227 results about "Acetamido-CNU" patented technology

The invention discloses a synthesis method of a pharmaceutical intermediate of tertiary butyl-(2-(biphenyl-4-yl)-1-(methylol) ethyl) carbamate, which comprises the steps that: diethyl acetamidornalonate and 4-substituent biphenyl are taken as initial raw materials and undergone six steps of reactions including condensation, decarboxylation, hydrolysis, reduction and acylation to obtain the tertiary butyl-(2-(biphenyl-4-yl)-1-(methylol) ethyl) carbamate. The method of the invention has the advantages of available raw materials, convenient operation, high reaction yield rate, recoverable solvents used in the synthesis course, thereby reducing environmental pollution and greatly reducing production cost; according to test results, the products obtained by the method has reliable quality and stable performance.

The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and / or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.

Disclosed herein is the crystalline form of the potassium salt of 2-((3R,6S)-2-hydroxy-3-(2-(thiophen-2-yl)acetamido)-1,2-oxaborinan-6-yl)acetic acid. The crystalline form maybe formulated for treating subjects with bacterial infection. Accordingly, some embodiments relate to compositions and methods of administering the potassium salt of 2-((3R,6S)-2-hydroxy-3-(2-(thiophen-2-yl)acetamido)-1,2-oxaborinan-6-yl)acetic acid.

The present invention relates to acetamido glucose derivatives of indomethacin and their synthesis process and use. The kinds of acetamido glucose derivatives of indomethacin prepared with indomethacin and acetamido glucose are 1-O-[1-(4-chloro-benzoyl)-5 -methoxy-2-methyl-3-indolyl-acetoxy]-2-acetylamino-2-deoxy-alpha-D-glucose and 6-O-[1-(4-chloro-benzoyl)-5-methoxy-2-methyl-3-indolyl-acetoxy]-2-acetylamino-2-deoxy-alpha-D-glucose. The derivatives of the present invention has the activity of inhibiting mouse ear dropsy caused by croton oil and may be used in preparing antiphlogistic medicine.

The invention provides an improved synthesis method of iodixanol and macroporous adsorbent resin chromatography column purification and solvent recrystallization purification processes which are easy to be used for industrialization. In the synthesis method, iodixanol is synthesized by dimerisation of 5-acetamido-N, N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide ('Compound A'), wherein hydroxyacid containing boron or borate and the like are used to form a buffer solution for controlling the pH value of a reaction process, thus side reactions such as excessive alkylation and the like are effectively inhibited and the transformation ratio for transforming into the iodixanol is improved, the crude product containing 85-90% of iodixanol is obtained and then is purified by a macroporous adsorbent resin chromatography column, the total recovery of the iodixanol is 90-95%, the purity of the iodixanol is more than 97%; and the iodixanol is subjected to recrystallization in a solvent containing 2-methoxy ethanol, the recovery of the iodixanol is 90-95%, and the purity of the iodixanol is more than 99%.

The invention discloses a method for treating organic waste acids in p-acetamidobenzene sulfonyl chloride synthesis, and the method comprises the following steps: (a) pumping the organic waste sulfuric acids into a macroporous resin bed, and carrying out organic matter adsorption interception to obtain a sulfuric acid solution; (b) mixing the sulfuric acid solution with an oxidant, introducing themixture into an oxidation reactor, carrying out oxygenolysis, and decolorizing to obtain purified sulfuric acid, wherein the oxidant is hydrogen peroxide or ozone, and the mass ratio of the oxidant to the sulfuric acid solution is (0.02-0.15): 1; (c) carrying out backwashing desorption on organic matters adsorbed by the resin in the macroporous resin bed by using a backwashing solvent to obtain an eluent; and (d) introducing the eluent into an evaporator to evaporate and recover the solvent, treating the obtained product by a dryer, and recycling. The obtained product is directly used for sulfonation reaction and is used for sale or downstream sections.

The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and / or prevention of diseases and also to their use for the production of medicaments for the treatment and / or prevention of diseases, more particularly for the treatment and / or prevention of cardiovascular disorders.

