35 results about "Aminoketone" patented technology

The disclosure relates to compositions comprising a phentermine and a unicyclic aminoketone and methods of use thereof. The methods of use include inducing weight loss or reducing weight gain in a human subject. The unicyclic aminoketone may be diethylpropion or bupropion. In some embodiments, the compositions further include tadalafil or naltrexone.

The invention discloses a near-infrared two-window fluorescent probe for detecting viscosity as well as a preparation method and application thereof, belongs to the technical field of biological fluorescence imaging contrast agents, and provides a structural formula of a viscosity probe and a preparation method of the near-infrared two-window fluorescent probe for detecting viscosity. Comprising the following steps: S1, cyclohexanone and 4-diethylaminoketonic acid are subjected to a reaction in concentrated sulfuric acid, and a solid product (a compound 1) is obtained through post-treatment; and S2, carrying out a reaction on the compound 1 obtained in the step S1 and 9-aldehyde julolidine in an ethanol solution. And carrying out post-treatment to obtain solid R-CHO. The detection method disclosed by the invention has the advantages of simplicity and convenience in operation, rapidness, accuracy, high sensitivity and the like, and is suitable for biomedical research, clinical diagnosis and other related fields.

The application discloses a method for preparing chiral amino alcohol compounds by using water as a hydrogen source and nickel metal as a catalyst. The method comprises the following steps: dissolving a nickel metal catalyst, zinc powder, an additive and a ligand in a dry organic solvent under an inert gas atmosphere; then adding an o-phthalimido ketone compound and water; and reacting at 40-70 DEG C to obtain a target product. The additive is one or more of silver iodide, cuprous bromide, cuprous iodide and cuprous chloride. The ligand is ( S, S p )- t‑ Bu-Phosferrox, S, S p )-Bn-Phosferrox, R, R p )-Ph-Phosferrox or R, R p )- i‑ Pr-Phosferrox. The application uses water as a hydrogen source and nickel metal as a catalyst to catalyze amino ketone compounds to obtain a series of chiral amino alcohol compounds. The method is simple, clean and environmentally friendly, and is suitable for the conventional preparation of chiral amino alcohol compounds.

The present application relates to the field of pharmaceutical preparations, in particular to 5-amino-ketoglutaric acid metal complex, liposome and preparation method thereof. The 5-amino-ketoglutaric acid metal complex of the present application is formed by 5-amino-ketoglutaric acid and metal ion through coordination bond, and is a photosensitizer which can be used for photodynamic therapy of tumor. After ALA forms complex with metal ion, the reaction activity of amino and ketone groups in ALA molecule is reduced, the adverse influence of external environment on the molecule is delayed, and the stability is enhanced. Moreover, the co-aggregation of ALA and copper ion (or iron ion) to target tissue, the two means of ALA photodynamic therapy of tumor and copper (iron) ion promoting tumor cell apoptosis play drug efficacy, and have synergistic anti-tumor effect. The present application further provides liposome loaded with 5-amino-ketoglutaric acid metal complex, and preparation containing 5-amino-ketoglutaric acid metal complex or liposome.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to preparation and application of beta-, gamma-or delta-aminoketone derivatives, the structure of the derivatives is shown as a general formula (I), in the formula, R1 is alkyl, aryl and the like; r2 represents an aryl group, a heteroaryl group, an alkynyl group, an alkenyl group, a cyano group or the like; r3 is hydrogen, alkyl, aryl or the like; r4 represents an aryl sulfonyl group, a heteroaryl sulfonyl group, an alkyl sulfonyl group, a sulfonate group or the like; in the structural formula, n represents the length of a carbon chain, and the value is 0-2. The derivative is novel in structure, has good antiviral activity, particularly has a good inhibition effect on H1N1 virus, and has great application potential in the aspect of antiviral effect; meanwhile, the preparation method has the advantages of few reaction steps, no need of metal catalysis, no need of complex substrate preparation, simplicity and safety in operation, mild reaction conditions, low cost, higher atom economy and high yield.

