46 results about "Benzopyrans" patented technology

The invention discloses a double-targeting probe and a preparation method and application thereof.The structure of the double-targeting probe is shown in the formula I. The double-targeting probe has the beneficial effects that SO2 can be monitored in the cell apoptosis process, the dynamic change of SO2 between mitochondria and lipid droplets in cells can be tracked, the core structure of the probe MLR is based on a coumarin part, and the core structure of the probe MLR can be used for detecting the apoptosis of the cells. The probe MLR is connected with a benzopyran cation structure specially designed for detecting SO2, SO2 generated in the death process of copper enables charges of a cation part in the probe MLR to be redistributed, a Michael addition reaction of SO2 and carbon-carbon double bonds is triggered, a fluorescence signal of the probe is changed, and the fluorescence signal is detected. The design of the probe provides a new tool for monitoring key biochemical changes in the copper death process, and is helpful for deeply understanding the molecular mechanism of copper death.

The disclosure relates to a benzopyrylium dye of the formula (I),in which R200, R201, R202, R203, R204, R205, R206, R207 and R208 independently of one another are each hydrogen, C1 to C16 alkyl, C4 to C7 cycloalkyl, C7 to C16 aralkyl, C6 to C10 (het)aryl, hydroxyl, C1 to C6 alkoxy, or dialkylamino, the dialkylamino being selected from the group consisting of diethylamino, dimethylamino, diisopropylamino, a six-membered saturated ring attached via the N of the amino group, which may additionally contain an N or O and may be substituted by nonionic arbitrary radicals, or a combination of at least two thereof, and / or R200 with R201 or R201 with R202 or R202 with R203 and / or R205 with R206 and / or R206 with R207 each independently of one another form a —CH═CH—CH═CH— bridge, and A is a —CH2— or a —CH2—CH2— bridge, where the anion Ann− has a molecular weight of ≥200 g / mol and does not contain a halogen atom.

The present application relates to a kind of 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative purposes, 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative structure as shown in formula I, this 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative has the potential to be developed as anti-radiation drug and antitumor drug.

To provide a novel compound derived from an extract of Agrimonia pilosa.SOLUTION: The invention provides a compound represented by Chemical Formula 3.SELECTED DRAWING: Figure 5

The invention discloses a method for detecting a nebivolol hydrochloride intermediate, namely 6-fluoro-3, 4-dihydro-alpha-[[(phenyl methyl) amino] methyl]-2H-1-benzopyran-2-methanol and an isomer of the nebivolol hydrochloride intermediate, namely 6-fluoro-3, 4-dihydro-alpha-[[(phenyl methyl) amino] methyl]-2H-1-benzopyran-2-methanol. The method can effectively elute, separate and quantitatively detect each component through optimization of chromatographic conditions, is high in sensitivity, strong in specificity and high in accuracy, and provides accurate, rapid and effective quality control for nebivolol hydrochloride products and a preparation process.

The application relates to the technical field of liquid flow batteries, and discloses a low-temperature-resistant liquid flow battery electrolyte, a preparation method thereof and a zinc-bromine liquid flow battery. The low-temperature-resistant liquid flow battery electrolyte comprises water, an electrolyte salt, a supporting electrolyte, a 2-phenyl benzopyran type cationic additive and an alcohol solvent. The 2-phenyl benzopyran type cationic additive has a double regulation function, can synchronously solve the problems of polybromide shuttling effect and zinc negative electrode irreversibility, and can construct a high-performance zinc-bromine liquid flow battery. The alcohol solvent has little influence on the electrolyte conductivity and viscosity, can reduce the freezing point of the electrolyte, and can improve the reaction kinetics of zinc under low-temperature conditions. The interaction between the alcohol solvent and the 2-phenyl benzopyran type cationic additive enables the zinc-bromine liquid flow battery to operate more stably and efficiently under low-temperature conditions, and solves the problem of low energy efficiency of the zinc-bromine liquid flow battery under low-temperature conditions in the prior art.

