24 results about "Benzisoxazole" patented technology

The invention belongs to the technical field of pesticides, and particularly relates to a substituted benzisoxazole compound, a preparation method thereof, an insecticidal composition and application. The compound is shown as a general formula I, wherein Z1, Z2, Z3, Z4 and Z5 independently represent N or CR; r independently represents hydrogen, halogen, alkyl, alkenyl or the like; x represents an alkyl group, a haloalkyl group, an alkenyl group or the like; y represents alkyl. The compound has excellent prevention and treatment effects on pests such as spodoptera frugiperda, armyworm, plutella xylostella and prodenia litura.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

The present invention relates to a treatment agent for various diseases of the nervous system and mental illnesses which contains the compound represented in formula (1) or a pharmaceutically acceptable salt thereof as the active component (in the formula, R1 represents a hydrogen, etc., R2 represents a halogen, etc., and R3, R4, R5 and R6 represent a hydrogen, etc.).

The application provides a benzene [d] isoxazole compound and an application thereof. The compound has the structure shown in the following formula I. The benzene [d] isoxazole compound provided by the application can induce degradation of BET protein and / or GSPT1 protein, and has an anti-proliferation effect on cancer cells. Therefore, the compound and the composition provided by the application can be used for preparing a drug for treating or preventing tumor formation, inflammation, viral infection, cell proliferative disorder, autoimmune disease, sepsis and the like.

The invention provides a preparation method of 2-amino-5-chlorobenzophenone, and relates to the technical field of medicine synthesis. The method comprises the following steps: dissolving 5-chloro-3-phenyl-2, 1-benzisoxazole in ethyl acetate, under the action of a composite catalyst, vacuumizing, introducing hydrogen for reaction until the content of 2-amino-5-chlorobenzophenone in a reaction liquid detected by HPLC (High Performance Liquid Chromatography) is not lower than 93%, carrying out filter pressing, collecting filtrate, carrying out reduced pressure distillation on the filtrate, and recrystallizing to obtain the 2-amino-5-chlorobenzophenone. Drying is carried out, such that 2-amino-5-chlorobenzophenone is obtained; the composite catalyst is a nitrogen-doped porous graphene loaded platinum monatomic catalyst. According to the method for preparing the 2-amino-5-chlorobenzophenone, Pt (at) NHG is adopted as the catalyst, the dosage is small, and the catalyst can be recycled and reused; compared with a traditional iron powder / acid reduction process, a large amount of metal waste residues and acid-containing waste water are not generated, and environment friendliness is achieved.

The present invention relates to compounds of formula (I)or pharmaceutically acceptable salts thereof, wherein Ring A, R1-R8, and n are defined herein. The novel benzisoxazole sulfonamide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in patients. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in patients.

The invention provides a preparation method of 2-amino-5-chlorobenzhydrol, and relates to the technical field of medicine synthesis. The method comprises the following steps: dissolving 5-chloro-3-phenyl-2, 1-benzisoxazole in ethanol, reacting with sodium borohydride under the catalytic action of nitrogen-doped porous graphene-silicon dioxide until the content of 2-amino-5-chlorobenzhydrol in a reaction solution detected by HPLC (High Performance Liquid Chromatography) is not lower than 93.5%, stopping the reaction, filtering, and collecting filtrate, thereby obtaining the 2-amino-5-chlorobenzhydrol. And carrying out reduced pressure distillation on the filtrate, cooling, recrystallizing, carrying out suction filtration, and drying to obtain the 2-amino-5-chlorobenzhydrol. According to the preparation method disclosed by the invention, the 2-amino-5-chlorobenzhydrol is synthesized in one step through direct reduction by a one-pot method, synthesis and separation of an intermediate are not needed, and the reaction process is remarkably shortened.

The invention relates to a compound for use in a method of treating or preventing a KMO mediated disorder in a subject in need thereof; wherein said compound is a benzisoxazole of formula (I) or a pharmaceutically acceptable salt thereof, wherein said method comprises administering said compound to the subject as an intravenous infusion at a dose rate of between about 200 µg / h and about 2.5 mg / h for a period of at least 12 hours.

