23 results about "Phthalazine" patented technology

The invention provides a 4-phenylbenzo [f] phthalazine-1 (2H)-ketone derivative, a preparation method thereof and an electroluminescent device. The structural formula of the 4-phenylbenzo [f] phthalazine-1 (2H)-ketone derivative is shown in the specification. According to the electroluminescent device, the 4-phenylbenzo [f] phthalazine-1 (2H)-ketone derivative is used as a guest luminescent material, the luminescent efficiency of the electroluminescent device is effectively improved, the service life is prolonged, light emitted by the electroluminescent device has good color purity, the emission wavelength of the electroluminescent device is in the range from blue light to visible light, and the electroluminescent device has good application prospects. And the application requirements of different scenes are met.

Provided is a method for producing an olaparib precursor, said method comprising the step of performing the following steps (a) to (c) continuously without isolating a reaction intermediate. (a) Reacting dimethyl(3-oxo-1,3-dihydro-2-benzofuran-1-yl)phosphonate and 2-fluoro-5-formylbenzoic acid in DMF, acetonitrile, or THF and in the presence of diazabicycloundecene. (b) Reacting the reaction mixture obtained in the reaction of (a) with hydrazine. (c) Adjusting the reaction liquid obtained in the reaction of (b) to a pH of not more than 4, to obtain 2-fluoro-5-(4-oxo-3,4-dihydro-phthalazine-1-ylmethyl)-benzoic acid, which is an olaparib precursor.

The present invention provides a substituted heteroarylphthalazine derivative represented by formula (I-0) having excellent NLRP3 inhibitory activity, its use as an NLRP3 inhibitor, and a preparation method thereof. JPEG2024535475000146.jpg4488

The invention discloses a preparation method of a 25-hydroxyvitamin D3 intermediate, which comprises the following steps: taking 3 beta-tert-butyldimethylsiloxy ergosta-5, 7, 22-triene as a raw material, carrying out DA reaction on the 3 beta-tert-butyldimethylsiloxy ergosta-5, 7, 22-triene and phthalylhydrazine under the action of lead dioxide and acetic acid to generate 3 beta-tert-butyldimethylsiloxy-5a, 8a-(1, 4-dioxo-1, 2, 3, 4-tetrahydro-phthalazine-2, 3-diyl) ergosta-6, 7, 22-triene, and reacting the 3 beta-tert-butyldimethylsiloxy-5a, 8a-(1, 4-dioxo-1, 2, 3, 4-tetrahydro-phthalazine-2, 3-diyl) ergosta-6 and carrying out simple crystallization to obtain a high-content crystal product. Reaction raw materials are simple and easy to obtain, silicon ether bond breakage is avoided, meanwhile, raw materials with high dangerousness are not used, no other toxic and harmful by-product residues exist in a product, safety is high in the production process, and the product meets the use standard. Therefore, the whole preparation method needs less manpower, material and financial resources, is high in safety and is suitable for large-scale industrial production.

The invention relates to the technical field of coatings, and discloses a high-temperature-resistant waterproof coating and a preparation method thereof. The preparation method comprises the following steps: introducing a hydroxyl-terminated nitrile rubber / montmorillonite composite material, 4-(4-hydroxyphenyl) phthalazine-1-ol, N-(4-hydroxyphenyl) maleimide and a perfluorinated chain extender into waterborne polyurethane acrylate; and then free radical polymerization is carried out on the modified starch, carbon-carbon double bond-containing monomer oxazolidinone acrylate, gamma-methacryloxypropyltrimethoxysilane, hexafluorobutyl methacrylate and styrene under the condition of an initiator, and the obtained coating is excellent in high temperature resistance and waterproof performance and good in mechanical property.

The application discloses application of 1-chloro-4-hydrazinyl phthalazine as a reactive matrix in monosaccharide MALDI MSI in-situ analysis. The monosaccharide includes glucose, fructose, fucose and arabinose. The application develops 1-chloro-4-hydrazinyl phthalazine (CHP) as a reactive matrix, which is used for derivatization of monosaccharide in biological tissues and in-situ differentiation of monosaccharide isomers. Taking carrot as a model, monosaccharide on the carrot tissue is derivatized, and a MALDI-MSI experiment is carried out. It is worth noting that characteristic fragments generated by secondary mass spectrometry of the derivatization product can be used for further distinguishing aldoses and ketoses, thereby differentiating monosaccharide isomers and revealing different spatial distributions of monosaccharide isomers in organisms.

