78 results about "Aminoketone" patented technology

The invention provides an alpha, beta unsubstituted 1, 4-ketoaldehyde compound and a metal-free photocatalytic aqueous solution acetaldehyde alpha-position selective single alkylation reaction preparation method and application thereof, a photosensitizer and alpha bromine / chloro aryl ethyl ketone are mixed in an organic solvent, then TEEDA, nBu4NI and an acetaldehyde aqueous solution are sequentially added, white light irradiation stirring reaction, separation and purification are performed, and the alpha, beta unsubstituted 1, 4-ketoaldehyde compound is obtained. Compared with the prior art, the method has the advantages that by improving the light source, the reaction can be amplified to the gram scale level, the yield of the corresponding alpha and beta unsubstituted 1, 4-ketoaldehyde product is not obviously reduced, and a basis is provided for the industrialization process of the reaction. The reaction disclosed by the invention has the characteristics of wide substrate range, high functional group tolerance, simplicity in operation, mild reaction conditions and the like. Moreover, the product disclosed by the invention can be subjected to reductive amination with cyclic secondary amine to obtain a series of gamma-aminoketones with biological activity, which shows that the reaction has potential synthesis application value in the field of pharmaceuticals.

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.

A method for preparing glycine by using threonine relates to a fermentation process in which threonine is decomposed into glycine and acetaldehyde by aldolase. Glycine and acetyl coenzyme A can be produced in a fermentation process, in which acetaldehyde is reduced into acetyl coenzyme A or an acetyl coenzyme A derivative by acetylating acetaldehyde dehydrogenase; or threonine is dehydrogenated by threonine dehydrogenase to obtain 2-amino-3-ketobutyric acid, which is then ligated by 2-amino-3-ketobutyrate CoAligase to obtain acetyl coenzyme A. Coenzyme A can be converted into an acetyl coenzyme A derivative under different fermentation conditions.

The present invention discloses a preparation method for synthesizing α-amino ketone compounds from fatty aldehydes and secondary amines, belonging to the technical field of organic chemical synthesis. The fatty aldehyde, secondary amine, and sodium percarbonate are added to a reaction vessel for mixing, and the reaction is carried out at a temperature of 95 to 115 °C for 16 to 24 hours. After purifying the reaction mixture, α-amino ketone compounds are obtained. The fatty aldehydes and secondary amines used in the method of the present invention are commercially available raw materials or are prepared from commercially available primary alcohols and primary amines through simple oxidation or reduction; the substrate has a wide range of applicability and is applicable to the above-mentioned various fatty aldehydes and secondary amines. The method of the present invention can be prepared only by oxidizing and rearranging with cheap and easily available sodium percarbonate, without the need for additional catalysts and additives, and has the characteristics of high economy, wide commercial sources, and environmental friendliness; the method of the present invention has few reaction steps and has the characteristic of simple operation.

The present invention relates to the field of Mannich base synthesis, and specifically relates to a pyrazole-based ionic liquid 1,2-dibenzyl-3,5-dimethylpyrazolium salt and its synthesis method, and provides a method for catalyzing the Mannich reaction therewith; at room temperature, the pyrazole ionic liquid is used as a catalyst and a solvent, and an aromatic aldehyde, an aromatic amine and cyclohexanone are subjected to a three-component Mannich reaction, and the product and the catalyst are separated with ethanol to obtain the Mannich base β-aminoketone; by screening the types of ionic liquids, solvents, the molar ratios of reactants, the dosage of ionic liquids and reaction temperatures, a series of Mannich bases with higher yields are obtained under the optimized conditions, and the yields are in the range of 77% - 93%. Moreover, the catalyst used is green and effective, has good thermal stability, can catalyze the synthesis of Mannich bases in a short time, the product and the catalyst are easily separated, and the catalyst can be recycled multiple times without obvious reduction in activity.

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 discloses a preparation method of alpha-aminoketone compounds, which is characterized in that in the presence of water as a reaction solvent and inorganic base, iodine as an accelerant, propiophenone compounds and amine compounds are subjected to sp3 C-H amination reaction to prepare a series of alpha-aminoketone compounds at high yield. Compared with the prior art, the method has the advantages that the use of an organic solvent and organic alkali is avoided, the production cost and the operation difficulty are remarkably reduced, and meanwhile, the atom economy and the production safety of the preparation process are also remarkably improved. The method disclosed by the invention has good substrate universality, can be carried out at room temperature, is simple in preparation and post-treatment operation and pollution-free, conforms to the green chemical development concept, and is suitable for industrial production.

The present invention relates to the technical field of pharmaceutical synthesis and development of drugs, and to a process for preparing cyclic 2-amino-1-one derivatives and to the reaction products and intermediates obtainable by this process. The present invention further relates to pharmaceutical compositions, in particular drugs or medicaments, comprising the cyclic 2-amino-1-one derivatives and to their use as medicaments, in particular in the prophylactic or therapeutic treatment of diseases of the human or animal body, preferably of neurodegenerative diseases or psychiatric disorders.

