39 results about "Acrylophenone" patented technology

The present invention discloses a chalcone-based fluorescent probe, its preparation method and application in detecting H2S, which relates to the technical field of hydrogen sulfide detection. The chalcone-based fluorescent probe of the present invention, the chemical formula of Cha-N3 is (E)-3-(4-azophenyl)-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one. This chalcone fluorescent probe has strong signal enhancement ability in the application of detecting hydrogen sulfide in aqueous environment. The fluorescence enhancement at the emission wavelength of 570 nm can reach 258 times, and qualitative analysis of hydrogen sulfide can be carried out by naked eyes. The detection limit is 122 nM, and it has the ability to monitor low-content hydrogen sulfide. At the same time, the monitoring of hydrogen sulfide in a variety of natural aqueous environments shows that it has strong anti-interference ability, and the fluorescence intensity of Cha-N3 shows a good linear relationship with the concentration of hydrogen sulfide.

A preparation method of compound (R, E)-l-(3-(4-(trifluoromethyl)styryl)pyrrolidin-l- yl)prop-2-en-l-one and crystalline forms thereof.

The invention discloses a method for constructing an alpha-aza-aromatic hydrocarbon substituted propenone compound through dipole reversal alpha-position amination reaction of phosphine-catalyzed acetylenic ketone, and relates to a preparation method of the propenone compound. The reaction of the method can be carried out under the following conditions: small organic molecule triphenylphosphine is used as a catalyst, the temperature is 25-50 DEG C, dichloromethane is used as a solvent, acetylenic ketone and an N-heterocyclic aromatic compound are used as reaction substrates, the corresponding functionalized alkenyl ketone compound is obtained, and the highest conversion rate can reach 99%. The method has the advantages of mild reaction conditions, no use of a metal catalyst, environmental friendliness, wide substrate application range, high yield, simple operation, good regioselectivity and commercially available catalyst, and in addition, the target product alpha-aza-arene substituted propenone has potential biological activity and medicinal value.

The invention discloses a preparation method and application of an alkoxy substituted chalcone derivative, and belongs to the field of medicines, the alkoxy substituted chalcone derivative refers to a compound (E)-3-(3, 4-dihydroxyphenyl)-1-(2, 5-dimethoxyphenyl) prop-2-ene-1-ketone, and the structural formula is shown in the specification. The preparation method comprises the following steps: adding 3, 5-dimethoxyacetophenone into a reaction container, adding absolute ethyl alcohol for dissolving, adding a 60% sodium hydroxide aqueous solution, stirring at room temperature, adding 3, 4-dihydroxybenzaldehyde, stirring at 70-90 DEG C for reaction, cooling to room temperature after the reaction is finished, acidifying with hydrochloric acid, extracting with ethyl acetate, drying with anhydrous sodium sulfate, and concentrating under reduced pressure to obtain the 3, 5-dimethoxyacetophenone. And purifying through silica gel column chromatography to obtain a product. The invention also provides application of the alkoxy-substituted chalcone derivative in preparation of drugs for inhibiting oxidative stress injury of nerve cells and application of the alkoxy-substituted chalcone derivative in preparation of drugs for treating neurodegenerative diseases. # imgabs0 #

Applications of a diphenylpropenone compound of general formula (I), or a stereoisomer thereof, or a geometric isomer thereof, or a tautomer thereof, or a solvate thereof, or an acceptable animal feed salt, in the preparation of an animal feed additive or feed. Confirmed by animal breeding trials, the diphenylpropenone compound, or a stereoisomer thereof, or a geometric isomer thereof, or a tautomer thereof, or a solvate thereof, or an acceptable animal feed salt, can be used as the animal feed additive or animal feed. The weight of the animals can be effectively increased, survival rates can be enhanced, and the compound has a good effect on improving animal production performance.

