91 results about "Pyran" patented technology

The application belongs to the field of compound synthesis, and discloses a kind of compound containing seven-membered lactam and pyrone skeleton and its construction and application, and the chemical structure is shown in the following, wherein R1 is selected from any one of hydrogen, alkyl, halogen;R2 is selected from any one of alkyl, aryl;R3 is selected from any one of hydrogen, phenyl.The seven-membered lactam and pyrone skeleton has good drug activity, and can be used for preparing antitumor drugs.The application also discloses a construction method of the seven-membered lactam and pyrone skeleton.The construction method of the seven-membered lactam and pyrone skeleton has the advantages that raw materials and catalysts are cheap and easy to obtain, operation is simple and convenient, and the universality of substrates is wide.

This invention provides a method for screening β-galactosidase inhibitors, belonging to the field of pharmaceutical technology. The first step of this method uses fluorescence sensing technology to rapidly identify natural products with β-Gal inhibitory activity. The principle is based on the fluorescence quenching property of p-nitrophenol (PNP) on sulfur quantum dots (SQDs); β-Gal catalyzes the hydrolysis of p-nitrophenyl-β-D-galactopyranoside (PNPG) to generate the specific product PNP; in the presence of β-Gal, PNPG can be enzymatically catalyzed to generate PNP, quenching the fluorescence of SQDs; when screened for β-Gal inhibitory activity, the fluorescence of SQDs can be restored. The second step uses affinity chromatography to capture components in samples with β-Gal inhibitory activity. This method involves immobilizing β-Gal on a support material, eluting with a solvent to obtain components that can bind to β-Gal, and then using liquid chromatography-mass spectrometry (LC-MS) to identify the components. This method can rapidly and accurately screen β-Gal inhibitors from natural products.

Provided herein are compounds of Formula (II) (e.g., Formula (II-a), (II-b), (II-a1), (II-b1), (II-a2), (II-b2), (II-3), (II-a3), (II-4), (II-a4), (II-5), (II-a5), (II-6), (II-a6), (II-7), (II-a7), (II-7), or (II-a8)), Formula (III) (e.g., Formula (III-1), (III-2), (III-3), (III-4), (III-5), (III-6), (III-7), or (III-8)), Formula (IV) (e.g., Formula (IV-a), (IV-b), (IV-c), (IV-a1), (IV-b1), (IV-a2), (IV-b2), (IV-a3), (IV-b3), (IV-a4), (IV-b4), (IV-a5), (IV-b5), (IV-a6), (IV-b6), (IV-a7), (IV-b7), (IV-a8), or (IV-b8)), Formula (V) (e.g., Formula (V-a) or (V-b), (V-a1), (V-c), (V-d), (V-b1), (V-a2), (V-b2), (V-a3), or (V-b3)), Formula (VI) (e.g., Formula (VI-a), (VI-b), (VI-c), (VI-d), or (VI-e))), or Formula (A) (e.g., Formula (I-a1)), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein (e.g., a dysregulated KRas protein (e.g., a mutated or amplified KRas protein)). This disclosure also provides compositions containing the compounds as provided herein, or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

This invention discloses a green synthesis process for 2-chloropyranose-1-yl)-4'-ethoxydiphenylmethane, belonging to the field of pharmaceutical intermediate preparation. The method involves forming a mixture of a substrate in the protected state of Formula I and a reducing agent containing siloxane bonds, which is continuously fed into a microreactor loaded with a confined-domain MOF (Metal-Oxide-Fractions) supported catalyst for room-temperature reduction. The MOF catalyst has a rigid pore size of 1.2~2.5 nm and internally coordinates and anchors metal trifluoromethanesulfonate. This invention utilizes the limiting confinement effect of rigid channels to lock the substrate conformation, blocking the surface attack of reactants and achieving extremely high configuration selectivity. Simultaneously, the efficient mass transfer of the continuous flow microchannel and the online infrared spectroscopy closed-loop control system completely eliminate the need for traditional cryogenic conditions, remove highly corrosive fluorine-containing waste liquid, significantly reduce synthesis costs, and achieve efficient, green, and stable continuous industrial production of this core intermediate.

