48 results about "Alcohol derivative" patented technology

The invention provides a fluorenyl alcohol derivative which can be used as an antibiotic adjuvant with a broad-spectrum synergistic effect. According to the compound, bacteria outer membrane asymmetric protein MlaC and phospholipase A1 PldA are taken as targets, and a series of fluorenyl alcohol derivatives targeting the bacteria outer membrane asymmetric protein MlaC and phospholipase A1 PldA are obtained through screening. The preferable compound WTU-15 can improve the antibacterial activity of antibiotics such as polymyxin, cefepime, tetracycline and the like on negative bacteria such as sensitive and drug-resistant escherichia coli, salmonella, klebsiella pneumoniae, acinetobacter baumannii and the like, and can also improve the in-vivo treatment effect of cefepime on mice infected by the drug-resistant acinetobacter baumannii. And the visceral organs of the mice survived after administration have fewer bacteria, and the mice are better after being healed. Normal physiological and visceral organ functions of the mouse are not affected by single and continuous administration of the WTU-15.

This invention provides a novel phosphine oxide compound that inhibits SHP2, a composition thereof, a method for preparing the compound, and a method for treating SHP2-related diseases (such as cancer).

Provided is a composition capable of suppressing generation of a trimer even when an aliphatic aldehyde at a high concentration of 90 mass% or more is stored at a low temperature. The composition contains 90 mass% or more of an aliphatic aldehyde having 8-16 carbon atoms and 100 ppm or more and 1 mass% or less of an additive with respect to the mass of the aliphatic aldehyde, wherein the additive is one or more selected from the group consisting of polyalkylene glycol derivatives represented by formula (I), sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbitol fatty acid esters, amino acids represented by formula (II), anthranilic acid esters represented by formula (III), and pyrazine derivatives represented by formula (IV).

The application discloses a W / O / W composition and a preparation method thereof, and belongs to the technical field of cosmetics. The W / O / W composition comprises the following components in percentage by weight: 0.5-2% of lipophilic surfactant, 1-5% of hydrophilic surfactant, 5-20% of oil phase, 0.5-2% of cholesterols and / or sterol derivatives, 5-20% of polyhydric alcohol and 0.1-2% of thickening agent. Based on the long-term stability of multiple emulsions, the application adds cholesterols and / or sterol derivatives to obtain a W / O / W composition which is long-term stable and has excellent skin feeling. In addition, the preparation method of the W / O / W composition is less than 40 DEG C, which can reduce the production energy consumption and the risk of inactivation of temperature-sensitive active ingredients.

The present application relates to the technical field of medicine, and provides a lanosterol derivative, a preparation method and application thereof.The structural formula of the lanosterol derivative provided by the present application is shown as formula I or formula II.The lanosterol derivative provided by the present application has both fat solubility and water solubility, can effectively penetrate into the pathological site in the body, and improves the drug utilization degree;the results of examples show that the solubility of the lanosterol derivative provided by the present application in water is obviously higher than that of lanosterol or 25-hydroxy lanosterol, and the lanosterol derivative shows obvious cataract treatment effect in animal body experiments, and has a broad prospect in the preparation of drugs for treating eye diseases or conditions.

The invention belongs to the technical field of lubricants, and discloses a lubricant containing Guerbet alcohol derivatives and a preparation method and application thereof. The lubricant is prepared from the following components in parts by weight: 2 to 6 parts of Guerbet alcohol derivative, 0.2 to 1 part of sulfurized isobutylene, 0.05 to 0.3 part of tungsten disulfide nanosheet, 0.01 to 0.1 part of surface modified fullerene, 0.5 to 1.5 parts of triisopropanolamine borate, 80 to 95 parts of 2-octyl-dodecyl cyclopentane, 0.3 to 0.8 part of antioxidant and 0.1 to 0.5 part of antirust agent. The Guerbet alcohol derivative is an ester derivative of Guerbet alcohol; the surface modified fullerene is obtained by modifying fullerene by using dodecyl mercaptan and azodiisobutyronitrile. When ester synthesized from isostearyl alcohol is used as an ester derivative of Guerbet alcohol, the lubricant still has good lubricating performance. Furthermore, the high-temperature-resistant and high-pressure-resistant oxidation performance is good.

