.

The invention discloses a novel methylpyrazole propionamide derivative as well as a preparation method and application thereof. According to the invention, 3-hydroxypyrazole is used as an active matrix skeleton and is combined with a pharmacodynamic group propionamide with herbicidal activity to develop a novel hydroxypyrazole herbicide, and a series of novel 3-oxypropionamide-1-methylpyrazole-carboxylic ester derivatives are designed and synthesized. The invention also provides biological activity of the compounds for controlling agricultural, horticultural and forestry weeds, a determination method of the compounds, and application of the compounds in the fields of agriculture, horticultural and forestry.

The invention provides high-gloss ASA rubber powder and a preparation method thereof, and relates to the technical field of high polymer material processing. The high-gloss ASA rubber powder is a grafted copolymer of acrylate rubber and a styrene-acrylonitrile copolymer, and comprises a core layer, a core layer and a shell layer from inside to outside, the particle size of the core layer is 50 to 100 nm; the particle size of the high-gloss ASA rubber powder is 100 to 300 nm; the core layer is prepared from the following raw material components in parts by mass: 100 to 120 parts of butyl acrylate; 1 to 5 parts of methyl propanamide; 1-10 parts of a composite emulsifier; 0.1 to 1 part of an initiator; 0.5 to 1.2 parts of nano silicon dioxide; and 100 to 180 parts of water. By optimizing the monomer components and proportion and optimizing the preparation method, the glossiness of the ASA colloidal particles is remarkably improved while the weather resistance, heat resistance and impact strength of the ASA colloidal particles are ensured.

The invention belongs to the technical field of medicines, and relates to a preparation method of a rucotinib phosphate key intermediate, in particular to a preparation method of 3-cyclopentyl acrylonitrile. Comprising the following steps: reacting 3-cyclopentyl propionyl chloride with ammonia water to generate 3-cyclopentyl propionamide; 3-cyclopentyl propionamide is dehydrated in the presence of a dehydrating agent such as phosphorus oxychloride to generate 3-cyclopentyl propionitrile; in a certain solvent, 3-cyclopentyl propionitrile reacts with a halogenating reagent (NCS, NBS and the like) to generate 2-halogenated-3-cyclopentyl propionitrile; and finally, in a certain solvent, eliminating the 2-halogenated-3-cyclopentyl propionitrile under an alkaline condition to generate the target product 3-cyclopentyl acrylonitrile. The method is simple to operate, mild in condition, excellent in yield and quality and suitable for industrial production.

The invention provides a method for preparing a storage-resistant water-insoluble isothiazolinone, and belongs to the technical field of chemical synthesis. The invention first uses N,N'-di-n-octyl dithiodipropionamide, a chlorinated solvent and chlorine as raw materials for chlorination reaction to prepare 2-n-octyl isothiazolin-3-ketone OIT and / or 4,5-dichloro-2-n-octyl isothiazolin-3-ketone DCOIT finished products with less impurity content, thereby reducing the discoloration reaction caused by impurities; the product is then mixed with a stabilizer, and the inhibitory effect of the stabilizer on the free radical discoloration process is utilized to finally obtain a storage-resistant water-insoluble isothiazolinone, thereby solving the problem of discoloration of the water-insoluble isothiazolinone during storage.

2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2-oxopyrrolidin-1-yl)propanamide derivatives with R-configuration at the stereogenic center are disclosed, showing broad-spectrum protective activity in animal models of epileptic seizures, pain, depression and anxiety that are simultaneously devoid of undesirable sedative effects. Additionally, the disclosed derivatives have neuroprotective effects in the in vitro and in vivo studies.

The invention discloses a small molecular proteasome agonist as well as a preparation method and application thereof. According to the invention, cyclohexylamine is used as an initial raw material, and 3-(1-(benzo [D] thiazole-2-carbonyl)-2-(furan-2-methylene) hydrazone group)-N-cyclohexylpropanamide and N-cyclohexyl-3-(2-(furan-2-methylene)-1-(quinoline-2-carbonyl) hydrazone group) propanamide are prepared through a five-step reaction. The two compounds provided by the invention have good 20S proteasome agonistic activity and ischemic injury myocardial cell protection activity, do not have obvious cytotoxicity, and are expected to become effective choices for ischemic cardiomyopathy and other proteotoxic diseases.

