52 results about "2-Oxazolidone" patented technology

The invention discloses a method for preparing 5(S)-aminomethyl-3-aryl-2-oxazolidinone. The method comprises the following steps of: reacting (S)-glycidyl phthalimide and aryl aniline to prepare an addition compound; and finally preparing the 5(S)-aminomethyl-3-aryl-2-oxazolidinone through cyclization reaction and aminolysis reaction. The method has the advantages of high total yield and low cost; all intermediates and a product synthesis method have the characteristics of convenience in recovery and purification; and the purity of a final product of the method is at least over 99.9 percent.

The invention relates to a medicine producing field, specifically, to an improved producing method of antibacterial medicine nifuratel. The method makes use of thiourea as initial material to produce nifuratel. The improvement is that it is no longer to use methyl mercaptan or methomyl in the known method while producing the intermediate 2-(methylthiomethyl)hydropropane. Furthermore, the invention is no longer to use metal natrium in the known method when the 3-methylthio-2-hydroxy-propylhydrazine and diethyl carbonate are heated to produce N-amido-5-methylthiomethyl-2-oxazolidone in the existance of alkali. All of the improvements largely improve the preparation of the nifuratel, especially for the production condition in a large scale, reduce the environment pollution and benefit to ensure the production safety.

The present invention discloses the preparation process of one kind of chiral 4-substituent-2-oxazolidone. The preparation process includes the first reducing chiral amino acid into alcohol in the presence of Lewis acid and catalyst metal boron compound, the subsequent acylation with acyl chloride compound and no phosgene, and cyclization in buffering solution with strong alkali catalyst. The present invention has low cost, less reaction steps, less wastes produced, high product quality and high total yield, and is suitable for industrial production.

The invention discloses a nifuratel with a optical activity. Specifically, the invention provides a (S)-nifuratel, i.e. (S)-5-[(methylthio)methyl]-3-[(5-nitryl-2-furan)methylene]amido]-2-oxazolidone, the producing method and the combination including the optical activity compound. Compared to the racemic nifuratel, (S)-nifuratel has a better anti-inflammatory and anti-fungi activity. The invention also discloses the producing method for (S)-nifuratel which has the (S)-chloroepoxy propane as initial material, adopts the 3-dimension and selective synthesis method and produce a high optical purity (S)-nifuratel with a high yield.

The invention relates to a method for preparing nifuratel. The method comprises the steps of (1) synthesizing 2-(methylmercapto-methyl)-oxacyclopropane through epoxy chloropropane and sodium methyl mercaptide; (2) generating reaction between hydrazine hydrate and the 2-(methylmercapto-methyl)-oxacyclopropane to synthesize 3-methylmercapto-2-hydroxy-propyl hydrazine; (3) generating reaction between diethyl carbonate and 3-methylmercapto-2-hydroxy-propyl hydrazine to prepare N-amino-5-methylmercapto-methyl-2-oxazolidinone; (4) hydrolyzing 5-nitrofuran formaldehyde diacetate ester under an acidic condition to prepare 5-nitro-2-furaldehyde; (5) generating reaction between the 5-nitro-2-furaldehyde and the N-amino-5-methylmercapto-methyl-2-oxazolidinone obtained in the step (3) to obtain the nifuratel, wherein in the step (1), 15-crown ether-5 is used as a catalyst, so that the conversion rate is high; no organic solvent is used during posttreatment of a product, and the posttreatment is simple.

The invention discloses a chemiluminescence detection kit of furazolidone metabolin, comprising a detection plate and a reagent, wherein the reagent comprises an antibody and a detection target standard solution, wherein the detection target is a p-nitrobenzene derivative 4-NPAOZ of furazolidone metabolin 3-amino-2-oxazolidone. The detection kit of the furazolidone metabolin not only can realize the fast and mass detection, but also has very high specificity and sensitivity, and achieves the detection sensitivity of 0.005 ppb.