The invention discloses a method for producing m-acetamino-N,N-diethyl aniline, which comprises the following steps: (1) mixing m-phenylenediamine, glacial acetic acid and hydrobromic acid to perform an acylation reaction to obtain an acetylated compound; (2) performing ethylation of the acetylated compound and bromoethane, and after the reaction is finished, diluting and filtering the reaction system, and eluting the product filtered out to obtain m-acetamino-N,N-diethyl aniline; (3) concentrating mother solution produced by filtration and elution in the step (2); and (4) dripping sulfuric acid and ethanol into the mother solution to perform an reaction to obtain bromoethane and collecting the bromoethane for use in the ethylation in the step (2). The production method of the invention has the advantages that: the active ingredients in waste water produced in production are fully used; the recycling of the waste water reduces cost; and clean production is realized.

A process for preparation of 7-[D-α-amino-α-(4-hydroxyphenyl)acetamido]-3-(1-propen-1-yl)-3-cepham-4-carboxylic acid viz. Cefprozil of formula (I) igh purity, substantially free of impurities, which comprises preparation of mixed acid anhydride by selecting the sequence and temperature of addition of the reagents and its subsequent condensation with a protected 7-APCA; followed by hydrolysis, isolation and purification to give Cefprozil of formula (I) in the form of a monohydrate.

The invention discloses a medicine composition containing aspirin, acetaminophen and caffeine and a preparation method thereof. The medicine composition includes aspirin particles and acetaminophen-caffeine particles, wherein the aspirin particles are prepared by the following compositions by parts of weight: 25 parts of aspirin, 1.8-2.2 parts of microcrystalline cellulose, 0.8-1.2 parts of polyvinylpolypyrrolidone and 0.13-0.15 part of silica; and the acetaminophen-caffeine particles are prepared by the follow compositions by parts of weight: 25 parts of acetaminophen, 6.5 parts of caffeine, 2.3-2.7 parts of microcrystalline cellulose, 0.3-0.7 part of polyvinylpolypyrrolidone and 0.12-0.16 part of silica. The preparation method respectively performs dry palletizing on the aspirin, the acetaminophen and the caffeine and proper accessories, effectively prevents the aspirin from directly contacting with moisture in the air, prevents the acetaminophen from quickening degradation of the aspirin and obviously improves stability of the aspirin contained in the prepared medicine composition.

The invention relates to a process for producing p-acetamidobenzene sulfonyl chloride. The process comprises: adding chlorosulfonic acid and antifebrine into acetanilide serving as a raw material to perform chlorosulfonation to obtain sulfonated oil; adding water into the obtained sulfonated oil to perform a hydrolysis reaction; subjecting the product of the hydrolysis of sulfonated oil to vacuum filtration; circularly absorbing one hydrogen chloride gas product to prepare diluted hydrochloric acid; and dissolving the other p-acetamidobenzene sulfonyl chloride product in a dissolving kettle, crystallizing, centrifuging and drying to obtain finished p-acetamidobenzene sulfonyl chloride. The process is characterized in that: dichloroethane is added in the dissolution process as a solvent, the finished product obtained after centrifugation is dried by air flow and then packed under vacuum, and thus, the finished product is obtained. In the production process disclosed by the invention, the mass ratio of the added dichloroethane solvent and the acetanilide raw material is (4-8):1, air flow is used for drying, the quality guarantee period of the prepared finished product is as long as 180 days, and the finished product is more stable.

A novel substituted N-acetyl-L-cysteine (NAC) derivative and methods of using this compound for the treatment of diseases and / or conditions, including but not limited to diseases and / or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

The invention belongs to the technical field of medicine, and in particular relates to a process for producing memantine hydrochloride. The process for producing the memantine hydrochloride comprises the steps of performing acetyl amination reaction on 1-bromo-3,5-dimethyladamantane and acetonitrile at 5-10 DEG C under the action of concentrated sulfuric acid to obtain 1-acetamino-3,5-dimethyladamantane; performing hydrolysis reaction on the 1-acetamino-3,5-dimethyladamantane and polyol which does not contain an ether bond under an alkali condition to obtain 1-amino-3,5-dimethyladamantane; and acidifying the 1-amino-3,5-dimethyladamantane with hydrochloric acid, and performing re-crystallization to obtain the high-purity memantine hydrochloride. The process for producing the memantine hydrochloride, disclosed by the invention, has the advantage that the product yield of the memantine hydrochloride is increased by controlling process parameters and changing process conditions based on an existing synthetic process.

Described herein are crystalline forms of (R)-3-(2-(trans-4-(2-aminoethylamino)cyclohexyl)acetamido)-2-hydroxy-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylic acid. In some embodiments, the crystalline forms are formulated for treating a subject in need thereof with a bacterial infection.