Disclosed herein is a compound that is (R)-(2-(3-((((2-ethylbutanoyl)oxy)methoxy)carbonyl)-2-hydroxyphenyl)-1-propionamidoethyl)boronic acid citrate coordination complex, or a pharmaceutically acceptable salt or solvate thereof. Also disclosed herein are methods of treating a bacterial with a compound that is (R)-(2-(3-((((2-ethylbutanoyl)oxy)methoxy)carbonyl)-2-hydroxyphenyl)-1-propionamidoethyl)boronic acid citrate coordination complex, or a pharmaceutically acceptable salt or solvate thereof in combination with ceftibuten.

The application belongs to the technical field of organic synthesis, and particularly relates to a preparation method of 5-chloro-2-methyl-4-isothiazoline-3-ketone. N,N'-dimethyl-3,3'-dithiodipropionamide is mixed with ethyl acetate, cooled to 8-10 DEG C, and chlorine is added in stages, and the reaction is continued after the chlorine is passed; the adding mode of the chlorine is as follows: in the first stage, 25-30% of the chlorine is passed in 0.5h while maintaining the temperature of the reaction system at 10-12 DEG C; in the second stage, 25-30% of the chlorine is passed in 1h while maintaining the temperature of the reaction system at 13-14 DEG C; and in the third stage, the remaining chlorine is passed in 1.5h while maintaining the temperature of the reaction system at 15-18 DEG C. The application controls the generation of 5-chloro-2-methyl-4-isothiazoline-3-ketone by controlling the adding amount of the chlorine and the reaction temperature, and improves the yield of 5-chloro-2-methyl-4-isothiazoline-3-ketone.

The invention discloses application of a propanamide derivative in preparation of a medicine for treating nervous system diseases, and belongs to the technical field of medicines, and the propanamide derivative is N-[(6-methoxy-1H-benzimidazole-2-yl) methyl]-3-(pyridine-3-yl) propanamide. The invention discloses the neuroprotection application of the propanamide derivative for the first time by adopting the propanamide derivative to prepare a medicine for treating nervous system diseases, and the protection efficacy of the propanamide derivative is equivalent to that of a positive medicine MK-801.

The invention provides a fentanyl transdermal patch and a preparation method thereof. The fentanyl transdermal patch comprises a backing layer, a drug-containing adhesive layer and a release layer, the drug-containing adhesive layer comprises fentanyl or pharmaceutically acceptable salts thereof, and the mass percentage of 1-(2-phenethyl)-4-(N-phenylpropanamide)-piperidine-N-oxide in the drug-containing adhesive layer is less than 0.5% based on the total mass of the drug-containing adhesive layer; the method comprises the step of annealing a semi-finished product of the fentanyl transdermal patch to obtain the fentanyl transdermal patch. The method is easy to operate, the content of 1-(2-phenethyl)-4-(N-phenylpropanamide)-piperidine-N-oxide in the fentanyl transdermal patch is smaller than 0.5%, related substances of the fentanyl transdermal patch meet the quality standard, and the fentanyl transdermal patch has the advantages of being low in impurity content, high in stability and the like.

The present invention relates to a composition containing (a) a guanidine and / or an unsubstituted guanidine salt, and (b) at least one further component selected from the group consisting of 5-chloro-2-methyl-4-isothiazolin-3-one, 2-methyl-4-isothiazolin-3-one, 1, 2-benzisothiazolin-3-one, N-butyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, 2-benzisothiazolin-3-one, N-methyl-1, the cleaning agent is prepared from 2-benzisothiazolin-3-one, octyl isothiazolinone, bronopol, dibromo-nitrilopropionamide, dibromo-dicyanobutane, butyl carbamic acid iodopropynyl ester, aminomethyl propanol, aminoethyl propylene glycol, monoethanolamine, ethylhexylglycerin, hexylglycerin, 1, 2-pentanediol, 1, 2-hexanediol, 1, 2-heptanediol, 1, 2-octylene glycol, phenoxy ethanol and phenethyl alcohol. The cleaning agent is prepared from phenyl propanol, benzyl alcohol, isopropanol, ethylenediamine tetraacetic acid, (1-hydroxyethylidene) diphosphonic acid, 2-mercaptopyridine sodium oxide, 2-mercaptopyridine zinc oxide, o-phenylphenol, sorbic acid, benzoic acid, salicylic acid, lactic acid, citric acid and zinc. The invention also relates to an industrial product containing components (a) and (b), and to the use of said composition for the preservation of containers and for the preservation of industrial products. The invention also relates to the use of (a) a guanidine and / or an unsubstituted guanidine salt for improving the antimicrobial efficacy of one or more compounds selected from the group (b) described above.

