27 results about "Isobenzofuran" patented technology

The present invention relates to use of a multifunctional isoquinoline ligand, namely 1-(7-amino-4,5,6-triethoxy-1-oxo-1,3-dihydro-3-isobenzofuran)-8-methoxy-2-methyl-6,7-methylenedioxy-2,3,4-tetrahydroisoquinoline or tritoquinoline, for treating dry eye, meibomian gland dysfunction and lacrimal gland dysfunction.

This invention provides a method for preparing high-purity olaparib, belonging to the field of pharmaceutical synthesis technology. The method uses dimethyl (3-oxo-1,3-dihydroisobenzofuran-1-yl)phosphate as the starting material, reacting it with compound 2 via a Wittig reaction to generate compound 3. Compound 3 reacts with hydrazine hydrate to generate compound 4. Compound 4 is hydrolyzed and acidified to give compound 5. Compound 5 reacts with thionyl chloride to give compound 6. Compound 6 is then condensed with compounds 7 and 9 to obtain olaparib. This invention uses readily available raw materials, is simple to operate and process, has mild reaction conditions, achieves a total yield of up to 90%, a purity >99%, is environmentally friendly, and is suitable for industrial production.

The invention relates to a novel preparation method of escitalopram pamoate ((S)-(+)-1-(3-(dimethylamino) propyl)-1-(4-fluorophenyl)-1, 3-dihydro-5-cyano isobenzofuran pamoate) crystal form A. The method is environment-friendly and pollution-free, and the escitalopram pamoate crystal form A prepared by adopting the method is high in purity, high in purity, high in purity, high in purity, high in purity, high in purity and high in purity. The repeatability is good.

The invention belongs to the field of microbial natural products, and particularly relates to a method for preparing an ultraviolet absorbent by utilizing Kocuria rhizophila and application of the ultraviolet absorbent. According to the invention, the ultraviolet absorbent separated and prepared from the Kocuria rootrophila is 3-butyl-1-isobenzofuranone, and the ultraviolet absorbent is 3-butyl-1-isobenzofuranone. The ultraviolet absorbent comes from coral mucus microorganisms, and is more environmentally friendly than a traditionally used chemically synthesized ultraviolet absorbent. Compared with the traditional ultraviolet absorbent benzophenone, the ultraviolet absorbent has higher ultraviolet absorption capacity and can replace the traditional chemically synthesized ultraviolet absorbent.

The invention discloses an isobenzofuran-1 (3H)-ketone derivative and application thereof, and relates to the isobenzofuran-1 (3H)-ketone derivative as shown in a formula (I), and an isotope form, a stereoisomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a hydrate, a prodrug and a polymorphic substance of the isobenzofuran-1 (3H)-ketone derivative, the invention also discloses a preparation method of the compound and application of the compound in cardiovascular ischemic diseases. # imgabs0 #

The application provides a method for preparing roxadustat intermediate III, i.e. 3-methyl-5-phenoxyisobenzofuran-1(3H)-one, which comprises the following steps: generating 5-bromo-3-methylisobenzofuran-1(3H)-one through self-cyclization by taking 4-bromo-2-ethylbenzoic acid as a raw material; and generating roxadustat intermediate III through carbon-oxygen coupling reaction of 5-bromo-3-methylisobenzofuran-1(3H)-one and phenol. The method can significantly shorten the reaction time, improve the reaction yield, and simplify the reaction conditions, and is suitable for industrial production.

The application relates to a novel preparation method of eslicarbazepine acetate crystal form A ((S)-(+)-1-〔3-(dimethylamino)propyl〕-1-(4-fluorophenyl)-1,3-dihydro-5-cyanoisobenzofuran acetate), which is environment-friendly and pollution-free, and eslicarbazepine acetate crystal form A prepared by the method has high purity and good repeatability.

