85 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.

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 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 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.

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)

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.

The invention relates to the technical field of concrete admixtures, in particular to a micro-crosslinking type water-retaining agent for inhibiting delayed bleeding of concrete and a preparation method of the micro-crosslinking type water-retaining agent. The water-retaining agent takes dodecanoic acid containing halogen and hydroxyl as a raw material to synthesize a 13-membered ring lactone intermediate, the 13-membered ring lactone intermediate reacts with straight-chain saturated dicarboxylic acid to form a linear polyester chain intermediate with an alternating repeating unit, and then 3-aminopropanamide and linear polyethyleneimine are added to prepare the water-retaining agent. The linear polyethyleneimine and halogen atoms in 13-membered ring lactone on a linear polyester chain intermediate are subjected to nucleophilic substitution reaction, linear polyethyleneimine is used as a cross-linking agent and subjected to nucleophilic substitution with halogen atoms on different polyester chains through primary amine groups at the two ends of the linear polyethyleneimine, and finally the micro-cross-linking type water-retaining agent is formed. According to the micro-crosslinking type water-retaining agent, the problems of segregation, bleeding and pump blockage in the middle and later periods of concrete premixing are remarkably solved on the premise that the workability of concrete in the early stage of premixing is not influenced, meanwhile, the air content of the concrete is not influenced, and the negative influence on the strength of the concrete is avoided.

The invention relates to the field of food, in particular to an antioxidant and application thereof in food preparation. The invention provides application of N-[2-(3, 4-dimethoxyphenyl) ethyl]-3, 4-dimethoxycinnamic acid amide and / or 3-[(4-amino-2, 2-dioxo-1H-2, 1, 3-benzothiadiazine-5-yl) oxygen]-2, 2-dimethyl-N-propyl propionamide in any of the following items: N-[2-(3, 4-dimethoxyphenyl) ethyl]-3, 4-dimethoxycinnamic acid amide and / or 3-[(4-amino-2, 2-dioxo-1H-2, 1, 3-benzothiadiazine-5-yl) oxygen]-2, 2-dimethyl-N-propyl propionamide. Oxidation resistance; and / or preparing an antioxidant. The antioxidant composition disclosed by the invention has a remarkable protection effect on food containing fat and other photosensitive components, can prevent fat oxidation and attenuation of nutritional components, and keeps fresh sensory experience and nutritional and healthy properties of the food.

This application relates to a method for preparing (S)-2-((3-((benzo[d][1,3]dioxopenta-5-oxy)methyl)benzyl)-amino)propionamide of formula I or a pharmaceutically acceptable salt thereof, and also to an intermediate for preparing the compound. This method is low-cost, simple to operate, safe and environmentally friendly, exhibits high reaction selectivity and high yield, and is suitable for large-scale industrial production.

The application provides a preparation method of chiral alpha-hydroxy-amidoxime ether and belongs to the technical field of organic synthesis. The preparation method of the chiral alpha-hydroxy-amidoxime ether comprises the following steps: S1, protecting the hydroxyl group of chiral alpha-hydroxy propionamide by a protecting group; S2, sequentially reacting the chiral alpha-protecting group-propionamide with an oxonium salt donor and an alkoxyamine hydrochloride to prepare chiral 1-[(E)-alkoxyimino] alpha-protecting group-prop-1-amine; and S3, removing the protecting group from the chiral 1-[(E)-alkoxyimino] alpha-protecting group-prop-1-amine to prepare a product. The application aims to overcome the core defects of a low yield, a high impurity content, a big reagent safety and environmental protection risk, a high pyridine consumption and a complicated operation of an existing process, and develop a new chiral alpha-hydroxy-amidoxime ether synthesis process with high yield, high purity, low cost, high safety and suitability for industrial amplification.

