14 results about "Ethyl pyruvate" patented technology

Methods of treating or preventing conditions in a subject are disclosed, the methods including administering to the subject a therapeutically effective amount of ethyl pyruvate, or a derivative or analog thereof, or a pharmaceutical composition thereof. Methods of treating or preventing conditions in a subject including administering to the subject a therapeutically effective amount of ethyl pyruvate, or a derivative or analog thereof, or a pharmaceutical composition thereof, and one or more additional therapeutic agents, are described.

Disclosed is a method of treating or preventing a condition in a subject, the method comprising administering to the subject a therapeutically effective amount of ethyl pyruvate or a derivative or analog thereof, or a pharmaceutical composition thereof. Methods of treating or preventing a condition in a subject are described, comprising administering to the subject a therapeutically effective amount of ethyl pyruvate or a derivative or analog thereof, or a pharmaceutical composition thereof, and one or more other therapeutic agents.

The invention provides a preparation method of a sacubitril valsartan key intermediate, which comprises the following steps of: reacting (R)-1-(1-([1, 1 '-biphenyl]-4-yl)-3-chloropropane-2-yl) pyrrolidine-2, 5-diketone and trialkyl phosphite under the action of a catalyst to generate a Witting-Horner reagent, then reacting with ethyl pyruvate under an alkaline condition to generate a double-bond product, and reacting with ethyl pyruvate under an alkaline condition to generate the sacubitril valsartan key intermediate. Hydrolyzing the double bond product to generate (R, E)-5-((1, 1 '-biphenyl)-4-yl)-4-amino-2-methyl-2-ethyl pentenoate; the preparation method comprises the following steps: firstly, taking 4-methyl-2-pentenoic acid as a raw material, then protecting the 4-methyl-2-pentenoic acid through BOC anhydride under the action of an acid-binding agent, and finally hydrolyzing under an alkaline condition to obtain (R, E)-5-([1, 1 '-biphenyl]-4-yl)-4-((t-butyloxycarboryl) amino)-2-methyl-2-pentenoic acid. The preparation method has the advantages of simple process steps, convenient operation, easily available raw materials, and easy industrial production.

The present invention relates to a process for the preparation of highly pure enantiomer of Fezolinetant, and in particular highly pure (R)-Fezolinetant. The invention also relates to chiral resolution by acid for the preparation of highly pure R-Fezolinetant. Additionally, the invention relates to a process for preparing intermediates useful for the preparation of (R)-Fezolinetant, their uses and a process for preparing (R)-Fezolinetant. In particular, the intermediate (R)-3-methylpiperazin-2-one is prepared by reductive amination with an imine reductase from Myxococcus stipitatus and ethylene diamine and ethyl pyruvate.

The invention belongs to the technical field of chemical processes, and particularly relates to a method for continuously synthesizing pyruvic acid through catalytic oxidation of ethyl lactate and coupled reaction rectification. According to the method, ethyl lactate and hydrogen peroxide are used as raw materials, a titanium silicalite molecular sieve is used as a catalyst, pyridine-2-formic acid is added as an auxiliary agent, ethyl pyruvate is synthesized in a tubular reactor filled with the catalyst, then under the condition of reduced pressure, pyruvate is hydrolyzed through a continuous reactive distillation tower, and a pyruvic acid water solution is obtained at the tower bottom. According to the invention, a tubular reactor model is adopted, the side reaction of hydrogen peroxide caused by backmixing of kettle reaction is solved, meanwhile, pyridine-2-formic acid is added as an auxiliary agent, the invalid decomposition of hydrogen peroxide in the catalytic oxidation process is solved, and the utilization rate of hydrogen peroxide is improved. Reaction rectification is coupled in the ethyl pyruvate hydrolysis process, continuous hydrolysis of ethyl pyruvate is achieved, a reaction section is filled with styrene resin with sulfonic acid groups to catalyze hydrolysis of ester, the reaction rate is increased from the thermodynamic angle, ethyl alcohol is promoted to be moved out of a system in the decompression hydrolysis kinetics, the reaction time is greatly shortened, and the yield is increased. And high-efficiency, continuous and green synthesis of pyruvic acid is realized.