The present application belongs to the technical field of electronic atomization, and particularly relates to a tobacco extract composition, a preparation method and application thereof. The tobacco extract composition comprises methylcyclopentenolone, guaiacol, neophytadiene, cedrene diol, dihydroactinidiolide, maltol, furaneol, palmitic acid, 6-ethyl-5,6-dihydro-2H-pyran-2-one and scopoletin; the range of (methylcyclopentenolone+guaiacol) / neophytadiene is 0.01-2.5 by mass; the guaiacol content is 0.003-0.02 mg / g by dry matter mass; the tobacco roasting aroma is richer, the tobacco roasting sweet note is more obvious, and the tobacco-like feeling is better. The preparation method comprises: extracting tobacco raw materials twice at medium and low temperatures to obtain tobacco flavor substances, extracting the tobacco raw materials at high temperature to obtain smoke flavor substances, and mixing the tobacco flavor substances and the smoke flavor substances at a certain ratio to obtain the tobacco extract composition.

The invention discloses a piperazine bridged ring substituted pyrimidinopyran compound and application thereof, and particularly discloses a compound as shown in formula (I ''), (I ') or formula (I), and a stereoisomer and pharmaceutically acceptable salt thereof.

This invention discloses a sulfated arabinoglycoside, its preparation method, and its applications, belonging to the field of biomedical technology. The technical solution includes a sulfated arabinoglycoside derived from *Streptococcus linearis* polysaccharide; a degree of polymerization of 2-5; arabinose as the main monosaccharide, and containing galactose; the molar percentage of arabinose is not less than 80%, and the molar percentage of galactose is not more than 20%; the main chain is composed of (1→4)-β-L-pyranose arabinose groups, with the sulfate groups of the arabinose mainly substituted at the C-3 position. This invention is applied to inhibiting the abnormal aggregation of human pancreatic islet amyloid peptide (hIAPP), solving the problem of the lack of safe and effective intervention methods for the abnormal aggregation of human pancreatic islet amyloid peptide in existing technologies. It features stable raw material sources, high safety, a simple and mild preparation method suitable for large-scale preparation, and the ability to inhibit the abnormal aggregation of human pancreatic islet amyloid peptide and reduce pancreatic β-cell damage.

The present application relates to a kind of 2-aryl-3-carbonyl-substituted tetrahydrofuran and tetrahydropyran compound preparation method, its reaction general formula is as follows: the present application is prepared by one-pot method under photocatalytic condition 2-aryl-3-carbonyl-substituted tetrahydrofuran and tetrahydropyran compound of unsaturated alcohol, alkyl or aryl acyl oxime ester.The starting material of this method is cheap and easy to obtain, simple operation, mild reaction condition, avoid using the dosage of oxidizing agent and additional reagent, provide a kind of green and efficient preparation method for 2-aryl-3-carbonyl-substituted tetrahydrofuran and tetrahydropyran compound.

The present disclosure relates to methods of treating neurological or psychiatric diseases or disorders, such as schizophrenia. Compound 1, or a pharmaceutically acceptable salt thereof, is an antipsychotic agent with a non-D2 mechanism of action. Adverse events associated with antipsychotic agents that target the D2 dopamine receptor can be reduced by treating disorders with Compound 1, or a pharmaceutically acceptable salt thereof.

The present disclosure relates to crystalline polymorph forms of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7H-imidazo[1,5-a]pyrazin-8-one.

The present invention provides a pyranone compound represented by formula (I). The pyranone compound has excellent anti-inflammatory activity and cholinesterase inhibitory activity, features a high blood-brain barrier penetration potential and good safety, and can ameliorate cognitive impairment related to Alzheimer's disease, reduce glial cell activation, decrease Aβ deposition and alleviate neuroinflammation.