The present invention encompasses a microcrystalline form of (R)-2-(N-[4-amino-5-(4-methoxybenzoyl) thiazol-2-yl]-4-fluoro-anilino) propanamide (I), and a process for the preparation thereof, as well as a pharmaceutical composition comprising the same. The present invention also encompasses a process for the preparation of (R)-2-(N-[4-amino-5-(4-methoxybenzoyl) thiazol-2-yl]-4-fluoro-anilino) propanamide.

The invention relates to the technical field of pesticide preparations, and particularly discloses a potato seed dressing agent with a disease-resistant function, which is prepared from the following raw materials in parts by weight: 8 to 12 parts of N-methoxy-N-o-tolyl-3-(furyl) propanamide, 5 to 8 parts of eugenol polyoxyethylene ether derivatives, 3 to 5 parts of salicylic acid glucoside, 6 to 10 parts of cationized modified chitosan and 2 to 4 parts of EDTA (Ethylene Diamine Tetraacetic Acid) chelated zinc. The preparation method comprises the following steps: treating raw materials; capsule preparation; mixing and granulating; and drying and screening. N-methoxy-N-tolyl-3-(furyl) propanamide is adopted to directly act on a key metabolic link of pathogenic bacteria, a plant-derived derivative plays a broad-spectrum antibacterial role, an inductive component activates a disease-resistant mechanism of potatoes, and meanwhile, cationized modified chitosan and other auxiliary components cooperate with each other, so that slow release of active components is realized, and the disease resistance of the potatoes is improved. The pathogenic bacteria are difficult to generate drug resistance, and the prevention and control effect is long-term and stable.

The invention discloses an anti-tumor application of a thiazole compound, and belongs to the technical field of medical chemistry. The thiazole compound is 3-[(4-fluorophenyl) thio]-N-[4-(pyridine-2-yl) thiazole-2-yl] propanamide, and the English name of the thiazole compound is 3-((4-fluoropheyl) thio)-N-(4-(pyridin-2-yl) thiazol-2-yl) propanamide. The structural formula of the thiazole compound is shown in the description. The invention provides the thiazole compound with broad-spectrum anti-tumor activity, the compound has relatively strong inhibitory activity on clinical refractory breast cancer, osteosarcoma, colorectal cancer, liver cancer and lung cancer, and a new candidate compound is provided for broad-spectrum anti-tumor drugs.

The present disclosure provides suspendable ophthalmic solutions with excellent redispersibility. The present disclosure provides an aqueous suspension agent comprising (E)-2-(7-trifluoromethylchroman-4-ylidene)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide or a pharmaceutically acceptable salt or solvate thereof, a cellulosic polymer, and a nonionic surfactant.

Examples of a biocide composition include an activated halogen compound selected from the group consisting of 2,2-dibromo-3-nitrlopropionamide; 2-bromo-2-nitropropane-1,3-diol; and 1,2-dibromo-2,4-dicyanobutane; benzisothiazolin-3-one; a pyridine-N-oxide selected from the group consisting of zinc pyrithione and sodium pyrithione; and a carbamate derivative selected from the group consisting of 3-iodo-2-propynyl butyl carbamate; zinc bis(dimethyldithiocarbamate); and bis(dimethyl carbamoyl) disulfide.

The invention relates to an androgen receptor antagonist with a disubstituted-N-(substituted polynary fused cyclo-2-yl) propanamide structure as well as a preparation method and application of the androgen receptor antagonist, the androgen receptor antagonist is shown in a general formula I, and the androgen receptor antagonist inhibits growth and proliferation of prostate cancer cells by inhibiting AR activity and blocking an androgen signal channel. Compared with the traditional AR antagonist, the novel compound provided by the invention has a novel action mechanism, and effectively overcomes the problem of drug resistance of the existing drug.

This disclosure provides a means for treating dry eye. This disclosure can provide: a composition for use in treating dry eye; and a use thereof. The composition includes (E)-2-(7-trifluoromethyl-chroman-4-ylidene)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalene-1-yl)acetamide, a pharmaceutically acceptable salt thereof, or a solvate thereof. This disclosure can provide: a composition for treating dry eye; and a use thereof. The composition includes a Vi / Vc zone inhibitor.