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 invention provides a method for rapidly synthesizing thiocyanate-substituted formanilide, belonging to the technical field of organic chemical preparation. Alpha-aminoketone and potassium thiocyanate are used as starting raw materials. Under the conditions of a copper catalyst, an oxidant and an organic solvent, the mixture is sealed and placed in an oil bath pot, stirred at 80°C, and heated for reaction for 24 hours. After the reaction is completed, the mixture is purified by column chromatography to obtain a thiocyanate-substituted formanilide compound. The copper catalyst comprises any one of copper chloride, copper acetate, copper sulfate, copper acetylacetonate and copper trifluoromethanesulfonate. The oxidant comprises one of iodophenyldiacetic acid, potassium persulfate, di-tert-butyl peroxide and tert-butyl peroxide. The method overcomes the problems of many reaction steps and low synthesis efficiency in the prior art and has the advantages of easy availability of raw materials, simple operation and the like.

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 for synthesizing an amide compound through photochemical driving, which comprises the following steps of: reacting a compound 1 as a raw material in acetonitrile under illumination for time t, and reacting through a dichloromethane system of iodine, triphenylphosphine and triethylamine to obtain a product 1; according to the method, the reaction conditions are relatively mild, and photochemical driving is utilized, so that the energy consumption and harsh condition requirements of the traditional thermal reaction are reduced; precise conversion of a compound with a specific alpha-aminoketone structure can be realized, a new path is provided for synthesis and modification of amide compounds, and preparation methods of the amide compounds in organic synthesis and related application fields are expanded.

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 discloses the preparation and application of a 5-aminolevulinic acid biosensor, relates to the technical field of biosensors, and comprises the following steps: step one: design and synthesize an RNA aptamer sequence with high affinity and specificity for 5-ALA; step two: combine the RNA aptamer sequence with the expression regulation region of a fluorescent reporter gene to construct a riboswitch structure; step three: clone the riboswitch structure into an expression vector, transform Escherichia coli or yeast; step four: screen and optimize the engineering strains for efficient expression; step five: immobilize the engineering strains on a biocompatible material to prepare a biosensor chip. In the present invention, an RNA aptamer capable of specifically recognizing 5-ALA is designed and combined with the expression regulation of a fluorescent reporter gene to achieve rapid and sensitive detection of 5-ALA.

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 a diaryl thioether photoinitiator as well as a preparation method and application thereof, an aryl thioether photocompound is prepared by reacting substituted benzene with sulfur chloride, and the preparation method specifically comprises the following steps: reacting a substituted benzene compound with S2Cl2 to synthesize an intermediate diaryl thioether compound; the preparation method comprises the following steps: reacting diaryl sulfide with parachlorobenzophenone or parachlorophenyl aminoketone, and synthesizing to obtain an aryl sulfide benzophenone compound or an aryl sulfide alpha-aminoketone compound; according to the synthesis method, thiophenol with stink is not used, and the preparation process is green and environment-friendly and is easy to industrialize; the synthesized compound can be used as a photoinitiator and shows a better photocuring effect.

A new aminoketone compound, and a preparation method therefor and the use thereof are provided. Specifically, the compound has a structure as shown in formula (I), wherein the definition of each group and substituent are as described in the description. A preparation method for the compound is provided. The compound can be used to treat depression.

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.

Disclosed are plasticizer compositions in the form of crop-based secondary amines prepared through catalyzed reductive amination (RA) of furans with aminated ketones. Exemplary furans include, but are not limited to, furfural, 5-(hydroxymethyl) furfural (HMF), and 2,5-diformylfuran (DFF). These furans may be crop-based. Furfural, for example, may be made through dehydration of xylose isolated from corn cobs. Exemplary aminated ketones include, but are not limited to, crop-based aminated ketones such as 2-aminoundecane. For example, 2-aminoundecane may be prepared through catalyzed RA of 2-undecanone from the seed oil of Cuphea. These RA reactions may be catalyzed using, for example, Pd / C. In some embodiments, the plasticizer compositions function as plasticizers when blended with polyvinylchloride (PVC) and / or other polymers to form plasticized compositions. Processes for making the plasticizer compositions and plasticized compositions are also disclosed. The plasticizer compositions provide a sustainable and comparable alternative to known petroleum-based phthalate ester plasticizers, such as diethylhexyl phthalate (DEHP).

The invention relates to a Metal-containing film forming composition comprising a precursor having the formula M(=NR)X2L, in which M = V or Nb or Ta; R = H or C1-C10 alkyl group; X = Substituted or unsubstituted diketones, aminoketones, alkoxyalcohols, alkoxyalkanes, alkanediols, alkanolamines, aminoaldehydes, diimines, dienes; and L = Substituted or unsubstituted cyclopentadienes, cyclohexadienes, cycloheptadienes, cyclooctadienes, fluorenes, indenes, fused ring systems, propenes, butadienes, pentadienes, hexadienes, heptadienes.

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.

The invention belongs to the technical field of chemical synthesis methods, and discloses a synthesis method of beta-carboline compounds. The method comprises the following steps: cyclizing alpha-aminoketone (A) and 3-substituted acrolein (B), reacting the obtained product with hydroxylamine hydrochloride without purification under the catalysis of acid to prepare a 3-aminopyridine derivative, and synthesizing a compound with a beta-carboline structure as shown in a general formula I or a general formula II in the presence of an alkaline reagent or a copper catalyst. According to the method provided by the invention, alpha-aminoketone is taken as a raw material, the beta-carboline compound can be synthesized under a metal-free condition, and the route is short. The synthesis method has a high-efficiency and high-yield synthesis route for natural products, namely harmine and harmine. The synthesis method disclosed by the invention can be used for synthesizing harmine and harmine. The method is simple to operate and high in yield, and provides a new idea for efficient synthesis of the compounds.

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.