The present disclosure relates to novel quaternary salt compounds including, in one embodiment, a cation having a quaternary ammonium group that is coupled to a N-substituted amino ketoacetate anion as a counterion.

The application provides a water-triggered self-assembly gel, a use method and application thereof. The water-triggered self-assembly gel comprises 5-aminolevulinic acid hydrochloride 5-15 wt%, phospholipid 5-10 wt%, anionic glycolipid surfactant 0.2-0.8 wt%, polyethylene glycol 50-60 wt%, propylene glycol 20-27 wt% and antioxidant 0.05-0.1 wt%, and water <0.1 wt%; the mass ratio of the polyethylene glycol and the propylene glycol is (2-2.5):1. The water content of the water-triggered self-assembly gel is extremely low, so that the stability is good and the storage is easy; when used, the water-triggered mechanism of transdermal water loss can be used to actively extract water from the stratum corneum, the phase transition of the phospholipid from the disordered lamellar phase to the liposome is quickly completed, the nanometer liposome with uniform particle size and high encapsulation efficiency is spontaneously formed, the 5-ALA hydrochloride is wrapped, and the 5-ALA hydrochloride can be efficiently delivered to the deep layer of the skin.

The utility model discloses equipment for rapidly separating 5-aminolevulinic acid, and relates to the technical field of rapid separation of 5-aminolevulinic acid, the equipment for rapidly separating 5-aminolevulinic acid comprises a column body, the top end of the column body is provided with a top head seat, the upper end of the top head seat is provided with a feed inlet, and the lower end of the top head seat is provided with a discharge outlet. A bottom end base is arranged at the bottom end of the column body, a discharging port is formed in the lower end of the bottom end base, supporting legs are welded to the lower surface of the bottom end base, water inlet pipes are arranged on the two sides, close to the top base, of the column body, a water distribution assembly is arranged on one sides of the water inlet pipes, and a material distribution assembly is arranged at the upper end of the water distribution assembly. According to the scheme, the problems that most of existing separation columns for rapid separation of 5-aminolevulinic acid are subjected to single-barrel discharging and water discharging, are located in the centers of the columns and are subjected to single-point discharging and water discharging, the situation that more water is discharged in the middle and less water is discharged on the periphery is caused, and therefore distribution uniformity is caused, and the separation uniformity and efficiency are affected are solved.

The invention discloses a fluorescent probe for detecting the viscosity of a cell membrane as well as a preparation method and application of the fluorescent probe, and belongs to the technical field of small molecule probes. The structural formula of the fluorescent probe is shown in the specification. The preparation method specifically comprises the following steps: (1) reacting 4-diethylaminoketonic acid and cyclohexanone in concentrated sulfuric acid, pouring into crushed ice, stirring, adding perchloric acid, stirring, standing and filtering; (2) dissolving 4-diethylaminobenzaldehyde in absolute ethyl alcohol, heating and refluxing, removing the solvent, and carrying out chromatography; and (3) dissolving benzotriazole-N, N, N ', N'-tetramethylurea hexafluorophosphate and N, N-diisopropylethylamine in N, N-dimethylformamide, stirring at normal temperature, adding a compound 43-(tetradecyl amino) propane-1-sulfonate, continuously stirring, removing the solvent, and carrying out chromatography to obtain the compound 43-(tetradecyl amino) propane-1-sulfonate. The fluorescent probe has excellent anchoring and imaging capabilities and viscosity-triggered near-infrared (NIR) fluorescence response characteristics, can be used for fluorescence imaging of cell membrane viscosity, and can also be used for viscosity imaging analysis of breast cancer mice.