The present invention discloses a method for preparing a (R)-benzopyran-4-ol compound. The method comprises the following steps: in the presence of a catalyst 8, subjecting a compound represented by Formula II and a hydrogen donor to a reduction reaction as shown below to obtain a compound represented by Formula I. The method has high chiral purity and high yield, and provides a new method for synthesizing a key chiral intermediate of ticlopidine.

The invention relates to the technical field of fluorescence detection and molecular probes, in particular to a fluorescent probe for detecting bivalent palladium as well as a preparation method and application of the fluorescent probe. The fluorescent probe for detecting bivalent palladium is a compound with a structure shown in a formula (I). The fluorescent probe provided by the invention takes benzopyran as a fluorescent parent nucleus and propynyl as a recognition site, and is novel in structure. When the fluorescent probe is used for divalent palladium detection, the fluorescent probe has the characteristics of single selective recognition, high sensitivity and low detection limit (0.18 mu M) on divalent palladium, and the fluorescence intensity of the fluorescent probe and the concentration of divalent palladium are in a good linear relationship within the range of 0-40 mu M. Meanwhile, an application experiment verifies that when the fluorescent probe is used for detecting the divalent palladium in the traditional Chinese medicinal materials, the adding standard recovery rate ranges from 90.8% to 106.4%. Therefore, the fluorescent probe disclosed by the invention has a wide application prospect in the fields of bivalent palladium detection reagents and rapid detection of heavy metals in traditional Chinese medicinal materials.

Provided is an antibacterial application of a 3-phenyl-4H-benzopyran-4-one compound. Specifically, provided is use of a 3-phenyl-4H-benzopyran-4-one compound represented by formula I in the preparation of a product for inhibiting the proliferation of mycobacteria or treating diseases or conditions mediated by the proliferation of mycobacteria, and in the preparation of an in vitro reagent for inhibiting cytochrome bcc-aa3 oxidase and cytochrome bd oxidase of mycobacteria. Further disclosed are use of a 3-phenyl-4H-benzopyran-4-one compound represented by formula I' in the preparation of a product for improving the sensitivity of mycobacteria to cytochrome bcc-aa3 oxidase inhibitors, and a related composition. The compound is used for targeting a new target, and provides a new direction for the inhibition of mycobacterium tuberculosis and the treatment of related diseases.

The invention relates to a silibinin derivative as well as a preparation method and application thereof, and belongs to the technical field of chemistry. The invention relates to a silibinin derivative, which is 6-sulfonated silibinin sodium sulfonate, the chemical name of the silibinin derivative is 2, 3-dihydro-3-(4-hydroxy-3-methoxyphenyl)-2-hydroxymethyl-6-(3, 5, 7-trihydroxy-4-oxo benzopyran-2-yl) benzodioxane-6-sodium sulfonate, the molecular formula of the silibinin derivative is C25H21NaO13S, and the molecular weight of the silibinin derivative is 584.49. Sulfonic acid groups with hydrophilicity are introduced into different parts of the silibinin to prepare different types of silibinin sodium sulfonate, so that the solubility of the silibinin sodium sulfonate in water is enhanced, the pharmacokinetic characteristics of the silibinin are improved from the pharmacokinetic level, the affinity and biological activity of the silibinin to organisms are improved, and the application prospect of the silibinin sodium sulfonate is widened. The compound is further prepared into an injection for clinical treatment, and has important clinical drug treatment value.

The present disclosure relates to the technical field of pharmaceutical preparations, and provides a pharmaceutical preparation containing pranoprofen and a preparation method thereof. 5H-[1]-benzopyrano[2,3-b]pyridine-5-one is subjected to a reduction reaction and a dehydroxylation conversion to obtain 5H-[1]-benzopyrano[2,3-b]pyridine; the 5H-[1]-benzopyrano[2,3-b]pyridine is subjected to an acylation reaction to obtain a 2-halogenated propionyl substituted benzopyranopyridine intermediate; the 2-halogenated propionyl substituted benzopyranopyridine intermediate is treated to obtain crude pranoprofen; the crude pranoprofen is subjected to recrystallization to obtain pranoprofen wet crystals, and the pranoprofen wet crystals are added into an aqueous dispersion solvent to obtain the pharmaceutical preparation containing pranoprofen. The adverse effects of impurity accumulation in the synthesis process in the early stage are reduced, and the dispersion stability of the preparation in the later stage is improved, so that the dispersion stability of the preparation from the early stage to the later stage is realized.