The present invention belongs to the technical field of medicinal chemistry, and specifically relates to an azole alcohol derivative containing a difluorophenyl structure and the use thereof in the preparation of a drug for treating various diseases caused by fungal infection. The derivative is a compound represented by formula I, or a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof. Further provided are a preparation method therefor and the use thereof in the preparation of a drug for preventing or treating various diseases caused by fungal infection.

The invention belongs to the technical field of medicine, and discloses a bicyclol derivative shown as a formula (I) or pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition thereof and application thereof, especially application of the bicyclol derivative in medicines for treating liver diseases.

The invention generally refers to pharmaceutical uses of tetracyclic terpene 3-ols, as an example lanosta-8,24-dien-3-ol, bearing polar and / or charged moieties, as anti-inflammatory, anti-cancer and analgesic agents via the inhibition of the disordered activation of serine-threonine protein kinases, particularly PKC.

The invention relates to the technical field of medicine synthesis, in particular to ergosterol amino alcohol derivatives with antibacterial activity and a preparation method and application thereof. The structure is as shown in general formula (I). The ergosterol amino alcohol derivative disclosed by the invention is high in gram-positive bacterium and gram-negative bacterium resisting activity, and the antibacterial activity of the derivative with the optimal activity on staphylococcus aureus and escherichia coli is improved by 64 times and 32 times respectively, so that the ergosterol amino alcohol derivative is obviously superior to that of lead compound ergosterol and compounds reported in literatures. The IC50 values of the human body normal cells HK-2 (near-end renal tubular epithelial cells) and HEK-293 (human embryo renal epithelial cells) are obviously higher, and when MIC < lt > is less than MIC < lt >, MIC < lt > is less than MIC < lt >; the ergosterol amine alcohol derivative has the selectivity index SI of more than or equal to 6.0 when the molecular weight of the ergosterol amine alcohol derivative is 32 [mu] g mL <-1 >, has the characteristics of high efficiency and low toxicity, and has potential application value in the aspect of anti-infection drug development.

A liquid composition comprising a micronutrient dissolved in a solvent which is selected from the group consisting of polyhydric alcohols, derivatives of polyhydric alcohols, and mixtures thereof. The

The invention relates to the technical field of molecular design and synthesis of plant growth regulators, in particular to a high-water-solubility phytosterol derivative for plant growth regulation and application of the high-water-solubility phytosterol derivative. The derivative has a phytosterol-dibasic acid-hydrophilic transport head structure, phytosterol is an active part, dibasic acid is a hydrolyzable connecting arm, and a hydrophilic head is a polyol or polyethylene glycol unit, so that excellent water solubility is given to molecules. The derivative can form a true solution in water, can be easily absorbed by plant leaf surfaces and root systems, can be conducted in a plant body system, and releases phytosterol through enzymolysis, so that the biostimulation functions of promoting growth, enhancing stress resistance, increasing yield and the like are stably exerted. The technical problems that the phytosterol is poor in water solubility, low in absorption efficiency and inconvenient to apply are solved, and the phytosterol is suitable for preparing the efficient and environment-friendly plant growth regulator.

To provide a method for producing a (2R, 3S) - 2 - (benzo [d] imidazolylpropyl) piperidin-3-ol derivative in high yield even by a shortened process.SOLUTION: To provide a method for producing (2R, 3S) -2 - (3 - (4, 5-dichloro - 1H - benzo [d] imidazol-1-yl) propyl) piperidin-3-ol monohydrochloride which is a (2R, 3S) -2 - (benzo [d] imidazolylpropyl) piperidin-3-ol derivative. In addition, the present invention provides a method for preparing the compound represented by Chemical Formula 1-1, which is a starting material in the method for preparing the (2R, 3S) -2 - (benzo [d] imidazolylpropyl) piperidin-3-ol derivative. Further, the present invention provides a method for preparing an intermediate compound for preparing the compound represented by Chemical Formula 1-1.SELECTED DRAWING: None

The application discloses a preparation method of a cyclopentadiene derivative, which comprises the following steps: (1) uniformly mixing silica gel with a polymerization inhibitor, a dehydration catalyst and a solvent, and drying to obtain loaded silica gel; (2) sequentially adding the loaded silica gel and molecular sieve into a filler column to form a loaded silica gel layer and a molecular sieve layer in the filler column, and horizontally placing the filled filler column, wherein one end of the filler column close to the loaded silica gel layer is a feeding port, and the other end is a discharging port; (3) adding a cyclopentadiene alcohol derivative solution and an alkane solvent from the feeding port, maintaining negative pressure at the discharging port, and collecting the mixed solution flowing out of the discharging port; and (4) performing concentration treatment on the mixed solution collected in the step (3), and obtaining the cyclopentadiene derivative after removing the solvent. The preparation method can effectively improve the conversion rate of reactants and effectively inhibit the self-polymerization of products, and high-purity products can be obtained without purification, and the yield can be up to 83% or more.