The invention discloses a preparation method of a delta-aminoketone derivative, which comprises the following steps: reacting olefin, N-aryl sulfonyl aziridine, arylboronic acid, nickel iodide, 5, 5 '-dimethyl-2, 2'-bipyridine, formic acid, acetic anhydride, sodium carbonate and potassium iodide at 80 DEG C for 20 hours, and after the reaction is completed, performing post-treatment to obtain the delta-aminoketone derivative. According to the preparation method, olefin, N-aryl sulfonyl aziridine and arylboronic acid are taken as reactants, formic acid is taken as a carbonyl source, the reaction condition is mild, the operation is simple, the tolerance range of substrate functional groups is wide, and the reaction efficiency is high. Various delta-aminoketone derivatives can be synthesized according to actual needs, so that the method is convenient to operate, and the practicability of the method is widened.

The invention belongs to the field of high polymer material synthesis, and particularly relates to a high-performance TPEE elastomer and a preparation method thereof. According to the preparation method of the high-performance TPEE elastomer provided by the invention, chemically synthesized aminoketone is used as a ligand, titanium isopropoxide is used as a titanium source, an aminoketone coordinated titanate coordination catalyst is generated in situ, and the catalyst is used for preparing the TPEE elastomer, so that synthesis of high-elasticity TPEE under the condition of high soft segment content is realized; the heat resistance and tensile strength of the TPEE product prepared under the same hardness are remarkably improved, the TPEE product has excellent hue, the additional value of the product is improved, and the application scene of the product is widened.

The invention relates to the field of infrared materials, in particular to a light-proof and infrared-transmitting polycarbonate composite material and a preparation method thereof. The polycarbonate composite material is prepared from the following raw materials in parts by mass: 96 to 99 parts of polycarbonate, 0.1 to 0.8 part of antioxidant, 0.3 to 1 part of lubricant and 0.3 to 2 parts of pigment. Wherein the pigment is an aminoketone pigment BLACK HTG. The infrared light transmittance of the polycarbonate composite material under the thickness of 2.5 mm is larger than 80%, natural light and LED light cannot penetrate through the polycarbonate composite material, the market blank in the prior art is filled, and the application adaptability is high.

A kind of high photosensitivity slurry of pure copper photocuring 3D printing and preparation method thereof.The high photosensitivity slurry of pure copper photocuring 3D printing composition includes pure copper powder, active diluent, photoinitiator and auxiliary agent.The active diluent is acrylate monomer, and the photoinitiator includes two groups, one group is cleavage type alpha-amino ketone and its derivative, and the other group is thioxanthone and its derivative group.The thioxanthone photoinitiator has higher molar extinction coefficient in the ultraviolet light around 360nm-405nm wavelength, can compete with copper powder for ultraviolet light to avoid the high light absorption coefficient of copper powder to reduce the light initiation efficiency.At the same time, after thioxanthone absorbs ultraviolet light, energy transfer occurs with alpha-amino ketone, so that alpha-amino ketone photoinitiator jumps to excited triplet state, indirectly realizes slurry photopolymerization, greatly improves the light initiation efficiency, improves the photosensitivity of slurry, and solves the problem of high ultraviolet absorbance of copper powder.

This invention provides an in-situ gel delivery carrier for 5-aminolevulinic acid and its preparation method, belonging to the field of biomedical technology. The in-situ gel delivery carrier comprises TAT ​​peptide and *Rhizopus oryzae* lipase; the mass-to-volume ratio of TAT peptide to *Rhizopus oryzae* lipase is 0.03-0.07 g: 0.005-0.015 g. This in-situ gel delivery carrier combines a dual mechanism of "physical thermosensitive phase transition" and "biological thermosensitive enzyme activity" to achieve long-term, targeted adhesion to lesion sites. Through the nonlinear synergistic effect of *Rhizopus oryzae* lipase and TAT peptide, it precisely degrades lipid barriers and efficiently delivers drugs, thereby significantly reducing the drug concentration while exponentially increasing the conversion efficiency of protoporphyrin IX (PpIX) in target cells. The preparation method is simple to operate.

