84 results about "Acrylophenone" patented technology

The invention discloses novel triazoles compounds, whose chemical names are 3-(substituted phenyl)-1-(2,4-difluorophenyl)-2-(1,2,4-triazol-1-yl)-2-propen-1-one, 1-[3-(substituted phenyl)-1-(2,4-difluorophenyl)-2-(1,2,4-triazol-1-yl)allyl]piperidinium, 3-(substituted phenyl)-1-(2,4-difluorophenyl)-2-(1,2,4-triazol-1-yl)-2-propen-1-ol, and 1-[3-(substituted phenyl)-1-(2,4-difluoropheny)-2-(1,2,4-triazol-1-yl)proyl]piperidinium, with antimicrobial activity; further discloses the preparation method and pharmaceutical use thereof.

The invention provides a fluorescent probe PMPA as well as a preparation method and application of fluorescent probe PMPA. The fluorescent probe is 1-(pyrene-1-yl)-3-(6-methoxypyridine-3-yl) acrylketone. The preparation method comprises the steps of dissolving 1-acetylpyrene and 6-methoxy-pyridinedicarboxaldehyde into absolute ethyl alcohol in the molar ratio of 3:(3-5); adding a sodium hydroxide solution, further stirring at a room temperature for 32h and carrying out TLC tracking reaction; finally adding the absolute ethyl alcohol to generate a bright yellow flocculent; and carrying out standing, suction filtration and dying to obtain a yellow solid. Detection of the fluorescent probe on pH is rate type, detection on HSO3- is fluorescence quenching, and the fluorescent probe can be applied to detection of pH and HSO3- changes in a biological sample through combining a laser confocal microscopy.

The invention relates to a synthetic method of tomoxetine. The tomoxetine is generated by taking (E)-3-(N-methyl amino)-1-phenyl-2-propylene-1-ketone as the material through reduction and 2-benzyl halide etherification reaction. The synthetic method disclosed by the invention is simple in step, easy to operate, less in byproducts, better in yield, lower in cost and suitable for large-scale industrial production.

The invention discloses an asymmetric synthesis method of a gamma-alkenyl substituted butenolide or butenolactam compound. The method adopts cheap nickel to catalyze a [3+2] asymmetric cycloaddition reaction of a cyclopropenone compound and alpha, beta-unsaturated ketone or imine, the selective insertion reaction of intermolecular C=X after nickel-catalyzed C-C bond activation is realized for thefirst time, wherein X is equal to O or N, the gamma-alkenyl substituted butenolide or butenolactam compound is obtained in a high yield, high enantioselectivity and chirality controllable manner, thesynthesis method is novel, condition mildness, substrate with good applicability, simple and efficient reaction, cheap and readily available catalyst, according to the present invention, the synthesisprocess is simple, the atom economy is good, the synthesis product is easy to derivatize, the method can be widely used in completely-synthesized designed synthesis building blocks and new chiral drug derivatives, and the ligand compound is further provided, and can be used for the asymmetric synthesis of gamma-alkenyl substituted butenolide or butenolactam compounds.

The invention discloses application of (1,2,3-trimethoxybenzene)-acrylonitrile to preparing medicine for improving senileretinamacular degeneration. The (1,2,3-trimethoxybenzene)-acrylonitrile servesas an antioxidantcapable of activating two-phase enzyme and enhancing the mitochondrial function, has an inhibiting effect on mitochondrial dysfunction caused by acrolein, has an inhibiting effect oncell activity reduction caused by acrolein, and has an inhibiting effect oncell death caused by acrolein. The effect of the (1,2,3-trimethoxybenzene)-acrylonitrile is completed by activating the two-phase enzyme, and the (1,2,3-trimethoxybenzene)-acrylonitrile has wide pharmacological effects of being anticancer, anti-inflammatory, antibacterial and antiviral, treating diabetes, conducting neuroprotection and the like, and is efficient, safe and tidy medicine.