A method of treating or preventing pain and / or inflammation and / or controlling pyrexia or fever, comprising administering (2S)-7-tert-butyl-6-chloro-2-(trifluoromethyl)-2H-chromene-3-carboxylic acid, or a pharmaceutically acceptable salt thereof or a hydrate thereof.

Provided herein are crystalline forms of 3-({[(4R)-7-{methyl[4-(propan-2-yl)phenyl]amino}-3,4-dihydro-2H-1-benzopyran-4-yl]methyl}amino)pyridine-4-carboxylic acid, L-lysine salt, as histone demethylase inhibitors. Also provided herein are pharmaceutical compositions comprising such crystalline forms.

The present invention discloses a benzopyran derivative, a synthesis method, and an application thereof. Trifluoroacetone containing a benzene ring and different heterocycles and a substituted salicylaldehyde are used as raw materials, DMSO is used as a solvent, and a reflux reaction is performed to generate a crude benzopyran derivative with different substituents. The crude product is post-treated to obtain the benzopyran derivative. The reaction is tracked by TLC or liquid chromatography, and the reaction process is simple and easy to operate. Eighteen synthesized compounds were subjected to antifungal activity experiments to determine the antifungal activity of the compounds against Fusarium graminearum, Rhizoctonia solani, Fusarium moniliforme, and Fusarium oxysporum. At 200 ppm, thiophene dibromopyrone had the highest inhibition rate against Fusarium graminearum, at 98.84%; unsubstituted dichloropyrone had the highest inhibition rate against Fusarium graminearum, at 66.08%; pyridine dichloropyrone had the highest inhibition rate against Fusarium oxysporum, at 71.07%; and pyridine dichloropyrone had the highest inhibition rate against Fusarium moniliforme, at 69.12%. The benzopyran derivatives synthesized by the present invention will show good application prospects in various fields such as medicine, organic synthesis, biosensing and optoelectronic materials.

The invention discloses a novel 6, 6, 5-tricyclic compound structure, and in particular relates to a 3a-cyano-4-carbonyl-3-aryl-2, 3, 3a, 4-tetrahydrochroman [3, 4-c] pyrrolidine-9bH-1-carboxylic ester derivative, which is called benzopyran [3, 4-c] pyrrolidine derivative for short. In addition, the invention also discloses a preparation method of the benzopyran [3, 4-c] pyrrolidine derivative, which comprises the following steps: by using a transition metal catalyst, dissolving 3-cyano coumarin and a glycine imine ester derivative as raw materials in an organic solvent according to a certain proportion, and carrying out [3 + 2] 1, 3-dipolar cycloaddition reaction to obtain the benzopyran [3, 4-c] pyrrolidine derivative. The catalytic synthesis method is simple and convenient to operate, the used raw materials are all commercial reagents, the reaction condition is mild, the raw material application range is wide, the product yield is high, and certain stereoselectivity is achieved. The novel 6, 6, 5-tricyclic compound comprises coumarin and pyrrolidine structures with potential biological activity, and the synthetic method provides a synthetic scheme for the compound with potential biological activity and has important application value in the field of drug research and development.

The invention belongs to the field of tumor photodynamic therapy application, discloses a near-infrared photosensitizer as well as a preparation method and application thereof, and particularly relates to a benzopyran nitrile compound shown as a general formula (I). The compound has a near-infrared wavelength luminescence property, can efficiently generate active oxygen to kill tumor cells under an illumination condition, remarkably reduces toxic and side effects, and has good application potential in the field of imaging-induced photodynamic therapy.