3-acetamido-5-acetylfuran as a biomass-based nitrogen-containing platform compound can be used for synthesizing a plurality of important nitrogen-containing fine chemicals. The invention discloses a method for preparing the 3-acetamido-5-acetylfuran by taking chitin monomer N-acetylglucosamine as a raw material. The method is accomplished by the following means: the N-acetylglucosamine is taken asthe raw material, glycine ionic liquid is taken as a catalyst, calcium chloride is taken as a cocatalyst, N, N-dimethylacetamide is taken as a solvent, reaction is carried out for a certain period oftime at a certain temperature, the yield of the obtained product is as high as 52.61%, and in addition, the ionic liquid still shows good catalytic activity after being repeatedly used for eight times. The chitin monomer used in the method is cheap, easy to obtain and renewable, and the application field of chitin biomass is broadened. The ionic liquid used in the reaction is simple in preparation method, cheap and easily available in raw materials, recyclable, green and environment-friendly, and has a good industrial application prospect.

A novel substituted N-acetyl-L-cysteine (NAC) derivative and methods of using this compound for the treatment of diseases and / or conditions, including but not limited to diseases and / or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

The invention discloses a method for preparing 2-amino-4-acetamido anisole, and belongs to the field of organic chemistry synthesis. 2,4-dinitrobenzene methyl ether is adopted as raw materials, reduction is carried out through hydrazine hydrate under the action of diacetone catalysts to obtain mixed liquor of 2,4-dinitrobenzene methyl ether-solvents, then after acetylation is carried out under the action of acetic anhydride, reduced pressure distillation and recycling are carried out on the solvents, and the product of 2-amino-4-acetamido anisole is obtained after filtering and drying. The method has the advantages that the yield is high, the effect is good, environmental protection is achieved, the requirement for equipment is not high, and the method is easy and convenient to operate, and the good industrialized application value is achieved.

The invention discloses an isoflavone derivative modified by acetylaminoacid benzyl ester of a general formula Ia-q, in which R1, R2 and R3 are all CH2CO-AA-OBzl or both R1 and R2 are all CH2CO-AA-OBzl, while R3 is H, wherein the AA in the CH2CO-AA-OBzl is selected from glycin, lactamine, phenyl alanine, tryptophan, isoleucine, leucine, valine, aspartic acid and glutamic acid. The invention also discloses a preparation method of the isoflavone derivative modified by the acetylaminoacid benzyl ester of the general formula Ia-q. The invention adopts an S180 mouse model to evaluate the antitumor effects of the isoflavone derivative modified by the acetylaminoacid benzyl ester of the general formula Ia-q, thus indicating that the isoflavone derivative has excellent antitumor activity and can be used as an antitumor agent.

3-acetamido-5-acetylfuran is an important platform compound, and is a precursor for preparing fine chemicals; a large amount of chitin exists in nature and chitin is natural and renewable; and N-acetylglucosamine taking as a monomer of chitin has a promising application prospect. According to the invention, N-acetylglucosamine is used as a raw material, an ionic liquid is taken as a catalyst, a small amount of a metal salt and boric acid are added as cocatalysts, N, N-dimethylacetamide is used as a solvent to efficiently convert N-acetylglucosamine under normal-pressure reflux condition to obtain 3-acetamido-5-acetylfuran, the conversion process is realized by one-step method, a reaction system is green and efficient, and research in the field of chitin biomass is widened.

The invention discloses a method for synthesizing 2-(N-4-methyl benzyl) methoxy-acetamido methyl isobutyrate. The method is characterized by comprising the following steps of: mixing p-methyl iminobenzyl methyl acetate, N,N-dimethylformamide and tetrabutylammonium iodide, saturating carbon dioxide under normal pressure, performing electrical carboxylation reaction under the condition of constant current, esterifying and purifying to obtain the 2-(N-4-methyl benzyl) methoxy-acetamido methyl isobutyrate. Compared with the prior art, the method has the advantages of simple process, convenience for operation, safety and readily available raw materials; and the carbon dioxide serving as greenhouse effect gas is utilized effectively, atmospheric pollution is reduced greatly, and the conversion of aromatic imine compounds and the effective synthesis of N-carboxylation products are realized simultaneously, so the method is a process route with industrial synthetic value.