The invention discloses a benzo [b] azinone compound as well as a synthesis method and anticancer activity thereof, and belongs to the technical field of organic synthesis and drug discovery. The preparation method comprises the following steps: mixing an o-alkenyl aniline compound, a cyclopropenone compound, a catalyst, an additive and an organic solvent, heating, and carrying out a one-pot cascade reaction to prepare the benzo [b] azinone compound. The compounds with various substituents are screened, and anti-cancer cell activity tests prove that the compounds can obviously inhibit proliferation of three kinds of cancer cells, namely Hela, SW-480 and HCT-116, so that the compounds have obvious anti-cancer activity on cervical cancer and / or colon cancer and have potential medicinal value; meanwhile, the synthesis method is simple and efficient in process, and has the advantages that raw materials are cheap and easy to obtain, operation is easy and convenient, atom economy is high, the substrate application range is wide, and functional group tolerance is good.

The invention belongs to the field of organic compounds, and particularly relates to spiro benzoxazine derivatives and a preparation method thereof. The specific technical scheme is as follows: the method for synthesizing the spiro-benzoxazine derivative comprises the following steps: dissolving N-(o-chloromethyl) aryl amide or a derivative thereof and cyclopropenone in an organic solvent, adding alkali, and stirring at 25-40 DEG C for more than 12 hours to obtain the spiro-benzoxazine derivative. The one-step synthesis method provided by the invention is simple and mild in reaction condition and high in product yield, and has a relatively great application prospect.

The invention relates to the technical field of new energy, in particular to a preparation method of C9-C13 cycloalkane. The method comprises the following steps: in the presence of a base catalyst and a solvent, carrying out aldol condensation reaction on acetophenone and furfural or phenylacetaldehyde and furfural to obtain (E)-3-(cyclopent-1, 3-diene-1-yl)-1-phenylpropyl-2-ene-1-one or (Z)-3-(furan-2-yl)-2-phenylacrolein; under the action of a nickel-loaded catalyst, (E)-3-(cyclopentyl-1, 2, 4-triazole-3-yl)- The C9-C13 cycloalkane prepared by adopting the preparation method disclosed by the invention has the advantages of high density, high volume calorific value, excellent low-temperature fluidity and good thermal stability, and can be used for preparing the C9-C13 cycloalkane. The problems of low fuel energy density and insufficient performance in the prior art are solved.

The invention relates to a synthesis method of an abesilib intermediate, which comprises the following steps of: performing Grignard reagent treatment on 3, 5-difluorobromobenzene serving as a raw material, and reacting with 2-fluoro-N-methoxy-N-methylacetamide to obtain 1-(3, 5-difluorophenyl)-2-fluoroethane-1-ketone; then, carrying out nitration reaction to obtain 1-(3, 5-difluoro-4-nitrophenyl)-2-fluoroethane-1-ketone; in the presence of hydrogen and a catalyst, carrying out hydrogenation reduction to obtain 1-(4-amino-3, 5-difluorophenyl)-2-fluoroethane-1-ketone; the preparation method comprises the following steps: introducing acetyl through acetyl chloride, and condensing with N, N-dimethylformamide dimethyl acetal to prepare (Z)-N-(4-(3-(dimethylamino)-2-fluoroacryloyl)-2, 6-difluorophenyl) acetamide; the preparation method comprises the following steps: carrying out cyclization on 2-fluoro-1-(4-fluoro-1-isopropyl-2-methyl-1H-benzimidazole-6-yl) prop-2-en-1-one and isopropylamine under an alkali condition to obtain an abesiril intermediate (Z)-3-(dimethylamino)-2-fluoro-1-(4-fluoro-1-isopropyl-2-methyl-1H-benzimidazole-6-yl) prop-2-en-1-one; and finally, under an alkaline condition, carrying out cyclization on the compound and N-(5-(4-ethyl-piperazine-1-yl methyl) pyridine-2-yl) guanidine nitrate to obtain abesilib.

The invention discloses a separation membrane and a separation method of tanshinone homologues, and belongs to the technical field of separation membranes. The separation membrane takes a nylon membrane as a basement membrane, spherical polyion liquid (PILs) nanoparticles are loaded on the nylon membrane, and a preparation method of the spherical PILs nanoparticles comprises the following steps: by taking 1-vinyl-3-octyl-imidazole bromide, acrylonitrile, divinyl benzene and 2-hydroxy-4 '-(2-hydroxyethoxy)-2-methylallyl ketone as raw materials and 1-octanol as a solvent, carrying out a reaction at the temperature of 50-80 DEG C for 2-4 hours at the temperature of 50-60 DEG C for 1-2 hours to obtain the spherical PILs nanoparticles. Uniformly mixing; pouring the mixture into water, stirring to form an emulsion, and irradiating under 365nm ultraviolet light to carry out photo-initiation polymerization; and pouring the solution into ethanol to form a precipitate, filtering, washing and drying to obtain the PILs nano-particles. The separation membrane disclosed by the invention is high in water flux and has a relatively good separation effect on tanshinone homologues.