The application belongs to the technical field of dental antibacterial materials, and discloses a kind of nanometer composite antibacterial coating for dental material and preparation method thereof.Method: monomer modified arginine, monomer N-isopropyl acrylamide, monomer methyl hexyl acrylate, initiator azobisdimethylamino propanamide hydrochloride, dispersing agent cetyltrimethylammonium bromide and crosslinking agent N,N-methylene bis(acrylamide) are dissolved in water, and the reaction is carried out under protective atmosphere, dialysis, to obtain nanogel dispersion;The nanogel dispersion is mixed with the nanometer zinc oxide dispersion to obtain a nanogel composite zinc oxide antibacterial coating, and a coating is formed after coating.The nanometer composite antibacterial coating for dental material has excellent retention capacity and antibacterial performance.

This invention discloses a continuous synthesis apparatus and process for chloroamines, belonging to the field of organic synthesis technology. The continuous synthesis apparatus for chloroamines includes, in series, an acetamide sodium salt reactor, an allylamide reactor, a chloroamine synthesis reactor, and an automatic phase separator. The lower liquid outlet of the automatic phase separator is connected to a solvent removal tower, and the upper liquid outlet is connected to a dealcoholization tower. A condenser and an alcohol receiving tank are connected in series at the top of the dealcoholization tower, and the bottom of the dealcoholization tower is connected to an alkalization reactor, an automatic phase separator, and a product distillation tower. This invention also discloses a continuous synthesis process for chloroamines. The equipment of this invention can accurately monitor the reaction, shorten the reaction time, significantly improve product yield and output, and ensure stable product quality.

The present application provides a preparation method of racemic nicotine, including the following steps: Nicotinyl chloride and methylamine are reacted under alkaline conditions to obtain methylnicotinamide, then condensed with monochloroacetone to obtain N-methyl-N-(2-oxopropyl) nicotinamide, then self-aldol condensed to obtain 1-methyl-5-(pyridin-3-yl)-1,2-dihydro-3H-pyrrol-3-one, and finally reduced to obtain racemic nicotine.

The invention discloses a biological catalytic synthesis method of chiral 2-amino-1-methylenepropanamide and an enzyme catalyst of the chiral 2-amino-1-methylenepropanamide. According to the present invention, one or more key amino acids in the amide hydrolase derived from Rhodococcus erythropolis AJ270 are subjected to mutation to obtain the mutant, the mutant has characteristics of high or reverse enantioselectivity when the hydrolysis reaction of the racemization 2-substituted-2-amino-1-methylene propanamide substrate is catalyzed, and the chiral compound is obtained with the high ee value; and an enantiomer of a wild type amide hydrolase catalytic product can be obtained. A method for preparing chiral 2-substituted-2-amino-1-methylene propanamide by using the mutant through biological catalysis has the characteristics of simplicity and convenience in operation, high reaction efficiency, mild reaction conditions, high enantioselectivity, easiness in product separation and high product purity, and has a very good application prospect.

2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2-oxopyrrolidin-1-yl)propanamide derivatives with R-configuration at the stereogenic center are disclosed, showing broad-spectrum protective activity in animal models of epileptic seizures, pain, depression and anxiety that are simultaneously devoid of undesirable sedative effects. Additionally, the disclosed derivatives have neuroprotective effects in the in vitro and in vivo studies.

The invention relates to a synthetic method of a compound 4-hydroxy-2-trifluoromethylpyrimidine, which comprises the following steps: by taking a compound ethyl trifluoroacetate and a compound 3-aminopropanamide as raw materials, firstly converting the raw materials into a compound 3-(2, 2, 2-trifluoroacetamido) propanamide, and then carrying out ring closing reaction to obtain the target compound 4-hydroxy-2-trifluoromethylpyrimidine. The synthetic route has the advantages of short steps, simple operation, low cost, mild reaction conditions, simple post-treatment and ideal yield, and is suitable for process amplification.