The invention relates to a green preparation method of ethyl pyruvate. According to the method, ethyl lactate is taken as a raw material and is subjected to continuous gas-liquid phase oxidation in a fixed bed in the presence of oxygen-containing gas, a Mn-Cu-Co ternary oxide is loaded on a nitrogen-containing porous carbon catalyst, air calcination and CO2 atmosphere activation are matched, and pretreatment can be carried out in ethyl lactate / carrier gas so as to regulate and control the metal valence state and the oxygen vacancy structure. Water and trace lactic acid amide, glycine and alanine are introduced into the raw material solution, and optional phytic acid / phytate is combined with choline chloride to construct a weak coordination and hydrogen bond network to adjust the interface oxidability; the fixed bed is provided with double reaction zones for segmented temperature control and oxygen supply along the material flow direction. According to the method, high conversion of ethyl lactate and high selectivity of ethyl pyruvate are realized under relatively mild conditions, byproducts are few, and the stability of the catalyst is good.

A chemoenzymatic manufacturing process for the preparation of high value chemicals includes the enzymatic oxidation of ethanol using an oxidizing biocatalyst to form an acetaldehyde intermediate. In addition, the process includes contacting of the acetaldehyde intermediate with a carboligating biocatalyst to form pyruvic acid. Further, the process includes reacting pyruvic acid with ethanol to form ethyl pyruvate. Still further, the process includes contacting the ethyl pyruvate with a metal catalyst and hydrogen to form ethyl lactate. The process also includes hydrolyzing the ethyl lactate to produce lactic acid. Moreover, the process includes contacting at least a portion of the lactic acid with a dehydrating catalyst to form acrylic acid. In addition, the process includes contacting at least a portion of the lactic acid with a metal catalyst and hydrogen to form propylene glycol and n-propanol.

The invention belongs to the technical field of preparation of high-end high-purity wet electronic chemicals, and particularly relates to a preparation method and system of electronic-grade ethyl lactate. According to the method, food-grade ethyl lactate is taken as a raw material, ethyl pyruvate which is difficult to separate is reduced into ethyl lactate through reduction reaction, ethyl lactate homologues (methyl lactate, propyl lactate and butyl lactate) and light and heavy component impurities in the ethyl lactate are removed through vacuum distillation, and finally anions and cations in the ethyl lactate are removed through resin adsorption, so that the ethyl lactate is obtained. The content of the obtained ethyl lactate is higher than 99.99%, the anion content is smaller than or equal to 10 ppb, the metal ion content is smaller than or equal to 1 ppb, the acidity is smaller than or equal to 80 ppm, the moisture content is smaller than or equal to 100 ppm, and the requirements of electronic-grade ethyl lactate are met. The method can effectively remove ethyl pyruvate and ethyl lactate homologues which are difficult to remove in ethyl lactate, and has the advantages of low cost, low energy consumption, high production efficiency, environmental protection and the like.

The invention discloses an aza-tricyclic amide compound as well as a preparation method and application thereof, and belongs to the technical field of synthesis of organic compounds. The aza-tricyclic amide compound is prepared by taking an o-aminobenzaldehyde compound, ethyl 3-bromopyruvate and the like as raw materials through a one-step reaction. The target compound is prepared through condensation, acylation, methylation, cyclization, substitution, hydrolysis and other multi-step reactions. The compounds can significantly inhibit the growth of human colon cancer HCT116 cells, the ICC of the compound B2 reaches 0.45 mu g / mL, and the compounds can effectively act on a DNA-topoisomerase system and inhibit the proliferation of tumor cells, and can be used for the development of antitumor drugs.

The invention relates to a preparation method of apixaban, which comprises the following steps: carrying out aldol condensation on ethyl methoxyacetate serving as a raw material and ethyl pyruvate to obtain an intermediate II, carrying out alkylation reaction on the intermediate II and 1, 2-dichloroethane to obtain an intermediate III, carrying out pyrazole synthesis reaction on the intermediate III and 4-methoxyphenylhydrazine to obtain an intermediate IV, carrying out alkylation reaction on the intermediate IV and 4-nitroaniline to obtain an intermediate V, and carrying out recrystallization on the intermediate V to obtain the apixaban. The preparation method comprises the following steps: carrying out ester group hydrolysis to prepare an intermediate VI, carrying out molecular lactamization in the presence of a condensing agent to prepare an intermediate VII, carrying out nitro reduction to prepare an intermediate VIII, carrying out amidation on the intermediate VIII and 5-bromovaleryl chloride under the action of an acid-binding agent, further carrying out an intramolecular alkylation reaction under the action of a strong alkali to prepare an intermediate IX, adding tert-butyl hydroperoxide and ammonia water, and carrying out a reaction under the action of a strong alkali to prepare the intermediate IX. Under the catalysis of iodine, carrying out oxidation amidation to prepare apixaban; the method has the advantages of cheap and easily available raw materials, easy realization of industrialization, high product purity, no dangerous process, simple equipment, novel route and short synthesis route.