The invention relates to a crystal form of a quinazoline derivative and a preparation method thereof. Specifically, the invention provides an E crystal form, a D crystal form and an H crystal form of 1-(inner-3-((4-((4-([1, 2, 4] triazolo [1, 5-a] pyridine-7-yloxy)-2-fluoro-3-methylphenyl) amino) quinazoline-6-yl) oxy)-8-azabicyclo [3.2. 1] oct-8-yl) prop-2-en-1-one, and the E crystal form, the D crystal form and the H crystal form have good stability and can be better used for clinical treatment. Formula (I).

The invention relates to the technical field of organic synthesis, in particular to a coumarin derivative and a preparation method thereof, and the coumarin derivative has a structure as shown in a formula (1). According to the preparation method of the coumarin derivative, ring opening is conducted on cyclopropenone, then Michael addition reaction is conducted on cyclopropenone and nitrogen ylide, and the method is mild in reaction condition, easy to operate and good in yield. Formula (1).

An amorphous solid dispersion, its preparation method, and a pharmaceutical composition thereof are disclosed. The amorphous solid dispersion comprises a compound I named 1-((2S,5R)-5-((7H-pyrrolo[2,3-D]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one and a polymer matrix selected from hydroxypropyl methylcellulose, hydroxypropyl methylcellulose acetate succinate, or copovidone, wherein the mass ratio of compound I to the polymer matrix is ​​1:3 to 1:5. The preparation method comprises dissolving compound I and the polymer matrix together in a mixed solvent of dichloromethane and methanol, followed by spray drying. This invention is the first to discover that combining the free base of compound I with a specific polymer in the above-mentioned ratio to form an amorphous solid dispersion unexpectedly and significantly inhibits its inherent dimerization / oligomerization degradation tendency, exhibits chemical stability far exceeding that of existing crystalline formulations, and maintains good dissolution performance.

The invention discloses a method for synthesizing an indene compound, which comprises the following steps: reacting a 2-iodo styrene compound and diaryl cyclopropenone which are used as raw materials in an organic solvent under the combined action of a palladium catalyst, a ligand and alkali, and carrying out post-treatment after the reaction is finished to obtain the indene compound. The reaction formula of the synthesis method is as follows: in the # imgabs0 # formula, R1 is selected from one of hydrogen atom, alkyl, alkoxy and halogen; r2 is selected from one of a hydrogen atom, an alkyl group, an alkoxy group, an ester group and an acyl group; r is alkyl. According to the present invention, the easily prepared 2-iodo styrene compound and the commercial diaryl cyclopropenone are adopted as the raw materials, three chemical bonds are constructed through the one-pot method, and the rapid synthesis of the indene compound having the four-membered ring structure is achieved; the reaction has the advantages of simplicity in operation, low reaction cost, wide substrate applicability, easiness in separation of a target product and the like.

The invention relates to chemistry and agriculture, namely to the use of a 1,2,4-triazole derivative as an active compound againstFusarium lateritium.According to the invention, claimed is the use of (Z)-1-(2,4-dichlorophenyl)-3-(2-hydroxyphenyl)-2-(1H-1,2,4-triazol-1-yl)prop-2-en-1-one as an active compound against the phytopathogenic fungus of the speciesF. lateritium- one of the causative agents of root rot.The technical result consists in increasing the fungitoxic activity of the compound of the invention in relation to the closest solution by 6.5…21.6% for strain 17 of the fungusFusarium lateritiumon the last day of cultivation, in the concentration range of 0.02…0.01%, respectively.