The present disclosure relates to a photoinitiating composition suitable for UV-LED light irradiation comprising: a) a photoinitiating system suitable for LED light irradiation having a wavelength in the range of 340-420 nm; b) a dispersing medium; wherein the dispersing medium comprises an organic solvent which is miscible with water, wherein the photoinitiating system comprises an α-aminoketone and a photosensitizer having absorption in the wavelength range of 340-420 nm, wherein the photosensitizer comprises thioxanthone or derivatives thereof, and wherein the thioxanthone derivatives are substituted thioxanthone, optionally with alkyl, alkoxy, halogen, carboxyl, ester group, amide group or any combination thereof.

The invention provides a green synthesis method of an alpha-aminoketone compound based on visible light catalytic oxidation amination reaction, and belongs to the technical field of organic chemical synthesizing.According to the method, aliphatic aldehyde and secondary amine which are low in price and easy to obtain serve as raw materials, oxygen serves as a green terminal oxidizing agent, and the alpha-aminoketone compound is synthesized under normal temperature and visible light irradiation. The alpha-aminoketone compound is efficiently synthesized in one step through oxidative amination reaction catalyzed by organic photosensitizers such as rhodamine 6G and anthraquinone. According to the method, a noble metal catalyst and a stoichiometric oxidant are abandoned, the reaction condition is mild (room temperature), the operation is simple and convenient, the substrate application range is wide, and the method shows excellent compatibility to functional groups including various complex cyclic secondary amines (such as natural product derivatives of nornicotine, cytisine and the like); compared with the prior art, the method has the advantages that important transformation from thermal activation to light activation is realized on the reaction mechanism, and a novel green way which is more economical and environment-friendly and is easy for large-scale production is provided for synthesis of alpha-aminoketone.

The invention discloses a cannabidiol aminoquinone derivative as well as a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The cannabidiol aminoquinone derivative is a compound with a structure as shown in a formula I, a stereoisomer, a solvate, a hydrate or a pharmaceutically acceptable salt. Tests show that the cannabidiol aminoquinone derivative disclosed by the invention has excellent anti-neuroinflammation activity and anti-Alzheimer's disease activity, and shows huge application potential in the field of treatment of Alzheimer's disease.

The invention belongs to the field of molecular biology and enzyme engineering, and discloses an amine dehydrogenase mutant and application thereof in chiral beta-aminoketone synthesis. The amine dehydrogenase mutant provided by the invention can catalyze reductive amination of various 1, 3-diketone substrates, the substrate spectrum of the mutant is greatly broadened, the activity of the amine dehydrogenase in catalytic synthesis of chiral beta-aminoketone is remarkably improved, the problems of low activity, poor regioselectivity, narrow catalytic substrate range and the like of the amine dehydrogenase are solved, and the application prospect is broad. Wide application prospects are realized.

The invention discloses a method for directionally preparing tetra-substituted pyrazine and application of the tetra-substituted pyrazine in cigarettes, and belongs to the technical field of tobacco flavors. According to the method, ketone and glycine are used as raw materials, o-aminoketone is obtained through Strecker degradation, and tetra-substituted pyrazine is prepared through condensation of two molecules of o-aminoketone. Directional synthesis of tetra-substituted pyrazine is realized by regulating and controlling the types of ketones. When the essence is added into tobacco shreds of cigarettes, the aroma amount and the aroma quality of the cigarettes can be improved, the irritation of smoke is reduced, and the smoking comfort is improved. According to the method, accurate directional synthesis of tetra-substituted pyrazine is realized, the process is simple and controllable, the yield is high, the application effect is excellent, and the method has important popularization value.

The application provides a medical light guide gel with high light guide performance and a preparation method thereof. The medical light guide gel with high light guide performance comprises pure water, glycerol and carbomer, and further comprises aminolevulinic acid propyl ester hydrochloride. The aminolevulinic acid propyl ester hydrochloride is recrystallized, mixed with other components, stirred for 10-15 min, and then the product is prepared by standing. The technical scheme has the technical characteristics of high light penetration, and improves the treatment efficiency and the phototherapy effect.