The application provides a chromone-modified o-phenanthroline polypyridine Ru(II) series compound and a preparation method and application thereof, the preparation method synthesizes an intermediate A by taking 1,10-o-phenanthroline-5,6-diketone and 6-substituted-4-oxo-4H-benzopyran-3-formaldehyde as raw materials, then the intermediate A is heated to reflux in ethylene glycol solvent and cis-[Ru(2,2'-dipyridine)2Cl2]·2H2O at 120 DEG C for 6h, after the system is cooled to room temperature, an excess amount of a saturated aqueous solution of potassium hexafluorophosphate is added, after a precipitate is separated out, the filter cake is washed with clean water, and the final product is obtained after drying. The synthesis method is simple and easy to operate without steps such as column chromatography.

The invention discloses synthesis of a novel drug small molecular formula (1) containing a coumarin structure and an antitumor activity research formula (1), wherein R is shown in the specification, and R1, R2 and R3 are respectively independent H, OCH3 or COOCH3. 4-hydroxyacetophenone is used as a starting raw material to obtain an important intermediate compound; secondly, enabling an intermediate obtained by carrying out nucleophilic substitution reaction (acylation reaction) on chloroacetyl chloride and different amine compounds to react with 7-diethylamino-3-(4-hydroxybenzoyl)-2-ketone to obtain a drug small molecule containing a coumarin structure, namely a target compound. A CCK-8 experiment is carried out on a target compound, and a conclusion is drawn that methoxy substituted (7b, 7c and 7d): ortho-position methoxy and meta-position methoxy can remarkably inhibit the activity of Hepg-2 cells. Wherein the meta-methoxy group can also significantly inhibit the activity of HeLa cells. (7e, 7f, 7g) substituted by methyl benzoate: only meta-position has strong activity on HeLa. Cyano substitution (7h): the compound has relatively remarkable activity on HeLa and Hepg-2 at the same time.

The present invention proposes a method for synthesizing 6H-benzo[c]chromen-6-one, which belongs to the field of organic synthesis technology. Benzoic acid and iodobenzene are reacted to prepare 6H-benzo[c]chromen-6-one. The present invention starts from benzoic acid, first undergoes an arylation reaction with iodobenzene, and after obtaining the important reaction intermediate 2-arylbenzoic acid, continues to undergo an intramolecular cyclization reaction. A catalyst, an oxidant, an additive, and a solvent are added to a reactor, and the reaction is started. After the reaction is completed, the target product is purified by column chromatography or recrystallization to obtain the target product. Compared with the prior art, the present invention has the advantages of simple reaction operation, short steps, and low cost.

The application discloses a preparation method of a benzopyran derivative containing hexafluoroisopropyl ester, which comprises the following steps: reacting propargyl ether compound, hexafluoroisopropanol and N-iodosuccinimide at room temperature for 15 min, then adding palladium acetate, tris(2-furyl)phosphine, formic acid, acetic anhydride and potassium phosphate to react at 60 DEG C for 24 hours, and after the reaction is completed, post-treatment is carried out to obtain the benzopyran derivative containing hexafluoroisopropyl ester. The preparation method uses hexafluoroisopropanol as a reactant and a promoter, uses formic acid as a carbonyl source, has mild reaction conditions, simple operation, a wide functional group tolerance range of a substrate and high reaction efficiency. According to actual needs, a plurality of benzopyran derivatives containing hexafluoroisopropyl ester can be synthesized, and the method is convenient to operate and wide in practicability.

The invention belongs to the technical field of chemical synthesis of medicines, and particularly relates to a phenanthroline and imidazole terpyridyl ruthenium compound as well as a preparation method and application thereof. The core structure of the phenanthroline and imidazole terpyridyl ruthenium compound is [Ru (L1) (L2) Cl] PF6, L1 is a 4 '-substituted-2, 2': 6 ', 2' '-terpyridyl ligand, and L2 is 6-substituted-3-(1H-imidazo [4, 5-f] [1, 10] phenanthroline-2-yl)-4-oxo-4H-benzopyran. The invention provides chromone modified phenanthroline and imidazole terpyridyl Ru (II) series compounds and a preparation method thereof. The method is simple and easy to implement, and does not need the steps of column chromatography and the like. The data result of the embodiment of the invention shows that the compound provided by the invention has a relatively good inhibition effect on staphylococcus aureus.