The present invention provides a novel compound having a chromanone or its ring-opening form, phenylpropenone, as backbone and compositions for the preventing or treating multiple myeloma, comprising the same. The compounds of the invention exhibit significant killing effects against various multiple myeloma cell lines and show in vivo anti-cancer effects that exceed those of lenalidomide, a commercially available immunomodulator widely used in the treatment of multiple myeloma and myelodysplastic syndromes. In addition, the compounds of the invention exhibit a significant synergistic effect when co-administered with the thalidomide or its analog lenalidomide, and thus are useful as an efficient therapeutic agent or therapeutic aid agent composition for multiple myeloma which is an incurable disease.

The present invention discloses ibrutinib and a synthesis method thereof, comprising the following steps: (1) using SM1 (4-phenoxybenzoyl chloride) as a raw material, and carrying out a coupling reaction with SM2 (4,6-dichloropyrimidine) under the condition of a catalyst to obtain an intermediate M1 ((4,6-dichloropyrimidin-5-yl)(4-phenoxyphenyl)methyl ketone); (2) carrying out a cyclization reaction between M1 and SM3 (1-(3R-hydrazino-1-piperidinyl)-2-propylene-1-one) to obtain to the intermediate M2 (1-((R)-3-(4-chloro-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one); (3) subjecting M2 to a chlorination amination reaction to obtain ibrutinib (1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one). The ibrutinib synthesis method provided by the present invention has a reasonable route design, mild reaction conditions in each step, strong operability, low cost, high yield, simple process operation, is suitable for large-scale industrial production, and is of great significance.

The invention relates to a novel compound as well as a preparation method and application thereof, in particular to a derivative of (E)-3-aryl-1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-2-(trifluoromethyl) propan-2-ene-1-one as well as a preparation method and application of the derivative of (E)-3-aryl-1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-2-(trifluoromethyl) propan-2-ene-1-one. The structural formula of the (E)-3-aryl-1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-2-(trifluoromethyl) prop-2-ene-1-one is shown as a formula I, and R is selected from chlorine, bromine, methyl, methoxyl, 2, 3, 4-trimethoxy, ethyoxyl, nitryl and 2, 4-dichloro, and the structural formula of the (E)-3-aryl-1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-2-(trifluoromethyl) prop-2-ene-1-one is shown as a formula I. The invention further discloses a preparation method of the (E)-3-aryl-1-(2, 2-dimethyl-2, 3-dihydrobenzofuran-5-yl)-2-(trifluoromethyl) prop-2-ene-1-one. Experiments show that the compound disclosed by the invention especially shows relatively good antifungal activity on botryosphaeria dothidea and pythium aphanidermatum, and the activity of a part of drugs is equivalent to that of the drug fluxapyroxad on the market. The compound provided by the invention can provide more choices for research and development of antifungal drugs, and has a wide application prospect. # imgabs0 #

The present disclosure relates to a solid crystalline form of (R)-1-(3-(3-(4-aminopyrimidin-2-yl)-5-chlorophenyl)morpholino)prop-2-en-1-one and to methods for preparing such crystalline form. (R)-1-(3-(3-(4-aminopyrimidin-2-yl)-5-chlorophenyl)morpholino)prop-2-en-1-one is a potent KEAP1 modulator.

The invention discloses a preparation method of heterocycle-substituted gamma, delta-unsaturated butene lactone in the technical field of organic synthesis, and the synthesis route is as follows: # imgabs0 #: step 1, sequentially adding a metal palladium catalyst, a phosphine ligand, alkali, cyclopropenone and different iodobenzene-substituted olefins, then adding an organic solvent to obtain a mixture, and reacting for 2-4 hours; stirring the mixture at a certain reaction temperature under the protection of inert gas; and 2, after the reaction is finished, carrying out post-treatment separation to obtain the corresponding heterocycle substituted gamma, delta-unsaturated butene lactone. Researches find that the compound has the activity of resisting leukemia, lung cancer, liver cancer, breast cancer and colon cancer.

The invention relates to a crystal form containing an acrylketone biological inhibitor and a preparation method and application thereof. In particular, the present invention relates to a crystal form of a compound represented by general formula (I), a preparation method thereof, a pharmaceutical composition containing a therapeutically effective amount of the salt and / or the crystal form, and a use thereof as an inhibitor in the treatment of cancer.

