18 results about "Acrylophenone" patented technology

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.

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 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 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 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.

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.

The application discloses a kind of long-lasting antibacterial high-elasticity body-shaping clothes fabric and preparation method thereof, and relates to the technical field of fabric.The long-lasting antibacterial high-elasticity body-shaping clothes fabric is prepared as follows: first, dihydric alcohol and diester are copolymerized to form a pre-modified polyester, which is then reacted with cyano-(3-thiophene propyl) acetate to form a modified polyester;second, pretreated mica sheet, phosphoric acid and propylene oxide are reacted to form a pre-modified mica sheet, which is then reacted with 2-amino-1H-benzimidazole-5-carboxylic acid, and then reacted with 1,3-bis(3-thiophene)-2-propylene-1-ketone to obtain a modified mica sheet;finally, the modified polyester and the modified mica sheet are blended and spun to obtain modified polyester, which is blended and spun with spandex to form a fabric, and the fabric is finished with thiophene to obtain the long-lasting antibacterial high-elasticity body-shaping clothes fabric.The long-lasting antibacterial high-elasticity body-shaping clothes fabric prepared by the application has good antibacterial, anti-aging and anti-static properties.

The invention discloses a montelukast intermediate synthesis method, and relates to the technical field of chemical synthetic drug intermediates, in the presence of a solvent, in the presence of an alkali and under the catalysis of a nickel catalyst NiBr2 (acac) L, methyl o-bromobenzoate and (E)-1-(3-(2-(7-chloroquinoline-2-yl) vinyl) phenyl) propyl-2-ene-1-one (MK2) are subjected to a coupling reaction, and the montelukast intermediate is obtained. Synthesizing a montelukast sodium intermediate; the novel nickel catalyst NiBr2 (acac) L is adopted, coupling of olefin and halogen at low temperature and pressure is achieved, and the method has great significance for reducing the reaction cost and being suitable for large-scale industrial production.

The present invention relates to a solid form of 1-(4-{[6-amino-5-(4-phenoxyphenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, useful as BTK inhibitors.

The present invention relates to a propylene ketone-containing bioinhibitor, a preparation method therefor, and a use thereof. In particular, the present invention relates to the compound represented by each of the general formulas or a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof in the preparation of a drug for treating cancer and other related diseases.