The present invention discloses an isochromanone derivative and a synthesis method thereof, belonging to the technical field of organic synthesis. The present invention is a method for synthesizing an isochromanone derivative by reacting an α-ketoester with phthalic anhydride or 3-alkylene isobenzofuran-1(3 H )-ketone compounds react under the promotion of a phosphorus reagent to obtain isochroman-1-one or isochroman-1,4-dione derivatives; the raw materials used in the present invention are simple and easy to obtain, have good stability, and are simple to operate; the reaction conditions of the present invention are mild, easy to scale up, have good substrate universality and functional group compatibility, and can be used for the later modification of natural product molecules; the present invention provides candidate compounds for the design, synthesis, and development of new drug molecules containing isochromanone structures.

The application discloses a continuous preparation method of 1,3-dihydroisobenzofuran, which is carried out according to the following steps: (1) loading a catalyst into a reactor, introducing a carrier gas into the reactor, and activating the catalyst by heating, and adjusting the reaction temperature to a target reaction temperature after the activation is completed; (2) adding a reaction raw material, hexahydroisobenzofuran, into the reactor to carry out a reaction, and after the raw material contacts with a catalyst bed, the raw material is separated from the reactor under the driving of the carrier gas, enters a condenser and a gas-liquid separator, and then enters a product storage tank, and tail gas is exhausted; and (3) the product in the storage tank is subjected to vacuum rectification to obtain a product with a purity of more than 97%. The reaction has high selectivity, fundamentally solves the problems of high operation difficulty and cost in the traditional method, greatly reduces the difficulty of subsequent separation, further reduces production energy consumption and production cost, and is easy to realize industrialized production.

The invention discloses a synthesis method of a thermosensitive dye pink pigment, and particularly relates to a synthesis method of 9-(ethyl (isoamyl) amino)-3 'H-spiro [benzo [A] xanthene-12, 1'-isobenzofuran]-3 '-ketone. Comprising the following steps: reacting N-(3-hydroxyphenyl) acetamide with borane tetrahydrofuran at 50 DEG C to prepare N-ethyl-3-methoxyaniline, and reacting the N-ethyl-3-methoxyaniline with isovaleraldehyde and acetic acid sodium borohydride to prepare N-ethyl-N-isopentyl-3-methoxyaniline; then refluxing with an HBr / acetic acid system at 100 DEG C to prepare 3-(ethyl (isoamyl) amino) phenol; then reacting with phthalic anhydride at the temperature of 100 DEG C to prepare 2-(4-(ethyl (isoamyl) amino)-2-hydroxybenzoyl) benzoic acid; and reacting the obtained product in methanesulfonic acid or concentrated sulfuric acid at room temperature, and performing post-treatment to obtain a target product. The method is low in reaction temperature, free of byproducts, low in raw material cost and easy to industrialize.

The application discloses a preparation method of a chiral phthalic ester prodrug and relates to the technical field of organic chemical synthesis. In the application, isothiourea is used as a Lewis base catalyst, and acyl chloride is used as an acylating agent, so that an acylation dynamic kinetic resolution process of racemic 3-hydroxyisobenzofuran-1(3H)-one (hereinafter referred to as phthalide) is realized, thereby forming a chiral phthalic ester with good to excellent yield and enantioselectivity and natural products and drugs containing the structure.

The present disclosure relates to an isobenzofuran-1(3H)-one derivative, which is a kinase inhibitor, and a use thereof and, more specifically, to an isobenzofuran-1(3H)-one derivative having HPK1 inhibitory activity and MLK3 inhibitory activity and a pharmaceutical composition containing same for preventing or treating cancer, virus infectious diseases, Parkinson's disease, non-alcoholic steatohepatitis, or tuberculosis. In addition, the compound can be advantageously used as a composition for prevention or treatment of cancer as it is administered in combination with an anticancer agent or a cell therapy product.

The invention belongs to the technical field of pharmacy, and particularly relates to application of 3-butyl-6-hydrazinoisobenzofuran-1-one in preparation of a medicine for treating cerebral arterial thrombosis. The structural formula of the 3-butyl-6-hydrazino isobenzofuran-1-ketone is as shown in the specification. The 3-butyl-6-hydrazino isobenzofuran-1-ketone prepared by the preparation method disclosed by the invention has excellent anti-platelet aggregation effect, neuroprotective activity and antithrombotic activity. Derivatives, isomers or optical isomers, racemate, pharmaceutical salts, hydrates, solvates and pharmaceutical carriers or excipients of the compound can be applied to preparation of drugs for preventing or treating cardiovascular and cerebrovascular diseases and complications thereof caused by thrombus. .