The present invention relates to a copper fine particle dispersion that contains copper nanoparticles A dispersed in the dispersion with a polymer B, and a dispersion medium C, in which the polymer B contains a constitutional unit derived from a carboxy group-containing monomer (b-1) and a constitutional unit derived from a polyalkylene glycol segment-containing monomer (b-2), a content of the polyalkylene glycol segment in the polymer B is not less than 55% by mass and not more than 97% by mass, an acid value of the polymer B is not less than 20 mgKOH / g and not more than 250 mgKOH / g, and the dispersion medium C contains at least one compound selected from the group consisting of a (poly)alkylene glycol, a (poly)alkylene glycol derivative, a terpene alcohol, glycerin and a glycerin derivative; and a method for producing a bonded body, which includes the steps of allowing the aforementioned copper fine particle dispersion to intervene between a plurality of metal members; and heating the dispersion.

The invention discloses a perillyl alcohol derivative as well as a preparation method and application thereof. The structural formula of the compound is as shown in formula I in the specification. The preparation method comprises the following steps: (1) reacting perillyl alcohol with p-chloromethyl benzoyl chloride to obtain an esterification reaction intermediate; and (2) carrying out nucleophilic substitution reaction on the esterification reaction intermediate and different substituted piperazines to obtain the target compound I. The compound disclosed by the invention has good activity on gastric cancer cells MKN45 and SGC-7901.

The invention provides a method for preparing chiral sulfinic acid thioester through asymmetric oxidation, which is characterized in that a disulfide compound is used as a raw material, a chiral aminoindanol-derived alloxan compound is used as a chiral catalyst, hydrogen peroxide or oxygen is used as an oxidant, and the chiral sulfinic acid thioester is prepared through asymmetric oxidation. Compared with a traditional chiral imine ligand matched with a vanadyl acetylacetonate catalyst, an aminoindanol-derived alloxan compound is used as a chiral small-molecule catalyst, so that the chiral small-molecule catalyst has higher catalytic stability and high optical purity of a product, is not influenced by factors such as the stirring speed, the shape and size of a reaction bottle and the like, and is convenient for engineering amplification; meanwhile, compared with a chiral resolution method, the method for synthesizing the chiral sulfinic acid thioester in one step by using a chiral small molecule catalysis method has higher step economy, and the method is simple to operate, high in raw material conversion rate, good in reaction enantioselectivity, high in product yield and high in optical purity.

The present invention relates to a method for preparing (2R, 3S)-2-(benzo[d]imidazolylpropyl)piperidin-3-ol derivatives, and the preparation method according to the present invention has the advantage that the compound can be prepared in high yield even with a shortened process.

A copper fine particle dispersion including copper nanoparticles A dispersed in the copper fine particle dispersion with a polymer B, and a dispersion medium C. The polymer B contains a constitutional unit derived from a carboxy group-containing monomer (b-1) and a polyalkylene glycol segment-containing monomer (b-2). A content of the polyalkylene glycol segment in the polymer B is not less than 55% by mass and not more than 97% by mass. An acid value of the polymer B is not less than 20 mgKOH / g and not more than 250 mgKOH / g. The dispersion medium C includes at least one compound selected from the group consisting of a (poly)alkylene glycol, a (poly)alkylene glycol derivative, a terpene alcohol, glycerin and a glycerin derivative.

The application discloses a high-performance grinding aid for superfine composite mineral admixture and a preparation method thereof. The grinding aid is composed of the following components in percentage by weight: polyamine carboxylic acid polymer 35-50%, modified nano-silica 5-15%, polyol derivative 15-30%, and alcohol amine derivative 15-30%. The application utilizes the adsorption and dispersion of the polyamine carboxylic acid polymer, the particle skeleton and multi-level filling of the modified nano-silica, the crack penetration of the polyol derivative and the alcohol amine, and the charge neutralization and polymerization inhibition of the polar groups such as amine groups, hydroxyl groups and carboxyl groups in the components to form a synergistic grinding combination. Compared with traditional grinding aids, the grinding aid is more conducive to the extrusion, crushing and dispersion of particles, can effectively prevent the particles from being pasted on the surface of the grinding ball, has better grinding effect, higher grinding efficiency and more stable grinding performance.