The invention belongs to the technical field of conductive ink, and relates to pyrrole modified polyvinyl alcohol and polypyrrole grafted polyvinyl alcohol conductive ink as well as a preparation method and application thereof. The preparation method of the polypyrrole grafted polyvinyl alcohol conductive ink comprises the following steps: carrying out acetoacetic acid modification on polyvinyl alcohol to obtain acetoacetic acid polyvinyl alcohol, reacting the acetoacetic acid polyvinyl alcohol with an alpha-aminoketone compound to obtain pyrrole modified polyvinyl alcohol (PVAA-Py), adding water and pyrrole, uniformly mixing, adding ammonium persulfate, ferric trichloride and water, and uniformly mixing to obtain the polypyrrole grafted polyvinyl alcohol conductive ink. And uniformly stirring to obtain the polypyrrole grafted polyvinyl alcohol conductive ink. According to the polypyrrole grafted polyvinyl alcohol conductive ink prepared from the pyrrole modified polyvinyl alcohol, the dispersity, stability and conductivity of the conductive ink are improved, the conductive ink has uniform spreadability, and new conductive ink types and methods are provided for construction of paper-based or other base material conductive circuits.

The invention relates to the field of organic chemistry, in particular to an alpha-aminoketone derivative and application thereof.The chemical formula of the alpha-aminoketone derivative is shown in the formula (I). The alpha-aminoketone derivative has the advantage of being high in photo-initiation efficiency, the curing rate and curing strength can be effectively improved, and the curing time is shortened. And the curing agent is especially suitable for rapid and uniform curing of a large-thickness dark-color system. In addition, the alpha-aminoketone derivative provided by the invention has the advantages of small odor and yellowing resistance, and can be suitable for white paint, varnish and other products.

The invention discloses a modified waterborne polyurethane coating and a preparation method thereof, and belongs to the technical field of waterborne coatings. The coating is composed of 100 parts of polyol, 5-8 parts of a hydrophilic chain extender, 35-45 parts of isocyanate, 3-10 parts of an organosilicon modifier, 0.1-0.5 part of a specific structure leveling agent, 0.5-3 parts of a functional additive, 3-6 parts of a neutralizer and 150-250 parts of deionized water. The flatting agent is a compound containing a polyhydroxy cyclohexyl and aminoketone structure. The preparation method comprises the steps of prepolymer synthesis, chain extension modification, neutralization emulsification, composite dispersion and curing. Through the synergistic effect of the specific leveling agent and the organic silicon modifier, the leveling property of a coating film is remarkably improved, surface defects are eliminated, meanwhile, excellent adhesive force and film forming performance are kept, and the coating is free of toxic volatile matter, has antibacterial and weather-proof functions and is suitable for the fields of furniture, building materials, leather and the like.

The invention provides a pH fluorescent probe and application thereof in food microbiological detection, the chemical structure of the probe is (E)-6 '-(diethylamino)-4'-(2, 4-dimethoxybenzylidene)-2-(2-morpholinoethyl)-1 ', 2', 3 ', 4'-tetrahydrospiro [isoquinoline-1, 9 '-anthracene]-3-ketone, and the structural formula of the probe is shown in the description. The preparation method comprises the following steps: (1) carrying out acid catalytic condensation on cyclohexanone and 4-diethylaminoketonic acid; (2) carrying out aldehyde ketone condensation with 3, 4-dimethoxybenzaldehyde; and (3) finally, carrying out an amidation reaction with 4-(2-aminoethyl) morpholine under the mediation of BOP. The pH fluorescent probe has a good linear relationship between the fluorescence intensity and the pH value within the pH range of 5-8, and completely covers the whole food spoilage process (pH 5.8-7.5); after 4 times of acid-base circulation, the fluorescence recovery rate is gt; therefore, the composite material has excellent reversibility and stability; and the response steady-state value within 1 minute can reach 90% or above. The probe provided by the invention realizes rapid detection, provides an efficient tool for real-time and sensitive monitoring of food freshness, and can be extensively applied to microbial spoilage detection of foods such as aquatic products and dairy products.