The application relates to the field of polymer high molecular materials, and particularly discloses a preparation method of a high-flux monovalent selective double-side chain type anion exchange membrane. In the preparation method, under the condition of ensuring the proper selectivity of an ion membrane, isophthaldehyde ketone structure and rigid benzimidazole structure are introduced into a polyarylene ether sulfone main chain, long side chains, twisted folding structures and rigid structures are utilized, the intermolecular stacking is prevented, the structure relaxation and the loss of micropores are prevented, free volumes are generated in the polymer membrane, micropore channels (ion channels) are formed, the high-efficiency transmission of monovalent ions is promoted, and a kind of ion exchange membrane with stable structure, high permeation flux and selectivity is constructed.

The preparation method comprises the following steps: carrying out dearomatization-ring expansion reaction on benzene under mediation of metals such as chromium to obtain a fluorinated cycloheptatriene complex; the preparation method comprises the following steps: carrying out a ligand dissociation-cyclization reaction on a fluoro cycloheptatriene complex to obtain 4-fluoro-4, 4a, 5, 5a, 6, 6a-hexahydro-1H-4, 6-vinylidene cyclopropyl [f] isobenzofuran-1, 3 (3aH)-diketone, and carrying out a ligand dissociation-cyclization reaction on the fluoro cycloheptatriene complex to obtain 4-fluoro-4, 4a, 5, 5a, 6, 6a-hexahydro-1H-4, 6-vinylidene cyclopropyl [f] isobenzofuran-1, the preparation method comprises the following steps: further carrying out condensation reaction on 4-fluoro-4, 4a, 5, 5a, 6, 6a-hexahydro-1H-4, 6-vinylidene cyclopropyl [f] isobenzofuran-1, 3 (3aH)-diketone to obtain the tecovirimat fluoro derivative. At normal temperature, the compound is a white solid, is easily soluble in methanol, ethanol and dichloromethane, and is slightly soluble in water. According to the method, starting from a cheap and easily available chemical product benzene, rapid construction of the tecovirimat fluoro derivative is realized, and the method has the advantages of mild reaction conditions, wide substrate application range, good selectivity, simple operation, easy product separation and the like. At 37 + / -5 DEG C, the solubility of the tecovirimat fluoro derivative VI in water is 8 [mu] g / mL, and compared with a tecovirimat drug, the solubility is obviously improved.

The application discloses an isobenzofuranone compound, a preparation method and application thereof. The structural formula of the isobenzofuranone compound is shown as formula (I), wherein R 1 ~R 4 are respectively selected from C1-C6 alkyl, hydrogen, halogen or methoxy; R 5 is selected from C1-C6 alkyl, aryl or halogenated aryl. The application discloses a new compound with anti-pancreatic cancer activity, which has great drug research and development potential and can be used as a lead compound for the development of anti-pancreatic cancer drugs. The isobenzofuranone compound is synthesized by using a non-metal oxidant high-valence iodine catalyst, without using expensive metal catalysts, and meets the requirements of green chemistry. The isobenzofuranone compound has high biological activity, small toxicity and high selectivity, is a new compound which is not easy to be drug-resistant, and can effectively inhibit the proliferation of pancreatic cancer cells.

The present invention discloses a preparation method of 3,3-bis(4-hydroxyphenyl)-3H-isobenzofuran-1-one (phenolphthalein), belonging to the technical field of fine chemical engineering. A mixed solution of phenol, phthalic anhydride and sulfolane is dropped into sulfolane, tris(pentafluorophenyl)borane and sulfonic acid-based ionic liquid heated to 70-110 °C; after the dropping is completed, the reaction is carried out until the conversion rate of the phthalic anhydride raw material > 98%; the temperature is lowered and added to a non-polar solvent, and the product is precipitated and filtered to obtain a phenolphthalein product. The present invention adopts a high-temperature reverse dropping method for synthesis, which is easy to operate and has a small amount of catalyst used; a unique tris(pentafluorophenyl)borane catalyst is selected, with a fast reaction rate and high efficiency; the use of sulfonic acid-based ionic liquid greatly avoids the corrosion of production pipelines, flanges and other components. The product yield finally obtained by the present invention is 92-96%, and the purity detected by liquid chromatography normalization > 99.5%.