The invention relates to medicine application, and specifically discloses application of acrylophenone amide derivates to the preparation of anti-osteoporosis medicine. The structural formula of the acrylophenone amide derivates is shown as formula (I) or formula (II). The compound is different from a molecular skeleton of medicine for preventing and treating osteoporosis used clinically at present, does not belong to a phosphate compound, and is neither estrogen medicine. Cytology experiment researches indicate that the compound can inhibit osteoclast differentiation so as to be of an anti-osteoporosis effect; cytotoxicity tests indicate that the compound is little in toxicity, and can be used for preventing and treating related diseases, particularly osteoporosis, caused by osteoclast prosoplasia.

The invention discloses a naphthalene ring-aminopyrimidine type compound as well as a preparation method and application thereof, and belongs to the technical field of preparation of new drug compounds. The preparation method disclosed by the invention comprises the following steps: carrying out an acylation reaction between 1-methoxynaphthalene and substituted phenylacetic acid to prepare 1-(4-methoxynaphthalene-1-yl)-2-substituted phenylethane-1-one; carrying out a reaction between 1-(4-methoxynaphthalene-1-yl)-2-substituted phenylethane-1-one and DMF-DMA to prepare (E)-3-(dimethylamino)-1-(4-methoxynaphthalene-1-yl)-2-substituted phenylpropyl-2-ene-1-one, and finally performing a ring closing reaction with guanidine hydrochloride and potassium carbonate to obtain the naphthalene ring-aminopyrimidine compound as shown in the general formular (I) in the specification. The naphthalene ring-amidopyrimidine compound disclosed by the invention has good activity of inhibiting tubulin polymerization, can effectively inhibit the proliferation activity of human breast cancer MCF-7 cells, can be used as a novel lead compound for antitumor drug research, and is suitable for market popularization and application.

The invention discloses application of a heterocyclic acrylketone type compound as an antibacterial agent. The compound has remarkable antibacterial activity on gram-positive bacteria; in addition, the heterocyclic acrylketone type compound and polymyxin are combined to have remarkable anti-polymyxin drug-resistance bacterium activity on gram-negative bacteria.

The invention belongs to the field of drug synthesis, and relates to a derivative of N-methyl lomefloxacin, in particular to an acrylketone derivative of N-methyllomefloxacin and a preparation methodand application of the acrylketone derivative. The acrylketone derivative of N-methyllomefloxacin has the following structural general formula (I): in the formula, Ar is selected from any one of a benzene ring, a furan ring or a pyridine ring and a substituent group thereof. According to the acrylketone derivative of N-methyl lomefloxacin, a fluoroquinolinone skeleton and an acrylketone skeleton are effectively spliced, so that a novel fluoroquinolinone chalcone-like compound is constructed, the antitumor activity and the drug resistance of the novel compound are improved, the toxic and side effects on normal cells are reduced, and the fluoroquinolinone chalcone-like compound can be used as an antitumor active substance to develop antitumor drugs with brand new structures.

The invention discloses a preparation method of (S)-3-N,N-disubstituted amino-1-(2-thienyl)-1-propanol shown as the formula (I). The method comprises: taking 2-acetyl thiophene shown in the formula (II) as a raw material, and allowing 2-acetyl thiophene to completely react with di(trichloromethyl)carbonic ester (III) and N,N-disubstituted methanamide (IV) in an organic solvent under the catalysis of an organic base to obtain N,N-disubstituted amino-1-(2-thienyl)-1-acrylketone shown as the formula (V); and performing hydrogenation reduction with lithium aluminium hydride to obtain N,N-disubstituted amino-1-(2-thienyl)-1-propanol shown as the formula (VI); and performing splitting with S-mandelic acid and recrystallization with ethyl acetate to obtain the target product shown as the formula (I). The preparation method is low in cost, mild in reaction condition, less in waste water, waste gas and industrial residue, small in energy consumption, and high in yield. The preparation method is safe and is suitable for industrial production.