The utility model discloses a reaction device for an ethyl pyruvate extraction tower, which comprises an extraction tower body, the top of the extraction tower body is fixedly provided with a first feed pipe, the top of the extraction tower body is fixedly provided with a second feed pipe, and the top of the extraction tower body is provided with a driving assembly. A toothed plate is arranged at the top of the extraction tower body through a driving assembly, a gear is arranged on the front side of the toothed plate in a meshed mode, a rotating shaft is fixedly installed in the gear and rotationally connected with the extraction tower body, a stirring net plate is fixedly installed on the surface of the rotating shaft, and a vibration assembly is arranged on the right side of the extraction tower body. A complex flow field generated by reciprocating rotation and stirring has a more uniform mixing effect, substance transfer between an ethyl pyruvate solution and diethyl ether can be quicker and more sufficient, molecular movement in the ethyl pyruvate solution and the diethyl ether can be more violent through vibration, and the collision frequency and energy between molecules are increased.

The application belongs to the technical field of antibiotic application, and discloses that microplastics affect the absorption of ciprofloxacin in the intestinal tract through the TLR4 / NF-kappa B pathway regulating P-gp protein. Our research finds that microplastics can activate the expression of P-gp glycoprotein in intestinal epithelial cells through the NF-kappa B pathway in the intestinal tract, thereby reducing the absorption of ciprofloxacin hydrochloride in the intestinal tract, and further affecting the core mechanism of pharmacokinetics and pharmacodynamics of ciprofloxacin hydrochloride in animals. Pyruvate ethyl effectively inhibits the NF-kappa B pathway. The application also finds that after ivermectin inhibits the P-gp glycoprotein of Caco2 cells, the P-gp glycoprotein cannot efflux ciprofloxacin hydrochloride, so that the content of ciprofloxacin hydrochloride in Caco2 cells increases. Therefore, the application also protects the application of ivermectin in preparing a promoter of the content of ciprofloxacin hydrochloride in Caco2 cells incubated with microplastics.

The utility model discloses an ethyl pyruvate crystallization device which comprises a crystallization box, a feeding pipe is fixedly installed at the top of the crystallization box, a cooling pipe is fixedly installed on the surface of the crystallization box, a stirring assembly is arranged in the crystallization box, a scraper blade is arranged in the crystallization box through the stirring assembly, and the stirring assembly is connected with the scraper blade. A vibration assembly is arranged on the front side of the crystallization box, a connecting pipe is fixedly installed at the bottom of the crystallization box, a valve is arranged on the connecting pipe, a filtering box is fixedly installed at the bottom end of the connecting pipe, a filtering assembly is arranged in the filtering box, and a liquid outlet pipe is fixedly installed at the bottom of the filtering box. According to the ethyl pyruvate crystal cleaning device, the aim of cleaning ethyl pyruvate crystals attached to the inner wall of the crystallization box is achieved, waste of the ethyl pyruvate crystals can be reduced, automatic separation of a solution and the ethyl pyruvate crystals can be achieved, and the situation that an extra device is used for separating the solution and the ethyl pyruvate crystals is avoided.

The present invention discloses the use of ethyl pyruvate in the preparation of a drug for treating or preventing methamphetamine addiction. The present invention belongs to the field of pharmaceutical technology and provides the use of ethyl pyruvate in the preparation of a drug for treating or preventing methamphetamine addiction. Ethyl pyruvate inhibits the HMGB1-TLR4-MyD88-PI3K-AKT-NF-KB signaling pathway, reduces neuroinflammatory responses, and significantly reduces addictive behaviors and nerve damage caused by methamphetamine. This provides a new therapeutic strategy for the treatment of methamphetamine addiction and has broad clinical application prospects. Ethyl pyruvate has significant neuroprotective effects, can reduce nerve damage, and promote nerve repair.