The invention relates to preparation and application of diarylamine compounds containing a propionamido indole structure. The compounds have a structural formula as shown in a general formula (I). The invention relates to a compound shown in a general formula (I), which has a strong effect of inhibiting L858R / T790M / C797S and Del19 / T790M / C797S drug-resistant mutant EGFR kinase, and also relates to application of the compound and pharmaceutically acceptable salt thereof in preparation of drugs for treating and / or preventing diseases caused by drug-resistant mutation of EGFR kinase, the invention particularly relates to application in preparation of medicines for treating and / or preventing cancers. The invention also provides a preparation method of the compounds, a pharmaceutical composition containing the compounds and application of the pharmaceutical composition. The compound is especially used for preparing drugs for treating and / or preventing lung cancer, and has good antitumor drug development and application prospects. (I)

Proposed mixtures comprise a selected cooling agent (E)-3-benzo[1,3]dioxol-5-yl-N,N-diphenyl-2-propenamide and at least one further substance acting as a solvent for (E)-3-benzo[1,3]dioxol-5-yl-N,N-diphenyl-2-propenamide, wherein the substance is selected from the group consisting of benzyl alcohol, 2-phenylethanol, benzyl benzoate, diethyl succinate, triethyl citrate, triacetin, ethanol, peppermint oil, anethole, optamint, propylene glycol, further cooling agents or mixtures thereof.

Provided is a therapeutic or prophylactic agent for pain or interstitial cystitis comprising N-[2-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl) propanamide or a pharmaceutically acceptable salt thereof.

The application relates to the technical field of drug synthesis, in particular to a synthesis method and application of a 2-(cyclopropylamide)thiazole-4-amide derivative. The thiazole structure is shown in formula I. The preparation method of the 2-(cyclopropylamide)thiazole-4-amide derivative is as follows: the compound shown in formula I is obtained by reacting the compound shown in formula II in the presence of HATU, DIPEA, a primary amine or a secondary amine and tetrahydrofuran. The 2-(cyclopropylamide)thiazole-4-amide derivative has the effect of relieving Alzheimer's disease, and is characterized by strong cholinesterase inhibition activity.

Disclosed herein are crystalline forms of ((2-Ethylbutanoyl)oxy)methyl(R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate. Also disclosed herein are methods of treating a bacterial with a crystalline form of ((2-Ethylbutanoyl)oxy)methyl(R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate.

The application discloses a preparation method of bacteriostatic and deodorant plastic and relates to the technical field of plastics. The self-prepared antibacterial agent is prepared by using triethoxysilane butyraldehyde, 4-chloro-1-butylamine and (R)-2-(dimethylamino) propionamide, the Schiff base structure and the quaternary ammonium structure in the molecular chain of the self-prepared antibacterial agent interact, bacterial growth is effectively inhibited, and then the antibacterial and deodorant properties of the plastic are improved; then porous calcium silicate and porous calcium carbonate are used as deodorant fillers of the plastic, the self-prepared antibacterial agent is used as a crosslinking agent, the fillers and the urea-formaldehyde resin are combined with each other, the uniform dispersion of the fillers is facilitated, meanwhile, a crosslinked network structure is formed in the plastic, and the mechanical properties of the plastic are greatly improved.

The invention discloses a treatment method of a florfenicol by-product N, N-diethyl-2, 3, 3, 3-tetrafluoropropionamide, and belongs to the technical field of chemical engineering, the treatment method comprises a hydrolysis addition reaction and a cyclization reaction; the hydrolysis addition reaction comprises the following steps: mixing N, N-diethyl-2, 3, 3, 3-tetrafluoropropionamide with diethylamine and alkali liquor, and then carrying out hydrolysis reaction and addition reaction to obtain N, N, N ', N'-tetraethyl malonamide; the cyclization reaction comprises the following steps: mixing organic solvent solutions of N, N, N ', N'-tetraethyl malonamide and sodium methoxide, adding a mixed solution of formamidine and an organic solvent, carrying out reflux heat preservation reaction, evaporating materials to dryness, acidifying and filtering. According to the method, the malonamide intermediate is generated through fewer reaction steps, then the 4, 6-dihydroxypyrimidine is prepared, most of materials can be recycled, the atom economy is high, and the pollution to the environment and the post-treatment pressure are also reduced.