This disclosure relates to a hair care composition comprising a compound that can covalently bond to hair and an excipient suitable for administration to hair, wherein the compound that can covalently bond to hair is a compound of formula (I), or its tautomers and / or pharmaceutically acceptable salts, where (I), R 1 L1 represents a protecting group that can be hydrolyzed under physiological conditions after application of hydrogen or a hair care composition to the hair, L1, L2 and L3 independently represent a linker group or are absent, and A1, A2 and A3 independently represent a)C1~C 30 Partial, H, hydroxyl, amino, or halogen, or b) C1-C 60 Represents a part or polymer part, and at least one of A1, A2 and A3 is C1-C of group b). 60 It is a part or polymer part, and C1-C of group b) 60 The present invention relates to a hair care composition in which the polymer portion is configured to act as b1) a humectant, a hair beautifying coating, or a primer for adhering dye to hair, and / or b2) a humectant, a hair beautifying coating, or a fragrance for cleavage from the 3,4-dihydro-2H-pyran portion, and L1-A1 and L2-A2 do not represent portions containing an unsaturated CC bond or CN bond at the alpha position to the carbon atoms marked "a" and "b", respectively. [Formula 1] JPEG2026520679000070.jpg29128

A tobacco extract composition, a preparation method therefor, and a use thereof, relating to the technical field of electronic atomization. The tobacco extract composition comprises methyl cyclopentenolone, guaiacol, neophytadiene, a cembratriene-diol, dihydroactinidiolide, maltol, furanone, palmitic acid, 6-ethyl-5,6-dihydro-2H-pyran-2-one, and scopoletin. By weight: (methyl cyclopentenolone + guaiacol) / neophytadiene ranges from 0.01 to 2.5. By dry weight: the guaiacol content is 0.003 to 0.02 mg / g. Said tobacco has a rich roasted aroma, a pronounced sweet roasted flavor, and a more tobacco-like feel. The preparation method comprises: performing extraction on tobacco raw material twice at medium and low temperatures, and obtaining tobacco flavor compounds; performing extraction on the tobacco raw material at a high temperature, and obtaining smoke flavor compounds; and mixing the tobacco flavor compounds and the smoke flavor compounds in a certain ratio to obtain a tobacco extract composition.

To provide a compound exhibiting a high external quantum efficiency which is suitable as a photoelectric conversion material for blue light, a method for simply synthesizing the compound and a photoelectric conversion element containing the compound.SOLUTION: There is provided a pyran derivative represented by the formula (1). In the formula, R1 to R6 each independently represent H and an alkyl group having 1 to 4 carbon atoms; X1 and X2 each independently represent H, a halogen atom, a trifluoromethyl group or a cyano group and at least one of which is a cyano group; Ar1 represents an aryl group having 6 to 18 carbon atoms or a heteroaromatic group having 2 to 5 carbon atoms and the aryl group and heteroaromatic group may be substituted with one or more substituents selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an aryl group having 6 to 10 carbon atoms, a dialkylamino group having 2 to 5 carbon atoms and a diarylamino group having 12 to 18 carbon atoms; Ar2 represents a heteroaromatic group such as a benzofuran group.SELECTED DRAWING: None

The present invention relates to a mixture, blend or combination, comprising at two, preferably at least three, chosen from the following compounds: (A) a pyrone derivative, (B) a tropolone derivative, (C) a phenylpropanoid, (D) a monoterpene or monoterpenoid, (E) an aromatic acid or salt, (F) a dipeptide, and (G) an alkanediol, and its use as chelating mixture.

The present application relates to a kind of small molecule probes and its preparation method and application, the chemical structure of the probe is as shown in the following formula: Wherein, R1 is 1-propyl sulfonic acid or 1-butyl sulfonic acid;R2 independently selected from trifluoromethyl or sulfur pentafluoride group, the substitution position of R2 is the ortho, para or meta of hydroxyl on benzene ring;Preparation method is by the condensation reaction of salicylaldehyde containing fluorine substituent group and indoline, directly introduce containing fluorine substituent group into the spiro-pyran molecule structure with pH response, prepared with 19 F MRI and fluorescence imaging pH-responsive bimodal imaging small molecule probe.Compared with the prior art, the small molecule probe of the present application exhibits significantly different 19 F NMR chemical shift and fluorescence intensity, high-resolution 19 F MRI imaging and fluorescence imaging, greatly improve the sensitivity and accuracy of imaging, has important application prospect in the field of biosensing, cell imaging, medical diagnosis etc.