The invention belongs to the technical field of biological medicines, and particularly relates to a benzoborazole 7-position propanamide derivative as well as a preparation method and medical application thereof. The benzoborazole 7-position propionamide derivative provided by the invention has better activity of inhibiting tumor cell proliferation, can effectively inhibit the proliferation of ovarian cancer tumor cells, has the half inhibitory concentration (IC50) of nanomole level, has higher activity, solves the technical problem of insufficient antitumor activity of the compound, and has good application prospects. A promising candidate compound is provided for developing novel efficient antitumor drugs, and the compound is simple in synthesis process and low in cost.

This invention discloses a compound for preparing an antiviral drug, its preparation method, and its application, relating to the field of antiviral drug technology. The compound is obtained through a three-step organic synthesis: first, condensation of tert-butyloxycarbonyl-phenylalanine with p-fluorobenzylamine yields tert-butyl(1-((4-fluorobenzyl)amino)-1-oxo-3-phenylprop-2-yl)carbamate; then, deprotection with trifluoroacetic acid yields 2-amino-N-(4-fluorobenzyl)-3-phenylpropionamide; finally, sulfonylation with 5-bromothiophene-2-sulfonylchlorosulfonation gives the final product. This compound specifically targets the influenza virus HA protein, blocking viral invasion of host cells, exhibiting broad-spectrum antiviral activity against influenza A and B viruses, low cytotoxicity, and a mild and controllable preparation process. It can be used to prepare drugs for the prevention and treatment of influenza virus infection, providing a new candidate for the development of new antiviral drugs.

The invention discloses a synthesis method and application of (3S)-1, 3-dimethyl piperazine-2-ketone, and the method comprises the following steps: S101, dissolving D-alanine methyl ester hydrochloride in a first organic solvent, then adding alkali A and 2-methylaminoethanol, after addition, heating to 60-150 DEG C, carrying out stirring reaction for 8-20 hours, after the reaction is completed, carrying out first post-treatment on the reaction liquid, and carrying out second post-treatment on the reaction liquid, so as to obtain the (3S)-1, 3-dimethyl piperazine-2-ketone; the crude product of (R)-2-amino-N-(2-hydroxyethyl)-N-methyl propionamide is obtained; and S102, dissolving (R)-2-amino-N-(2-hydroxyethyl)-N-methylpropanamide in a second organic solvent, then adding (1, 2-bis (ethoxycarbonyl) hydrazino) triphenylphosphonium trifluoromethanesulfonate and alkali B, after addition, carrying out stirring reaction at 15-40 DEG C for 8-20 hours, and after the reaction is completed, carrying out secondary post-treatment on the reaction liquid to obtain the target (3S)-1, 3-dimethyl piperazine-2-ketone.

A continuous process to prepare N-(4-chloro-2-(pyridin-3-yl)thiazol-5-yl)-N-ethyl-3- (methylsulfonyl)propanamide (S2) is provided.

The present invention provides a compound containing a 2-methyl-2-(3-(piperidin-3-yl)phenoxy)-2-methylpropanamide skeleton. Specifically, the present invention provides a compound represented by Formula I or Formula II, or a pharmaceutically acceptable salt thereof. The compound represented by Formula I or Formula II of the present invention has excellent inhibitory activity against BCL9 / β-catenin interaction. Formula (I): JPEG2026503067000129.jpg3599 formula (II): JPEG2026503067000130.jpg35109

Disclosed in the present invention are a 4-sulfamoylphenylpropanamide compound and the use thereof. Provided in the present invention are a compound as represented by formula (I), an isotopically labeled substance thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a solvate of the pharmaceutically acceptable salt thereof, or a prodrug thereof. The compound can promote ALP expression in osteoblasts, exhibit a relatively good activity for promoting osteoblast differentiation, and has potential therapeutic effects in promoting bone anabolism and treating bone-related diseases.