The object of the present invention is to improve the dissolution and the absorption of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl-1-pyrrolidinyl)-2-propen-1-one effective as an antitumor agent from a pharmaceutical formulation comprising the same. Provided is a pharmaceutical composition comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl-1-pyrrolidinyl)-2-propen-1-one in combination with sodium alkyl sulfate having an alkyl group containing 10 to 18 carbon atoms, in particular, with sodium lauryl sulfate.

The invention provides a preparation method of a 1, 2-dihydrocyclopenta [b] chromene-3, 9-diketone compound, and relates to the technical field of chemistry. According to the preparation method of the 1, 2-dihydrocyclopenta [b] chromene-3, 9-diketone compound, 3-iodo chromone, norbornene and cyclopropenone are taken as raw materials, and a [2 + 2 + 1] series cyclization reaction is carried out in an organic solvent under the condition of a palladium catalyst, so a series of 1, 2-dihydrocyclopenta [b] chromene-3, 9-diketone compounds are synthesized; the compounds contain a chromone skeleton with potential biological activity, can provide a compound source for biological activity screening, and have important application value in the field of medicinal chemistry. Meanwhile, cyclopropenone is used as a unique carbonyl source to participate in the palladium-catalyzed carbonylation reaction for the first time, and a new method is provided for the palladium-catalyzed carbonylation reaction for synthesizing carbonyl compounds.

The invention belongs to the field of drug synthesis, and relates to a derivative without N-methyl ofloxacin, in particular to an acrylketone derivative without N-methyl ofloxacin and a preparation method and application thereof. The compound has a structural general formula (I) as shown in the specification, wherein in the formula I, Ar is any one of a benzene ring, a substituted benzene ring, afuran ring or a pyridine ring. According to the acrylketone derivative without N-methyl ofloxacin and the preparation method thereof, a fluoroquinolinone skeleton and an acrylketone skeleton are effectively spliced, so that a novel fluoroquinolinone chalcone-like compound is constructed, the antitumor activity and the drug resistance of the novel compound are improved, the toxic and side effects on normal cells are reduced, and the fluoroquinolinone chalcone-like compound can be used as an antitumor active substance to develop antitumor drugs with brand new structures.

The invention relates to the field of drug synthesis, and discloses a preparation method and application of a novel chalcone derivative QNL-Chalcone aiming at the problems of insufficient molecular activity and long synthesis route in the prior art. The preparation method comprises the following steps: (1) synthesis of 1-(2-methyl-4-phenylquinoline-3-yl) ethanone; and (2) synthesis of QNL-Chalcone; wherein acetylacetonamine, 2-aminobenzophenone and 2-bromobenzaldehyde are taken as raw materials, and QNL-Chalcone is prepared through the above two preparation steps. According to the invention, quinoline parent nucleuses are introduced, and a chalcone activity essential group: acrylketone structure is reserved, so that the compound QNL-Chalcone with strong anti-depression activity and low side effect is obtained; the synthetic route of the medicine is short, the cost is low, the process is good in controllability and easy for actual large-scale industrial mass production, and the preparedproduct is high in yield and purity.

The invention discloses a method for large-scale production of alpha, alpha, alpha-terpyridyl. The method adopts the following synthetic route: the reaction operation in the step a is as follows: adding 2-acetylpyridine, N, N-dimethylformamide dimethyl acetal and a catalyst into an organic solvent at room temperature, reacting under reflux, and after the reaction is finished, after cooling the reaction solution to room temperature, pouring the reaction solution into a sodium hydroxide aqueous solution, extracting a product by using dichloromethane, washing, drying and concentrating an obtained organic phase, and recrystallizing an obtained crude product to obtain an intermediate, namely 1-(3-pyridyl)-3-(dimethylamino)-2-propylene-1-ketone. The method not only is easy to realize large-scale production, but also is high in yield, low in cost, simple to operate and mild in reaction condition.