The application discloses a preparation method of a medical intermediate (R)-7-ethyl camptothecin, and relates to the field of chemical medicine synthesis. The application comprises the following contents: (R)-4-ethyl-4-hydroxy-7,8-dihydro-1H-pyrano[3,4-f]indolizine-3,6,10(4H)-trione (formula A) and 1-(2-aminophenyl)propan-1-one (formula B) are used as main raw materials, a target compound (R)-7-ethyl camptothecin is obtained through reaction in an organic solvent under the action of a catalyst. The application provides a novel preparation method of the medical intermediate (R)-7-ethyl camptothecin, and the preparation method is simple, stable, high in yield, and suitable for industrial production.

This invention relates to a method for producing an aqueous polymer dispersion by free radical-initiated aqueous emulsion polymerization of a monomer composition comprising 50% to 99.9% by weight of at least one (meth)acrylic acid C1 to C2. 10 Alkyl esters and / or vinyl aromatic compounds (Class I), or at least one vinyl aromatic compound and conjugated aliphatic diene by weight of 50% to 99.9% (Class II), or vinyl acetate, vinyl propionate, vinyl tert-carbonate, long-chain fatty acid vinyl esters and / or ethylene by weight of 50% to 99.9% (Class III), these amounts being based on total monomers in each case, the method being carried out by polymerizing the composition in the presence of an oligosaccharide having 1.5 to 10 β-1,4-glycosidic bonds linking pyranose units; relating to the dispersion obtained accordingly; and relating to the use of the dispersion as a binder, adhesive, sizing agent for fibers, for the production of coatings or for the production of paper coating formulations.

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.

This invention discloses a method for preparing and applying a dynamic pH / light-responsive bilayer programmable hydrogel, belonging to the field of hydrogel materials technology. The purpose of this invention is to address the problems of existing hydrogel materials, such as single crosslinking structure, irreversible crosslinking, difficulty in simultaneously achieving mechanical and responsive properties, single response mode, and insufficient programmable controllability. The method involves: 1. Preparing a borate ester crosslinked PVA-B-O-PVA hydrogel; 2. Preparing a pH / light-responsive bilayer hydrogel. This hydrogel can achieve swelling regulation through reversible breaking and recombination of borate ester bonds under varying acidic and alkaline conditions. Under light irradiation, it achieves photochromism and deformation response through the SP / MC structural transformation of spiropyran molecules. Furthermore, it achieves bending, folding, and programmable motion behavior through the synergistic effect of different functional layers in the bilayer structure. It can be applied to flexible actuators, programmable soft actuators, and environmental response sensors in complex environments.

The application relates to a method for synthesizing dihydropyrrolo[2,3-c]pyrazole analogs. Specifically, under the catalysis of a transition metal and a bidentate ligand, dihydropyrrolo[2,3-c]pyrazole analogs can be obtained in high selectivity by using the bidentate ligand synergy, taking pyrazolinone as raw material and reacting with 1,3-alkyne under the action of triethylenediamine. The application uses cheap and commercially available 1,3-alkyne and easily obtained pyrazolinone, and a series of heterocyclic compounds with potential medicinal value are obtained in high selectivity under simple and mild conditions.

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.

This invention belongs to the field of compound analysis and provides a method for detecting the content and isomer ratio of hydroxypropyltetrahydropyranotriol using high-performance liquid chromatography-differential refractive index (HPLC-DRI). The method includes the following steps: qualitative and quantitative analysis of prepared standard solutions and test solutions using HPLC-DRI. The method provided by this invention uses a simple and clean mobile phase with no impact on human health, simplifies sample pretreatment, has a low detection limit for hydroxypropyltetrahydropyranotriol, exhibits good linearity within the linear range, high correlation coefficient, high resolution of diastereomers, and good repeatability. It provides an effective detection method for ensuring the quality of hydroxypropyltetrahydropyranotriol and screening for superior grades.