The invention discloses a preparation method of (6S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole (formula I). The compound is an intermediate of a drug pramipexole hydrochloride (formula II) for treating Parkinson's diseases. The formula I and formula II are shown in the description. The preparation method comprises the steps of taking 4-acetamino cyclohexanone as an initial raw material; then subjecting 4-acetamino cyclohexanone to bromination and condensation cyclization with N-bromobutanimide and urea in glacial acetic acid; removing acetyl by hydrolysis; and then carrying out alkaline aqueous solution ionization and L-(+)-tartaric acid resolution to obtain a target compound. Compared with an original preparation method, the preparation method provided by the invention omits use of strong oxidizing and corrosive reagents such as potassium dichromate, concentrated sulfuric acid and bromine, changes two reaction steps of sodium hydroxide ionization and chiral resolution into a one-pot method, thereby reducing operation steps and increasing yield.

The invention discloses a compound (I) P-N-methyl acetamidophenyl rhodamine 6G pH fluorescence molecular probe as well as a preparation method and use thereof. Under the action of hydrogen ions, the rhodamine 6G lactam spiral ring in the probe molecule (I) is opened in ring from closed state, and the color of the solution is obviously changed from achromatic color to orange red with fluorescence-emission; and furthermore, fluorescent light can be given off under the action of exciting light with a certain wavelength. The compound I can be used for high-sensitivity naked eye color identification for hydrogen ions and also used as a fluorescent identifying probe.

The invention discloses an aporphine type alkaloid and a preparation method thereof. The compound is 8-acetamido-isocorydine, which is prepared through the nucleophilic substitution reactions between 8-amino-isocorydine, and the chemical structure formula of the compound is represented in the description. Through a Kunming white mouse tumor xenograft model, the results show that the provided alkaloid has a strong effect on inhibiting the tumor growth in body and has a good antitumor activity.

The invention provides a acetaminophen pharmaceutical composition preparation and a preparation method thereof. The preparation method comprises the following steps: uniformly mixing acetaminophen, crospovidone, povidone K30, methylparaben, ethylparaben and propyl hydroxybenzoate, and adding a binding agent aqueous solution to pelletize; drying through a gradient variable-temperature method afterpelletizing, controlling the temperature of each gradient to 20-40 DEG C, adding alginic acid, calcium carbonate and colloidal silicon dioxide to pre-mix for 3-5 minutes after drying, adding magnesiumstearate to mix for 3-5 minutes, and tabletting and covering. The preparation method for the acetaminophen pharmaceutical composition preparation is simple in operation step, and is gentle in operation condition; and the preparation method can realize quick dissolving-out of effective ingredients in the preparation, increases a dissolution rate, and is worthy of being widely popularized and applied.

The invention discloses a preparation method for 5-acetoacetamidobenzimidazolone. The preparation method comprises the following steps: with water as a solvent, adding 5-aminobenzimidazolone, a sodiumhydrosulfide solution and active carbon into the water, carrying out mixing, carrying out a reaction at a certain temperature for a certain period of time, and carrying out filtering so as to obtainan intermediate filtrate; and dropwise adding diketene into the intermediate filtrate at a certain temperature, keeping the temperature for a certain period of time, and carrying out cooling, filtering and drying so as to obtain the 5-acetoacetamidobenzimidazolone. According to the invention, by adoption of the sodium hydrosulfide solution, dissolution of the 5-aminobenzimidazolone can be accelerated, and oxidation of the 5-aminobenzimidazolone can be prevented; H2S gas generated by hydrolyzing of the sodium hydrosulfide at a high temperature can generate the sodium hydrosulfide solution afterbeing absorbed by the sodium hydroxide solution, so the H2S can be recycled, and emission of waste gas is avoided; the water is used as the solvent, so the cost of alcohol used as the solvent is reduced, the potential safety hazard during product drying is avoided, and the reaction time is short. The preparation method provided by the invention has the following advantages: a product purity is larger than or equal to 99.2%; the yield of the product is larger than or equal to 85%; the quality is guaranteed; and the yield is improved.

The invention discloses a biphenyl acetate n-acetamido-phenolic ester compound and preparing method with active component as drug composition, which comprises the following steps: adopting biphenyl acetate and thionyl chloride as raw material to prepare biphenyl acetyl chloride; reacting biphenyl acetyl chloride and n-acetamido-phenolic ester to produce rough crystal of product; recrystallizing to obtain the product.