Free halogen sources (e.g., sodium hypochlorite and chlorine) added as slimicides in high organic component process streams such as pulp and paper processing are rendered more efficacious by the addition of selected N-hydrogen compounds (namely, 5,5-dimethylhydantoin, 5-ethyl-5-methylhydantoin, cyanuric acid, succinimide, urea, 4,4-dimethyl-2-oxazolidinone, and glycouril) to the process stream. The latter compounds may be added to the process stream before or after the slimicide is added or combined with the slimicide and added directly thereto. The direct use of halogenated hydantoins has also been found to provide improved efficacy relative to free halogen sources. In addition, absorbable organic halogen by-products are reduced.

The invention discloses preparation and application of an N-heterocyclic carbene gold porous organic polymer. The preparation has the characteristics as follows: alkenyl-functionalized 1,3-bis(p-vinylbenzyl) imidazole carbene gold monochloride (I) is subjected to a polymerization reaction with divinyl benzene, azodiisobutyronitrile and N,N-dimethylformamide at the temperature of 70-100 DEG C, theN-heterocyclic carbene gold porous organic polymer is obtained, the porous organic polymer is taken as a catalyst in the cyclization reaction of CO2 and propynylamine compounds for synthesis of 2-oxazolidone compounds, and the catalyst obtained by filtering can be reused after being washed and dried. Compared with the prior art, the technology is simple, the synthesis period is short, the reaction process is low in toxicity and good in repeatability, the prepared N-heterocyclic carbene gold porous organic polymer has the advantages of adjustable specific surface area and pore volume and highcatalytic activity, is easy to separate, can be recycled and has great development potential and application prospect in the field of heterogeneous catalysis.

The present invention discloses preparation of nitrogen containing carbonyl compound, and is especially the process of preparing carbamate, urea and their derivatives as well as 2-oxazolidone through oxidizing and carbonylating organic amine compound in the presence of one kind of multifunctional catalyst. By using salt of VIII metal and Cu as main metal catalyst and the ionic solution of halogenated pyridine salt, quaternary ammonium salt or quaternary phosphate salt as co-catalyst and through oxidizing and carbonylating organic amine compound, carbamate, urea and their derivatives as well as 2-oxazolidone may be prepared at oxygen pressure of 0.2-1.0 MPa, CO pressure of 1.0-4.0 MPa, reaction temperature of 80-220 deg.c, and in reaction time of 0.5-4 hr. Compared with the technological process adopting traditional catalyst, the present invention has the advantages of simple system, easy preparation, mild reaction condition and high selectivity.

This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.

The invention discloses a safe environment-friendly ink detergent. The invention is characterized in that the detergent is prepared from the following raw materials in parts by weight: 4-5 parts of polyoxyethylene sorbitan fatty acid ester, 4-5 parts of polyoxyethylene castor oil, 6-8 parts of acetone, 4-6 parts of ethyl acetate, 2-3 parts of sodium gluconate, 1-2 parts of triethanolamine, 3-4 parts of isopropyl myristate, 1-2 parts of polydimethylsiloxane, 1-2 parts of 2-oxazolidone, 4-5 parts of magnesium sulfate, 4-5 parts of coconut oil fatty acid, 2-3 parts of tall oil fatty acid, 4-5 parts of assistant and 100-110 parts of water. The assistants are added to improve the technical properties of the detergent and reduce the toxic or side effect and environmental pollution; and the detergent has the advantages of excellent dissolution and dilution capability for inks, no toxicity, no volatilization, no harm to the human body, no corrosivity and low manufacturing cost, and is convenient to use.

The invention provides a method for synthesising ezetimibe intermediate, comprising the following steps of: dissolving (4S)-3-[5-(4-fluorophenyl)-1,5-di-oxo-pentyl]-4-phenyl-2-oxazolidone and chiral carbonyl reductase in a two-phase mixed solution which is composed of an organic solvent and phosphate buffer; and performing synthesis reaction for 10-30 hours in an nitrogen protection environment, and then obtaining (4S)-3-[(5S)-(4-fluorophenyl)-5-hydroxyl-1-oxo-pentyl]-4-phenyl-2-oxazolidone, wherein the temperature of the synthesis reaction is 20-50 DEG C, and the pH of the two-phase mixed solution is 5.5-8.5. Via the method, the technical problems of complex synthesis process and high production cost of (4S)-3-[(5S)-(4-fluorophenyl)-5-hydroxyl-1-oxo-pentyl]-4-phenyl-2-oxazolidone in the prior art are solved.

