14 results about "Isobenzofuran" patented technology

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 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 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 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 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.

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.