70 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).

A process for making L-glufosinate, the process comprising the following steps: a) reacting a compound according to formula (I), (I), wherein R1 is hydrogen, (C1-C12)-alkyl, (C1-C12)-haloalkyl, (C6-C10)-aryl, (C6-C10)-haloaryl, (C7-C10)-aralkyl, (C7-C10)-haloaralkyl, (C4-C10)-cycloalkyl, or (C4-C10)-halocycloalkyl, with a compound according to formula (II), (II), wherein R2 and R3 are independently from each other (C1-C8)-acyloxy, (C1-C8)-alkoxy or hydroxy, or R2 and R3 form together an epoxide group or an ethylene carbonate group, and optional subsequent acidic treatment to form a diol according to formula (III), (III), b) Oxidizing the diol according to formula (III) to form 2-oxo-4-(hydroxy(methyl)phosphinoyl)butyric acid (PPO); and c) aminating the PPO to L-glufosinate.

The application belongs to the technical field of chemical synthesis, and particularly relates to a trifluoromethyl-containing benzothiazole tertiary alcohol derivative, a preparation method and application thereof. 1 , R 2 are independently selected from hydrogen, C1-C3 alkyl, C1-C3 alkoxy or halogen; or R 1 , R 2 independently form a naphthalene ring with the substituted benzene ring together. The trifluoromethyl-containing benzothiazole tertiary alcohol derivative provided by the application has good bacteriostatic effect on one or more of Rhizoctonia solani, Fusarium moniliforme, Fusarium graminearum, Fusarium oxysporum and Phytophthora nicotianae.

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.

A preparation method of amino alcohol derivatives, the present application relates to the field of preparing amino alcohol derivatives by double functionalization of styrene derivatives, and aims to solve the technical problems of complicated steps and low utilization rate of raw materials in the existing synthesis of amino alcohol derivatives.Method: I. under the condition of nitrogen atmosphere and room temperature, the styrene derivative and N-benzamide-2,4,6-triphenylpyridine tetrafluoroborate derivative are dissolved in a mixed solvent containing alkyl alcohol, then a photocatalyst and a Lewis base are added, mixed uniformly, placed under blue LED light for photoreaction, after the reaction is completed, extracted with water and ethyl acetate, the organic phase is collected, the solvent is removed by rotary evaporation, and then separated and purified by silica gel column chromatography.The method can react at normal temperature and pressure, the reaction condition is mild, green and environmental protection, and has the advantages of simple and effective operation, safety, environmental protection, low cost and the like.The present application is used for synthesizing amino alcohol derivatives.

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 belongs to the technical field of coatings, and relates to a bi-component bionic super-hydrophobic ice and snow prevention coating and a preparation method thereof.The coating is prepared from a component A and a component B. The mass ratio of the component A to the component B is 1: (1-1.5), and the component A is prepared from 10-15 parts of modified hydroxyl-terminated polyurethane prepolymer, 20-30 parts of fluorosilicone resin, 2-5 parts of simethicone and 15-20 parts of graft modified inorganic particles; the modified hydroxyl-terminated polyurethane prepolymer is prepared by reacting diisocyanate, polymer dihydric alcohol and an alkyne-containing binary chain extender to prepare hydroxyl-terminated alkyne-containing polyurethane and then carrying out phenylacetylene in-situ graft polymerization; the grafted modified inorganic particles are prepared by in-situ grafting a mixture of phenylacetylene and phenylacetylene alcohol derivatives by taking alkynyl of an alkynyl silane coupling agent modified inorganic filler as an active site, and under the action of a component B polyisocyanate curing agent, a hydroxyl-terminated polyurethane prepolymer and active hydroxyl on the surfaces of the modified inorganic particles are subjected to a cross-linking reaction; and dense cross-linked networks are respectively formed, so that the coating has excellent hydrophobicity and durability.

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.

To provide compounds, pharmaceutical compositions, and uses thereof for activating Kv7 potassium channels and treating related disorders.SOLUTION: Compounds selected from the group consisting of (R)-N-((R)-2-(difluoromethoxy)-1-(3-(difluoromethoxy)phenyl)ethyl)-3-hydroxy-4,4-dimethylpentanamide; (S)-3-(3,3-difluorocyclobutyl)-N-((R)-2-(difluoromethoxy)-1-(3-(difluoromethoxy)phenyl)ethyl)-3-hydroxypropanamide; (R)-3-(3,3-difluorocyclobutyl)-N-((R)-2-(difluoromethoxy)-1-(3-(trifluoromethoxy)phenyl)ethyl)-3-hydroxypropanamide; and pharmaceutically acceptable salts thereof are provided.SELECTED DRAWING: None

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 application of a series of steviol derivatives in preventing and treating pathogenic bacteria of cow mastitis, and belongs to the field of medicinal chemistry. According to the present invention, with the application of the derivative, the excellent inhibition activity on the dairy cow mastitis pathogenic bacteria such as Streptococcus agalactiae ATCC 12386 and Streptococcus dysgalactiae ATCC 27957 can be provided, and the derivative can be used for the preparation of the dairy cow mastitis pathogenic bacteria such as Streptococcus agalactiae ATCC 27957, the synthesis method of the compound is simple, the raw materials are cheap and easy to obtain, and the compound has great development value in the aspect of natural product source compounds for preventing and treating cow mastitis. The structural formula of the compound is shown in the specification.

Disclosed is a 2,3-dimethoxy-5-methyl-1,4-benzoquinone alkyl alcohol derivative, a pharmaceutical composition containing the compound, and the use of the compound in the prevention and treatment of tumors.

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.

The present disclosure provides cannabicyclol derivatives and preparation methods thereof, belonging to the field of biomedical technology. In the present disclosure, citral (3,7-Dimethyl-2,6-octadienal) and derivatives thereof, and olive alcohol (1,3-Dihydroxy-5-pentylbenzene) and derivatives thereof are used as raw materials for the efficient synthesis of the cannabicyclol derivatives in a one-pot manner under an action of ethylenediamine and a photocatalyst.

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.