The present application relates to a kind of high-stable pyrylium alcohol derivatives with light protection, whitening activity and its preparation method and application.The present application is based on the molecular structure of pyrylium alcohol and is connected with different cinnamic acid side chain, obtains a series of cinnamic acid side chain modified pyrylium alcohol derivatives.The pyrylium alcohol derivatives of the present application can effectively improve the chemical stability of pyrylium alcohol, effectively solve the discoloration and inactivation problem of pyrylium alcohol in cosmetic formula.The pyrylium alcohol derivatives of the present application have excellent chemical stability, have the ability of rapid oxidation resistance, and can realize precise synergistic effect at cell level, the activity of inhibiting melanin, antioxidant and light protection in organism is significantly better than pyrylium alcohol.The pyrylium alcohol derivatives of the present application have higher fat solubility and lower effective concentration, can be used for preparing whitening, antioxidant, light protection and other cosmetics, and have important market value.

The invention discloses a paclitaxel derivative. The paclitaxel derivative is a compound as shown in a molecular formula 6. The invention also claims to protect a preparation method and application of the paclitaxel derivative, and an antitumor drug containing the paclitaxel derivative. The paclitaxel derivative provided by the invention can reduce the distribution of drugs to non-target tissues and organs, accelerate the in-vivo elimination process of the drugs, reduce the residence time of the drugs in blood, and reduce toxic and side effects such as blood toxicity and neurotoxicity of the drugs.

The oil-in-water emulsion composition of the present invention suppresses the denaturation of a retinol derivative, even in severe environments such as high temperatures. The present invention relates to an oil-in-water emulsion composition comprising: (A) 0.01 to 4% by mass of a retinol derivative; (B) 0.05 to 3% by mass of powder made from a highly water-absorbent polymer having an absorption ratio of 10 or more times its own weight; (C) an oil excluding higher alcohols which are solid at normal temperature; (D) water; and (E) a nonionic surfactant.

The present application provides a method for producing a dicarboxylic acid monoester having excellent selectivity and yield. The method for producing a dicarboxylic acid monoester of the present application is as follows: a dicarboxylic acid represented by the following formula (1) and an alcohol derivative represented by the following formula (2) are reacted in a mixed solvent of water and a hydrophobic solvent using a base to produce a dicarboxylic acid monoester represented by the following formula (3) or (4).X 1 - SP 1 - P 1 (2)

The application belongs to the technical field of pharmaceutical chemistry, and particularly relates to an azole alcohol derivative containing a difluorophenyl structure and application of the azole alcohol derivative in preparation of medicines for treating various diseases caused by fungal infection. The derivative is a compound shown in formula I, a stereoisomer, a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug of the compound, a preparation method of the derivative and use of the derivative in preparation of medicines for preventing or treating various diseases caused by fungal infection.

The application provides an anti-corrosion composition and application thereof. The anti-corrosion composition mainly comprises imidazoline derivatives, acetylenic alcohol derivatives, deoxidizing agents and metal salts, and secondly comprises surfactants and solvents. The anti-corrosion composition has good film forming performance, high anti-corrosion efficiency, can effectively prevent corrosion of carbon dioxide, hydrogen sulfide, oxygen and chloride ions, can be used as an anti-corrosion agent to effectively protect natural gas pipelines, and has the advantages of easy availability of raw materials, low cost, simple preparation method and application in the field of natural gas pipeline corrosion prevention.

The application provides a zedoary alcohol derivative, a synthesis method and application thereof, and a structural general formula of the zedoary alcohol derivative is as follows: wherein R1 is selected from a naphthyl group, a dimethylamino group, a substituted benzene group, an aromatic group and a substituted aromatic group. A sulfonate compound is introduced at a hydroxyl group of zedoary alcohol to obtain the zedoary alcohol derivative with anti-influenza virus activity, the synthesis method is green and environment-friendly, the reaction condition is mild, the efficiency is high, and the drug efficacy is better than that of a parent compound zedoary alcohol.