This application provides a method for preparing 1,2-benzisoxazole derivatives. This method is the first to develop a C-H activation strategy for generating 1,2-benzisoxazole using N-phenoxyamide as a substrate and acetic halide as a coupling agent under rhodium(III) catalysis. Under inert solvent conditions, and with the combined action of a transition metal catalyst and an oxidant, the acetic halide undergoes ortho-C-H bond alkynylation under the guidance of N-phenoxyamide, followed by intramolecular amine metallation of the carbon-carbon triple bond of the acetic acid. Finally, under the action of a base, deacylation and β-OH elimination occur, yielding a multifunctional 1,2-benzisoxazole derivative. Currently, the synthesis of 1,2-benzisoxazole remains challenging due to the scarcity of synthetic methods and limitations on specific substrates (multi-step synthesis, poor functional group compatibility, etc.). This reaction is expected to provide a new approach for the development and application of 1,2-benzisoxazole derivatives. It should be noted that the obtained product can also be applied to hole transport materials for perovskite solar cells. Specifically, a donor-acceptor structure is formed by combining a triphenylamine group with excellent hole transport capability and a benzoxazole group that can act as an electron acceptor. This molecule achieves a power conversion efficiency of 16.01%.

The application discloses a purification method of a risperidone intermediate, 6-fluoro-3-(4-piperidyl)-1,2-benzisoxazole hydrochloride shown in formula II, characterized in that the purification method comprises the following steps: adding 6-fluoro-3-(4-piperidyl)-1,2-benzisoxazole hydrochloride into ethanol, adding a certain amount of water, heating to reflux until the solution is clear, cooling to a certain temperature to perform crystal growing, then cooling to-5-10 DEG C, filtering and drying to obtain the product. The purification method of 6-fluoro-3-(4-piperidyl)-1,2-benzisoxazole hydrochloride provided by the application can effectively separate the formula V dimer, the purification yield is more than 85%, the chemical purity of the finished product can reach more than 99.9%, and the method will not produce amplification effect in mass production, and the process is stable.

The present invention relates to a medicament for treating various nervous system diseases or psychiatric diseases, comprising a compound of formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient, wherein R1 is hydrogen, etc., R2 is halogen, etc., R3, R4, R5, and R6 are hydrogen, etc.

The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Ring A, Y, R1-R8, m, n and p are defined herein. The novel cycloalkyl and heterocycloalkyl benzisoxazole sulfonamide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in patients. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in patients.

The invention discloses a preparation method of a 2-substituted quinazoline derivative, which comprises the following step: heating and stirring three components, namely an ammonium salt, a benzyl alcohol compound and a 2, 1-benzisoxazole compound in an organic solvent to obtain the 2-substituted quinazoline derivative. According to the method, ammonium iodide which is low in price and easy to obtain is used as a nitrogen source and an oxidizing agent, benzyl alcohol is used as a carbon source, and efficient construction from a 2, 1-benzisoxazole skeleton to a 2-substituted quinazoline skeleton is achieved through a carbon-nitrogen diatom inserted ring expansion reaction under the mild conditions of no metal and no additive. The synthetic method developed by the invention has a good application prospect in the industrial fields of biological medicines, pesticides and the like, and is particularly suitable for efficiently preparing the quinazoline compound with biological activity under simple and convenient conditions. The synthetic method developed by the invention has a good application prospect in the industrial fields of biological medicines, pesticides and the like, and a theoretical basis is provided for commercialized application of the derivatives in the field of medicines.

The present disclosure is concerned with chemical release agents containing a release trigger (e.g., a benzisoxazole), a polymeric element, and an active agent such as, for example, a radioligand, a residue of a peptide, a residue of a protein, a residue of an oligonucleotide, or a residue of a small molecule therapeutic agent, containing the compounds, and methods for using the same. Also disclosed are intermediate compounds useful in the preparation of chemical release agents. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The invention relates to the technical field of preparation of quinazolinone derivatives. The invention provides a method for preparing a quinazolinone derivative, which comprises the following steps of: adding a compound with a general formula 1, benzisoxazole, 2, 3-dichloro-5, 6-dicyanobenzoquinone and cuprous iodide into 1, 2-dichloroethane to react, and the chemical equation of the reaction is shown in the specification; wherein R is hydrogen, methyl, ethyl or methoxyl. The method provided by the invention takes copper as a catalyst, and has the characteristics of high stereoselectivity and single product geometric configuration. The copper catalyst is cheap and low in toxicity, and meets green chemical requirements; reaction conditions are mild, and industrial amplification is easy; meanwhile, by-products are few, and atom economy is good.

This disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azaphen-4-yl)acetamide or a pharmaceutically acceptable salt thereof for the treatment of thrombocytosis.

The application belongs to the technical field of organic synthesis, and particularly relates to an amino nitrile compound with a remote chiral center and a preparation method and application thereof. The nickel-hydrogen catalytic asymmetric hydrogenation reaction provided by the application is realized through non-covalent pi-pi interaction between a cyano group in an olefin substrate and a chiral bisoxazoline ligand. The method not only realizes efficient and high-selectivity conversion of various olefin substrates and amine electrophilic reagents, but also is compatible with secondary alkyl amine electrophilic reagents, amide electrophilic reagents and benzisoxazole electrophilic reagents, thereby providing a reliable way for synthesizing chiral amino nitrile compounds (formula I) with a remote (beta-, gamma- and delta-) stereogenic center and various structures.

The disclosure provides compounds, e.g., compounds of Formula I, and their use in treating medical diseases or disorders, such as neurological disorders. Pharmaceutical compositions and methods of making various azaindole and benzisoxazole compounds are provided. The compounds are contemplated to be modulators of the 5-hydroxytryptamine 2A (5-HT2A) receptor.

The invention discloses an N-substituted benzisoxazole-3-ketone compound as well as a preparation method and application thereof, and the preparation method of the N-substituted benzisoxazole-3-ketone compound comprises the following steps: mixing thioimine, a catalyst and an organic solvent to obtain a mixture; replacing the mixture with an inert atmosphere, and carrying out light irradiation stirring reaction for a preset time at a preset temperature to obtain a reactant; and carrying out separation and purification treatment on a reactant, so as to obtain the N-substituted benzisoxazole-3-ketone compound. According to the preparation method, thioimine is used as a nitrogen alkene precursor for intramolecular C-O insertion, C-N bonds and N-O bonds are constructed at the same time, the N-substituted benzisoxazole-3-ketone compound is synthesized, and the preparation method has the advantages of being high in target product yield, good in substrate universality, high in atom economy, simple in reaction condition, convenient in aftertreatment, green and safe.

The invention provides a synthesis method of a 2-((diphenylmethylene) amino)-N, 2-diphenylacetamide compound, which comprises the following steps: under the protection of inert gas and in an aprotic solvent, reacting a 3-aryl substituted 1, 1-diphenyl-2-aza allyl compound with an aryl substituted 2, 2-diphenylacetamide compound to obtain the 2-((diphenylmethylene) amino)-N, 2-diphenylacetamide compound. The preparation method comprises the following steps: mixing a 1, 1-benzisoxazole compound and alkali according to a molar ratio of 1: 2: 3 for reaction, then adding a saturated ammonium chloride aqueous solution for quenching, filtering, washing, drying by distillation under reduced pressure, and carrying out column chromatography separation to obtain the 2-((diphenylmethylene) amino)-N, 2-diphenylacetamide.

The disclosure provides compounds, e.g., compounds of Formula I, and their use in treating medical diseases or disorders, such as neurological disorders. Pharmaceutical compositions and methods of making various azaindole and benzisoxazole compounds are provided. The compounds are contemplated to be modulators of the 5-hydroxytryptamine 2A (5-HT2A) receptor.

The present invention relates to a high-selectivity FGFR2 inhibitor as well as a preparation method therefor and the use thereof. The compound of the present invention is useful in the treatment of tumors (particularly solid tumors, such as gastric cancer) and other disorders.

The present invention relates to the technical field of pesticides, and in particular relates to a substituted benzisoxazole compound and a preparation method therefor, an insecticidal composition, and a use. The compound is represented by general formula (I), where Z1, Z2, Z3, Z4, and Z5 independently represent N or CR, R independently represents hydrogen, halogen, alkyl, alkenyl, etc., X represents alkyl, haloalkyl, alkenyl, etc., and Y represents alkyl. The compound has excellent control efficacy against pests such as Spodoptera frugiperda, Mythimna separata, Plutella xylostella, and Spodoptera litura.