This invention relates to the field of organic compound synthesis technology, specifically to a spirocyclooxanthone compound, its preparation method, and its applications. 2-[4-(dihexylamino)-2-hydroxybenzoyl]benzoic acid is reacted with 4-bromo-3-methylphenol under concentrated sulfuric acid catalysis. The reaction product is post-treated to obtain a crude product, which is then separated and purified to obtain 2'-bromo-6'-(dihexylamino)-3'-methyl-3H-spiro[isobenzofuran-1,9'-xanthones]-3-one. This one-pot acid-catalyzed tandem cyclization method efficiently and selectively constructs complex spirocyclooxanthone skeletons in one step, solving key problems in traditional multi-step synthesis such as cumbersome steps, low yield, harsh conditions, and difficulty in controlling regioselectivity. It achieves the preparation of spirocyclooxanthone derivatives with high yield, high purity, and a simple process.

The invention relates to a method for synthesizing 2, 3, 6-trimethylphenol from 5-methyl-1, 3-dihydroisobenzofuran-4-alcohol or ester thereof, which comprises a ring opening step and a reduction step.

The present invention relates to compounds of formula (I), wherein R1, R3, Y and A are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

The application provides a preparation method of a flexible printed circuit board containing a low-dielectric-constant high-transmittance polyimide material. The method mainly synthesizes a novel fluorine-containing dianhydride monomer 5-(4-(2-(4-(1,3-dioxyl-1,3-dihydroisobenzofuran-5-yl)-3-(trifluoromethyl)cyclohex-3-en-1-yl)-9,9'-spirobifluorene-7-yl)-2-(trifluoromethyl)phenyl)isobenzofuran-1,3-dione, and the monomer is used to synthesize a polyimide for modifying the performance of the polyimide. Due to the presence of the bulky fluorine-containing group, the dielectric constant of the material is greatly reduced. Meanwhile, the fluorine element has high electronegativity, can inhibit the formation of charge transfer complexes, and makes the obtained material have excellent optical transmittance. The material is used to prepare a flexible printed circuit board, the dielectric constant and dielectric loss of the flexible printed circuit board are low, and the flexible printed circuit board can be used in the field of high-frequency high-speed communication.

A polyetherimide includes repeating units derived from a dianhydride selected from the group consisting of 4, 4 '-((propane-2, 2-diylbis (4, 1-phenylene)) bis (oxy)) bis (isobenzofuran-1, 3-dione), a first diamine, and a second diamine; or 4, 4 '-([1, 1'-diphenyl]-4, 4 '-diylbis (oxy)) bis (isobenzofuran-1, 3-dione); the first diamine comprises 9, 9-bis (4-aminophenyl) fluorene; the polyetherimides may exhibit a desired combination of properties, and the second diamine includes a diaminodiphenyl ether, 4, 4 '-diaminodiphenyl sulfone, m-phenylenediamine, or p-phenylenediamine The polyetherimides may exhibit a desired combination of properties, methods of making the polyetherimides, and polymer compositions and articles including the polyetherimides are also disclosed.

The application discloses a fluorescent probe for specifically and rapidly marking a double-cysteine tag protein, a preparation method and application, and the probe can emit a fluorescent signal only when reacting with two cysteines simultaneously. The newly designed fluorescent probe can rapidly react with a recombinant protein containing a specific double-cysteine-containing peptide tag, and can mark POI in a site-specific manner. The fluorescent probe has a structure as shown in formula I, is named as 3,7-dihydroxy-5,5-dimethyl-4,6-bis((E)-2-nitrovinyl)-3'H,5H spiro[di-benzo[b,E]silicon-10,1'-isobenzofuran]-3'-ketone, and is abbreviated as Si-FLNO2.