The application belongs to the fields of medicine and chemistry, and particularly relates to a preparation method of a dihydralazine impurity, S1: o-phenylenedinitrile is added into a reaction bottle, a solvent and a strong base are further added, and the reaction is stirred under heating and reflux; after the reaction is completed, the pH of the reaction system is adjusted by using an acid solvent, and then compound 2 is obtained through crystallization, filtration and drying, S2: compound 2 obtained in S1 and a solvent are added into a reaction bottle, hydrazine hydrate is added, after the reaction is completed, a part of the solvent is removed through concentration under reduced pressure, and compound 3 is obtained through crystallization, filtration and drying, S3: compound 3 obtained in S2 is added into a reaction bottle, a chloro reagent is added, and the reaction is completed under heating and reflux; after the solvent is removed through concentration, hydrazine hydrate is added. The method provides a preparation process of the dihydralazine impurity 1-amino-4-hydrazyl-phthalazine, and the process is simple, the reaction condition is mild, and the preparation can be completed by a laboratory.

The present specification provides a crystalline form of 4-[3-(3-[(cyclopropylamino)methyl]azetidine-1-carbonyl)-4-fluorobenzyl]phthalazine-1(2H)-one hydrochloride, a method for preparing the crystalline form, and a pharmaceutical composition comprising the crystalline form.

The invention discloses a method for preparing olaparib by adopting sulfur hexafluoride, which comprises the following steps: by taking 1-cyclopropyl formyl piperazine and 2-fluoro-5-((4-oxo-3, 4-dihydrophthalazine-1-yl) methyl) benzoic acid as raw materials, carrying out illumination reaction in an organic solvent under the conditions of a photocatalyst, alkali, sulfur hexafluoride and illumination to obtain the olaparib. The reaction conditions are mild, the used reaction raw materials are cheap and easy to obtain, and the method has the characteristics of cost saving, environment friendliness and industrial popularization. According to the method, the greenhouse gas SF6 is effectively activated and utilized, the decomposition product SF6 is fully utilized to realize the amidation reaction of carboxylic acid to prepare olaparib, the SF6 is turned into wealth, the required raw materials are simple and easy to obtain, the reaction conditions are simple and convenient, the method is green and energy-saving, and the method has relatively high application value.

The application provides an N,N'-disubstituted dihydrophenazine heterocyclic compound and a preparation method and application, the heterocyclic compound has a structure shown in formula I; wherein A is a substituted heterocycle selected from pyridine, pyrazine, pyridazine, quinoline, quinoxaline, phthalazine, benzoxadiazole, benzothiadiazole or benzoselenadiazole; the preparation method is to use N,N'-diaryl diamine and corresponding difluoro heterocyclic derivative as raw materials, to synthesize by nucleophilic aromatic substitution reaction, the method has the advantages of mild reaction condition, simple operation, no metal catalyst is used, overcomes the problems of many isomers, low yield and metal residue in the existing metal catalytic coupling method, provides a general strategy for efficient and green synthesis of target compounds, and the structure of the heterocycle A can be changed to accurately control the photophysical properties of the compound. The compound can be used as a fluorescent probe and can be used for preparing an organic electroluminescent device, and has a wide application prospect in the field of photoelectric functional materials.

The application discloses a method for preparing olaparib from sulfur hexafluoride, which takes 1-cyclopropylformylpiperazine and 2-fluoro-5-((4-oxo-3,4-dihydrophthalazine-1-yl)methyl)benzoic acid as raw materials, and performs a photo-illumination reaction in an organic solvent under the conditions of a photocatalyst, an alkali, sulfur hexafluoride and light illumination to obtain the olaparib. The method has the characteristics of mild reaction conditions, cheap and easily available reaction raw materials, cost saving, environmental friendliness and industrial promotion. The method effectively activates and utilizes the greenhouse gas SF6, fully utilizes the decomposition products of SF6 to realize the amidation reaction of the carboxylic acid to prepare the olaparib, changes the SF6 from waste to treasure, the required raw materials are simple and easily available, the reaction conditions are simple, green and energy-saving, and the method has high application value.