The invention provides carbonyl reductase, a gene, a mutant and application of the carbonyl reductase in synthesis of chiral beta-heteroaryl amino alcohol. Alpha-N-heteroaryl aminoketone (general formula I) can be converted to synthesize the chiral beta-heteroaryl amino alcohol (general formula II) through the carbonyl reductase and the mutant thereof. The carbonyl reductase disclosed by the invention is derived from Starmeria magnoliae, the amino acid sequence of the carbonyl reductase is as shown in SEQ ID NO.1, and a carbonyl reductase mutant is obtained by performing single-point mutation or multi-point combined mutation on aspartic acid at the 193 site and valine at the 198 site of the amino acid sequence as shown in SEQ ID NO.1. The carbonyl reductase and the mutant thereof can catalyze alpha-N-heteroaryl amino ketone (general formula I) to synthesize chiral beta-heteroaryl amino alcohol (general formula II), have the advantages of mild reaction conditions, simplicity and convenience in operation, safety, environment friendliness and the like, and have a very good industrial application prospect.

The invention provides a method for preparing alpha-trifluoromethyl-beta-aminoketone by photocatalysis of an isoxazoline derivative, which comprises the following steps of: mixing the isoxazoline derivative, sodium trifluoromethanesulfinate, a photosensitizer, an organic solvent and water in an inert gas atmosphere, stirring and reacting for 12-48 hours at the temperature of 25-35 DEG C under illumination, and filtering to obtain the alpha-trifluoromethyl-beta-aminoketone. And carrying out post-treatment on the obtained reaction liquid to obtain alpha-trifluoromethyl-beta-aminoketone. The method provided by the invention is a method for preparing a target product, which has the advantages of cheap and easily available catalyst, mild reaction conditions, simple operation, greenness and high efficiency.

The invention discloses a synthesis method of a chiral beta-aminoketone derivative, which comprises the following specific synthesis process: dissolving an alpha-vinyl ketone compound, an aromatic amine compound and a chiral primary amine catalyst in a low-polarity organic solvent, and reacting at 20-80 DEG C to obtain the chiral beta-aminoketone compound, a reaction equation in the preparation process is as follows: chiral primary amine is used as a catalyst, the asymmetric protonation reaction of Aza-Michael addition of an organic catalytic alpha-vinyl ketone compound and an aromatic amine compound is realized for the first time, and a brand-new synthesis method is provided for preparing a beta-aminoketone derivative with optical activity.

The invention discloses a method for efficiently synthesizing an alpha-aminoketone compound by taking amino acid as a substrate and combining the synergistic effect of visible light catalysis and nickel metal catalysis. Compared with the prior art, the method has the advantages that the amino acid is directly used as a decarboxylation substrate to be introduced into a light / metal synergistic catalysis system for the first time, and a tedious pre-functionalization step is avoided; a visible light driving strategy is adopted, and the high efficiency of a nickel catalyst is combined, so that the energy consumption and environmental load are reduced. The method is mild in condition and simple and convenient to operate, and a new thought is provided for derivatization of natural products and green synthesis of drug lead compounds. And the substrate has good universality and covers a variety of polar and non-polar amino acids.

The present invention relates to a new aminoketone compound, and a preparation method therefor and the use thereof. Specifically, the compound of the present invention has a structure as shown in formula (I), wherein the definition of each group and substituent are as described in the description. Also disclosed in the present invention are a preparation method for the compound and the use thereof against depression.

Provided is an optical detection chip that makes it possible to accurately measure, in a short time, hydrogen sulfide and methyl mercaptan contained in a gas subject to detection. An optical detection chip is provided with: an optically transparent substrate; and a layer structure provided with a pigment layer that is formed on the optically transparent substrate, that includes organic pigment molecules containing amino groups, ketone groups, or quinones, as well as metal ions of at least one kind selected from the group consisting of Mn, Fe, Co, Ni, Cu, Zn, Cd, Hg, Ag, Pb, and Tl, and that exhibits a color change in response to a gas subject to detection including at least one of hydrogen sulfide and methyl mercaptan.