The invention relates to the technical field of benzimidazole isoquinoline ketonization reaction, in particular to a synthesis method of benzimidazole isoquinoline ketonization reaction. The method comprises the following steps: sequentially adding potassium persulfate, a reactant I, a reactant II, a dimethyl sulfoxide and water mixed solution and a NO.5 magneton into a reactor, connecting a condenser pipe, introducing condensed water from bottom to top, putting the reactor into an oil bath pan at 100-120 DEG C, heating, stirring and reacting for 0.5-2 hours, terminating the reaction, filtering, washing, and drying to obtain a target product. Purifying the product to obtain a benzimidazole isoquinolinone product; the reactant I is selected from one of N-phenylpentyl-4-enamide, N-(p-tolyl) pentyl-4-enamide, N-(4-fluorophenyl) pentyl-4-enamide and N-(4-chlorphenyl) pentyl-4-enamide, and the reactant II is selected from one of N-phenylpentyl-4-enamide, N-(p-tolyl) pentyl-4-enamide and N-(4-chlorophenyl) pentyl-4-enamide; the reactant II is selected from the group consisting of 2-methyl-1-(2-phenyl-1H-benzo [d] imidazole-1-yl) prop-2-en-1-one, and the reactant II is selected from the group consisting of 2-methyl-1-(2-phenyl-1H-benzo [d] imidazole-1-yl) The method is mild in reaction condition, high in selectivity, relatively high in yield and environment-friendly; the benzimidazole isoquinolinone compound can be used in the field of synthesis of drugs, pesticides and paint dyes.

The invention relates to the technical field of medicinal chemistry, and discloses a 1-indanone derivative as well as a preparation method and application thereof. The structural general formula of the 1-indanone derivative is as shown in formula I: # imgabs0 # R1 is Me-or naphthenic base; r2 is Me <->, alkyl or alkyl impurity; r3 is Me <->, aryl or substituted alkyl; r4 is selected from alkyl or halogen. The 1-indanone derivative prepared by the invention is a compound with a brand-new structure, has certain biological activity, and can be used as a potential drug or a candidate drug molecule for research in the aspects of cancer resistance, tumor resistance, inflammation resistance, bacteria resistance and the like. The invention also provides a preparation method of the 1-indanone derivative, cyclopropenone and olefin are used as raw materials, one-step synthesis is performed under the action of a catalyst, a solvent and a reducing agent, and the 1-indanone derivative has the advantages of simplicity in operation, higher yield, good selectivity, wide substrate adaptability, convenience in industrial production and the like.

Applications of a diphenylpropenone compound of general formula (I), or a stereoisomer thereof, or a geometric isomer thereof, or a tautomer thereof, or a solvate thereof, or a salt acceptable for feed in the preparation of an animal feed additive or animal feed. Confirmed by animal breeding test, the diphenylpropenone compound, or the stereoisomer thereof, or the geometric isomer thereof, or the tautomer thereof, or the solvate thereof, or the salt acceptable for the feed can be used as the animal feed additive or the animal feed. Animal weight can be effectively increased, survival rates can be enhanced, and the compound has a good effect of improving animal production performance.

To provide an ophthalmic composition that prevents the occurrence of precipitation and the like.SOLUTION: An ophthalmic composition contains (A) at least one selected from the group consisting of tranilast and a salt thereof, (B) at least one selected from the group consisting of polyvinyl pyrrolidone and trometamol, and (C) at least one component selected from the group consisting of (C1) anti-histamine agent, (C2) anti-inflammatory agent, and (C3) amino acid, wherein a sodium ion concentration is set to be 250 mM or less, or the ratio of sodium ions is set to be 25 mol or less relative to (A) component 1 mol.SELECTED DRAWING: None

Hair treatment method comprising the application of an oil-in-water emulsion comprising an aqueous phase, an oily phase, and a polymer. The present invention relates to a hair treatment method comprising the application of an oil-in-water emulsion comprising: - at least one aqueous phase, - at least one oily phase comprising at least one oily substance, - at least one polymer comprising at least one 2-acrylamidomethylpropanesulfonic acid unit. Figure for the abstract: NONE