33 results about "1-benzofuran" patented technology

The present invention is directed to crystalline forms of the 5-HT_2C agonist {[(2R)-7-(2,6-dichlorophenyl)-5-fluoro-2,3-dihydro-1-benzofuran-2-yl]methyl}amine hydrochloride, as well as compositions, processes of preparation, and uses thereof.

There is provided a pharmaceutical composition comprising (1) (R)-5,6-dimethoxy-2-[2,2,4,6,7-pentamethyl-3-(4-methylphenyl)-2,3-dihydro-1-benzofuran-5-yl]isoindoline, (2) a lipophilic component, and (3) a surfactant, which can stably and sufficiently provide improvement in the absorbability of the drug without being affected by the amount and quality of a meal.

The present invention provides methods of decreasing the frequency of emergence, decreasing the level of resistance, and delaying the emergence of a treatment-resistant Hepatitis C viral infection, by administering to a subject, either in combination or in series, an inhibitor of the Hepatitis C RNA-dependent RNA polymerase NS5B, e.g., a benzofuran, such as 5-cyclopropyl-2-(4-fluorophenyl)-6-[(2-hydroxyethyl)(methylsulfonyl)amino]-N-methyl-1-benzofuran-3-carboxamide (HCV-796), and at least one additional anti-Hepatitis C agent, e.g., a ribavirin product or an immunomodulator, such as an interferon product. Additionally, the invention relates to methods of monitoring the course of treatment of a Hepatitis C viral infection, methods of monitoring and prognosing a Hepatitis C viral infection, and methods of identifying an individual with a decreased likelihood of responding to an anti-Hepatitis C viral therapy. These methods use the sequence and/or structure of the Hepatitis C RNA-dependent RNA polymerase NS5B to identify the emergence of a treatment-resistant Hepatitis C viral infection, particularly a benzofuran (e.g., HCV-796) treatment-resistant Hepatitis C viral infection.

The invention provides a method for preparing darifenacin intermediate 5-(2-bromoethyl)-2,3-dihydro-1-benzofuran. The method comprises the following steps of: directly reducing 2,3-dihydro benzofuran-5-acetic acid serving as a raw material into 2,3-dihydro benzofuran-5-ethanol in the presence of an ether solvent; and performing bromination on the 2,3-dihydro benzofuran-5-ethanol to obtain 5-(2-bromoethyl)-2,3-dihydro-1-benzofuran. The method has the advantages of simple and convenient operation, readily available raw material, high yield, low production cost and suitability for industrial production.

Substantially pure polymorphic forms of 5-cyclopropyl-2-(4-fluorophenyl)-6-[(2-hydroxyethyl)(methylsulfonyl)amino]-N-methyl-1-benzofuran-3-carboxamide are produced by recrystallization in an organic solvent.

The invention relates to the field of medical intermediate synthesis, in particular to a process route for synthesizing an important medical intermediate benzofuran. The process route for synthesizing benzofuran mainly comprises the following step of: reacting substituted o-hydroxybenzaldehyde, o-hydroxyphenyl alkyl ketone, or o-hydroxybenzonitrile with 2-halogenated aliphatic acid or the corresponding ester under the action of alkali to obtain the corresponding substituted benzofuran. The invention provides a method for preparing benzofuran, which is simple and can realize industrialized production; and the process route provided by the invention has the characteristics of economy, rapidness, environmental friendliness, high yield and the like.

Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain.

A novel compound or a salt thereof, which is characterized in that it has an amino group and R¹ (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3-dihydrdo-1-benzofuran, 2,3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R² and R³ (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.

The invention relates to a treatment agent for removing sulfide from oil-fired boiler tail gas. The treatment agent is prepared by compounding of the following components: 5, 7-trihydroxy-2- (3, 4, 5-trihydroxyphenyl)-4H-1-benzofuran-4-one, harringtonine, 7-hydroxy-6-methoxy-2H-1-benzopyran-2-one, pentahydroxyflavone-3-rhamnoside, 3-methyl pyridazine, 4-acetoxy-3-methoxy-(2-allyl)benzene, 4, 4'-sulfonyldianiline, and 3-methyl-3-phenyloxiranecarboxylic acid ethyl ester, 5-allyl-2, 3-(methylenedioxy)anisole, etc. The treatment agent has strong complexing ability with a target material, the complex precipitate forming rate is fast, the removal rate can reach 99%, the cost is low, the dosage is small, scaling does not form, and the treatment agent does not cause environmental harm.