The invention discloses a lysosome targeted copper ion fluorescent probe with an AIE (aggregation-induced emission) effect, which is obtained by taking 7-(diphenylamino)-2-oxo-2H-benzopyran-3-carboxylic acid (I) and 8-aminoquinoline (II) as raw materials and reacting and synthesizing under the action of 2-(7-azabenzotriazole)-N, N, N ', N'-tetramethylurea hexafluorophosphate and triethylamine. The chemical structural formula of the fluorescent probe is shown as a formula (III), and the fluorescent probe has an AIE effect, has the advantages of high selectivity and high sensitivity on Cu < 2 + > recognition and the like, and can be used for effectively detecting Cu < 2 + > in an environmental water sample; besides, the probe has good biocompatibility, can be positioned in a lysosome, and is applied to real-time fluorescence imaging monitoring of Cu < 2 + > concentration change in an autophagy process caused by starvation or a chemical inducer in living cells and zebra fish bodies; the invention provides a copper ion detection tool with excellent performance, which has huge potential in the fields of environmental monitoring and life science research.

The present invention relates to a compound or pharmaceutically acceptable salt, hydrate, solvate, N-oxide, stereoisomer, diastereoisomer, enantiomer, atropisomer, dimer or polymorph for use in medicine comprising the following chemical formula (I): wherein R 1 , R 2 and R 3 are selected independently of each other; R 1 is selected from aryl or heterocycle; R 2 is selected from H, alkyl, aryl, alkoxy, halogen, hydroxyl, amine, carbonyl or heterocycle; R 3 is selected from H or (II).

The application provides a triphenylamine-benzopyrylium salt derivative NIR-BT-P and a synthesis method and application thereof.The Chinese name of the derivative NIR-BT-P is (E)-6-(diethylamino)-4-(4(diphenylamino)benzylidene)-1,2,3,4 tetrahydroxanthylium, and the English name is (E)-6-(diethylamino)-4-(4(diphenylamino)benzylidene)-1,2,3,4 tetrahydroxanthylium.The derivative NIR-BT-P is used as a fluorescent probe, different fluorescent intensity signals are achieved in different organic solvents through a fluorescence spectrophotometer, and the polarity is detected.The method utilizes the difference between cancer cells and normal cells in a living body, realizes near-infrared fluorescence imaging, and is used for distinguishing and detecting tumor tissues and normal tissues in the living body.

This invention relates to the field of luminescent materials technology, specifically to a photochromic Pt(II) complex, its preparation method, and its applications. The photochromic Pt(II) complex has the structure shown in formula Pt-A. This invention primarily uses fluorene as a planar chiral framework, and obtains a chiral photochromic Pt(II) complex by modifying the 2-sites of the planar chiral framework. Furthermore, the rigid structure of the photochromic Pt(II) complex of this invention can hinder the ring-closing process of the benzopyran unit, thereby effectively increasing the stability of the chromophore of the chromotropic group and solving the problem of low stability of the chromophores in existing benzopyran-based photochromic compounds.

The present invention relates to solid forms of Compound A, methods of making, and use thereof for the treatment of disease.

The present application relates to a kind of chiral 2-amino benzopyran derivatives with bactericidal activity, and its preparation method and purposes.The chiral 2-amino benzopyran derivatives of the present application have the structure shown in general formula I, and the synthesis process of the present application is simple, and has certain inhibitory effect on plant pathogenic fungi.

The application belongs to the field of medicine, and specifically discloses a benzopyran COX-2 inhibitor and application thereof. The benzopyran COX-2 inhibitor is a compound shown in formula (I) or a pharmaceutically acceptable salt, ester, solvate, stereoisomer, prodrug or isotopic variant thereof. The compound shown in formula (I) has good COX-2 selective inhibitory activity, and an optimal compound has an IC 50 as low as 28 nmol / L, can reduce gastrointestinal side effects and renal toxicity, has excellent inhibitory effect on PGE2, has almost no inhibitory effect on hERG channel current, has low cardiotoxicity, has high stability in human and rat liver microsomes, has a long half-life and a fast peak time when administered orally or by injection, and can be used for the treatment of anti-inflammatory analgesic diseases and tumor-related diseases through injection and oral absorption administration.