The invention discloses a synthesis method of dihydrazinophthalazine and an intermediate thereof, and belongs to the technical field of chemical medicine bulk drugs. 1, 4-dichlorophthalazine can be directly obtained in a microwave treatment mode by taking phthalylhydrazine as a raw material and utilizing a thionyl chloride-phosphorus oxychloride composite chlorination reagent under the condition of not using an organic solvent; the reaction efficiency and the yield are greatly improved, the production time is shortened, the production efficiency is improved, and the industrial production of dihydrazinophthalazine is further facilitated.

A method for treating breast cancer, ovarian cancer, or prostate cancer in a subject, comprising administering to a subject in need thereof a therapeutically effective amount of (E)-3-(2-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1- yl)pyrimidin-5-yl)-N-hydroxyacrylamide, or a pharmaceutically acceptable salt thereof.

The present invention discloses a stable crystal form of a novel PARP inhibitor and a preparation method thereof. The novel PARP inhibitor is 4-(3-(1,1-dioxothiomorpholine-4-carbonyl)-4-fluorobenzyl)phthalazine-1(2H)-one, and the stable crystal form is crystal form B. The powder X-ray diffraction pattern of the crystal form B shows main peaks at 2θ of 16.439°, 18.512°, 20.008°, 21.594°, 24.070°, 26.094°, and 27.940°. The crystal form B has high purity, good stability, good powder fluidity, and the like.

A method for treating Ewing sarcoma in a subject comprising administering to a subject in need thereof a therapeutically effective amount of (E)-3-(2-(4-(2-fluoro-5-((4-oxo-3, 4-dihydrophthalazin-1-yl) methyl) benzoyl) piperazin-1-yl) pyrimidin-5-yl)-N-hydroxyacrylamide, or a pharmaceutically acceptable salt thereof.

To provide KRASG12C inhibitors for treating lung, pancreatic or colorectal cancer.SOLUTION: Benzisothiazole, isothiazolo [3, 4-b] pyridine, quinazoline, phthalazine, pyrido [2, 3-d] pyridazines and pyrido [2, 3-d] pyrimidine derivatives and associated compounds are provided as KRASG12C inhibitors.SELECTED DRAWING: None

The present invention relates to the field of healthcare. What is described is a method for treating immunodeficiency which includes intravenously administering 0.5-40.0 mg / kg body weight per day of sodium aminodihydrophthalazinedione. The invention enhances the effectiveness of parenteral therapy for immunodeficiency.

The application discloses an axially chiral phthalazine compound and a synthesis method and application thereof, and belongs to the technical field of pharmaceutical intermediates. The compound structure is shown in the following formula: or. The application takes a diazo compound as raw material, takes a chiral phosphorus catalyst as a catalyst, takes a Bronsted acid and an organic base as co-catalysts, takes silane as a reducing agent, takes an organic solvent as a solvent, takes 4A molecular sieve as an additive, and obtains the product through one-step reaction, column chromatography purification under a mild reaction temperature, has the advantages of high enantioselectivity and yield, and has the advantages of mild reaction condition, wide applicability of substrate range, simple operation and safety. The obtained axially chiral phthalazine compound has an antitumor effect, and is an important chemical, chemical and pharmaceutical intermediate.

The present disclosure relates to compounds of formula (III), as well as their pharma- ceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of IL-1 family cytokines by inhibiting inflammasomes, and can be used to treat diseases involving inflammasome activity, such as inflammatory, autoinflammatory, and autoimmune diseases, and cancer. TIFF2025504374000481.tif21128

The application relates to the technical field of paint, and discloses a high-temperature-resistant waterproof paint and a preparation method thereof. The preparation method comprises the following steps: introducing hydroxyl-terminated nitrile rubber / montmorillonite composite material into water-based polyurethane acrylate by adding 4-(4-hydroxyphenyl) phthalazine-1-ol, N-(4-hydroxyphenyl) maleimide and perfluoro chain extender; and then, under the condition of an initiator, free radical polymerization is carried out on the obtained water-based polyurethane acrylate by adding monomer oxazolidinone acrylate containing a carbon-carbon double bond, gamma-methacryloyloxypropyltrimethoxysilane, methyl methacrylate hexafluorobutyl ester and styrene; the obtained paint has excellent high-temperature resistance and waterproof performance and good mechanical properties.