The invention relates to a sealing material, in particular to long-lasting, high-humidity and mold-proof silicone sealant. The long-lasting, high-humidity, mold-proof silicone sealant is prepared from the following raw materials: alpha-hydro-omega-hydroxy-polydimethylsiloxane, 6-(beta-D-glucopyranosyl-oxy)-7-hydroxy-2H-1-benzofuran-2-one, (1,3,4,5,6,7-hexahydro-1,3-dioxo-2H-isoindol-2-yl)methyl (1R-trans)-2,2-dimethyl-3-(2-methylprop-1-enyl)cyclopropanecarboxylate, trimethyl[(1-methyl-ethenyl)oxy]-silane, 2-ethylhexyl 4-methoxycinnamate, and the like. The long-lasting, high-humidity and mold-proof silicone sealant is good in mold-proof performance, relatively long in storage time, simple in preparation method, relatively short in surface drying time, shortened in work time, improved in work efficiency, and free of yellowing, and is suitable for promotion and application in the field of mold-proof silicone sealant.

The invention discloses an EVA hot-melt adhesive for refrigerator sealing. The EVA hot-melt adhesive for refrigerator sealing is prepared from, by weight, 100 parts of EVA resin, 1-4 parts of a vinyl fused ring mixture, 30-50 parts of a tackifier, 10-15 parts of a viscosity modifier, 0.2-1 part of an antioxidant, 0.1-0.5 part of an initiator and 20-30 parts of filler, wherein the vinyl fused ring mixture is prepared from an acylated vinyl fused ring compound and a non-acylated vinyl fused ring compound, and the vinyl fused ring compounds are selected from 2-vinyl-1-benzofuran and 2-vinyl-1-benzothiophene.

Pharmaceutical formulations containing 5-cyclopropyl-2-(4-fluorophenyl)-6-[(2-hydroxyethyl)(methylsulfonyl)amino]-N-methyl-1-benzofuran-3-carboxamide and pharmaceutically acceptable additives including at least one surfactant are made.

An EVA hot melt adhesive for a storage battery is at least prepared from, by weight, 100 parts of EVA resin, 5-10 parts of a vinyl condensed ring mixture, 2-5 parts of alpha-olefin containing an aromatic ring substituent group, 20-40 parts of tackifier, 12-18 parts of a viscosity modifier, 0.01-0.5 part of an antioxidant, 0.05-0.2 part of an initiating agent and 30-40 parts of packing, wherein the vinyl condensed ring mixture comprises an acylated vinyl condensed ring compound and an non-acylated vinyl condensed ring compound, the vinyl condensed ring compound is selected from 2-vinyl-1-benzofuran or 2-vinyl-1-benzothiophene, and the aromatic ring substituent group contains elemental sulphur.

The invention relates to a synthesis method of 2,3-dihydro-1-benzofuran-4-carbaldehyde. The formula of 2,3-dihydro-1-benzofuran-4-carbaldehyde can be shown in the formula (I). The synthesis method comprises the steps of making a compound shown in the formula (II) be subjected to intramolecular cyclization reaction so as to produce a compound shown in the formula (III) under the existence of alkali metal compounds and Cu(1); making the compound shown in the formula (III) be subjected to reaction together with magnesium and a compound shown in the formula R3CONR1R2(IV) so as to obtain the compound shown in the formula (I). According to the synthesis method of 2,3-dihydro-1-benzofuran-4-carbaldehyde, reaction conditions are mild, procedures are simple, byproducts are few, and thus the synthesis method of 2,3-dihydro-1-benzofuran-4-carbaldehyde is suitable for being applied to large scale industrial production.

This invention relates to a process for the preparation of N-[2-n-butyl-3-{4-[(3- dibutylamino)-propoxy]-benzoyl} - 1-benzofuran-5-yl]-methane-sulfonamide of formula (I) and its pharmaceutically acceptable salts, according to one of the methylsulfonyl groups of the 2-n-butyl-3-[(di-n-butylamino-3-propoxy)-benzoyl]-5- bis-(methylsulfonamido)-benzofuran of formula (II) is selectively cleaved and if desired, the resulting compound of formula (I) is transformed into its salt.

The invention relates to a method for removing sulfide in oil burning boiler tail gas. The method includes the step that the oil burning boiler tail gas is introduced into enough desulfurizer through a pipeline, and sulfur dioxide, sulfur trioxide and hydrogen sulfide in the tail gas react with the desulfurizer to form complex precipitates to be filtered out. The desulfurizer is prepared from, by weight, 5,7-trihydroxy-2-(3,4,5-trihydroxy phenyl)-4H-1-benzofuran-4-ketone, harringtonin, 7-hydroxy-6-methoxy-2H-1-benzofuran-2-ketone, pentahydroxy flavone-3-rhamnoside, 3-methyl pyridazine, 4-acetoxyl-3-methoxy-(2-propenyl) benzene, 4,4'-sulfonyldiphenylamine and the like. According to the treatment method, the capacity of complexing the target substances is high, the speed of forming the complex precipitates is high, the removal rate can reach 99%, cost is low, usage amount is small, scale formation is avoided, and the environment is not damaged.