A composition containing a poly-functional molecule; a polysaccharide having a molecular weight of at least 10,000; and mono(hydroxyalkyl)urea and/or 2-oxazolidone crosslinking agents is disclosed. The poly-functional molecule contains at least two functional groups selected from the group consisting of carboxyl, anhydride and amine. The composition is useful as a crosslinking system.

The invention provides a method for preparing a sofosbuvir intermediate. The method includes following steps: allowing 2-C-methyl-4, S-O-(1-methylethylene)-D-arabonic acid ethyl cyclosulfate and 4-phenyl-2-oxazolidone to be in condensation reaction to obtain a first compound; allowing the first compound and a fluorinating agent for fluorinating reaction, and adding acid for deprotection reaction to obtain a second compound; allowing the second compound to react with sodium ethoxide to obtain a third compound; allowing the third compound to be in rearrangement reaction, and allowing a rearrangement product to react with benzoyl chloride to obtain the sofosbuvir intermediate. The method provides a new idea for synthesizing the sofosbuvir intermediate.

The invention discloses a linezolid preparation method. Dichloromethane is taken as a solvent, a potassium bromide solution is added, cooling is carried out, (5R)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-5-hydroxymethyl-2-oxazolidinone is added, a catalyst of a tetramethyl piperidinyloxyl nitride oxide is added while stirring is carried out, a sodium hypochlorite solution is added dropwise, after adding is carried out dropwise, reaction is carried out for 1-3 hours at the temperature of 0-10 DEG C, dichloromethane is added for extraction, an organic phase is dried and filtered through anhydrous sodium sulfate, and (5R)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-5-formaldehyde-2-oxazolidinone is obtained after the solvent is condensed. Methyl alcohol is taken as a solvent, the (5R)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-5-formaldehyde-2-oxazolidinone is added and heated to 20-50 DEG C, acetamide is slowly added, liquid-phase chromatogram track reaction is conducted, a reduction agent is directly added after the reaction is completed, precipitation and filtering are carried out, and linezolid is obtained. The method is moderate in reaction condition and environmentally friendly, and can be used for industrial large-scale production.

The invention discloses a cyclization method of 4-substituted-2-oxazolidone. The method is implemented through the following steps: (1) acylation: acylating chiral alkamine in a toluene solvent by adopting chloro-formate in the presence of potassium carbonate, so as to obtain chiral alkamine acylate; (2) cyclization: carrying out cyclization reaction through taking PEG-400 as a phase transfer catalyst, thereby obtaining 4-substituted-2-oxazolidone. Compared with the prior art, the cyclization method disclosed by the invention has the advantages that the adopted phase transfer catalyst is low in cost and is free of risk, reacting steps are reduced, the cost is reduced, and the conditions are mild, so that the method is suitable for industrial production.

The invention discloses a preparation method of a medicinal intermediate N-Boc-cis-4-methyl-L-proline methyl ester. The preparation method comprises the following steps: a compound D-glutamic acid isdiazotized, esterified and hydrolyzed to obtain a compound 16; the compound 16 is reacted with TBSCl to obtain a compound 17; the compound 17 is hydrolyzed, and then reacted with (S)-4-benzyl-2-oxazolidone to obtain a compound 18; the compound 18 undergoes a substitution reaction to obtain a compound 19; the compound 19 is reduced to form a compound 20, and the compound 20 is reacted with DPPA andDBU to obtain a compound 21; the compound 21 is deprotected to obtain a compound 22; the compound 22 is dehydroxylated, then is dissolved in methanol, and the obtained solution is reacted in the presence of potassium hydroxide and iodine to obtain a compound 23; the compound 23 is deprotected, and then reacts with paratoluensulfonyl chloride to obtain a compound 24; and the compound 24 undergoesa cyclization reaction under a catalytic condition, an alkaline substance is added, and the obtained mixture reacts with Boc anhydride to obtain a compound 3. The preparation method of the invention overcomes the defect of poor stereoselectivity in the preparation of the N-Boc-cis-4-methyl-L-proline methyl ester in the prior art, uses the cheap and easily-available starting material, and increasesthe yield of the preparation.