50 results about "Pyrimidifen" patented technology

The invention relates to preparation and application of a trifluoroethyl thiophenylpyrimidinamine derivative. Specifically, the invention relates to a compound as shown in a formula (I), or an isotope labeled compound thereof, or an optical isomer, a geometric isomer, a tautomer or an isomer mixture thereof, or a pharmaceutically acceptable salt thereof, and application of the compound in preparation of insecticides for pest control. The compound can achieve a better pest control effect at a lower dosage, especially for pests such as tetranychidae, microcosaridae, acaridae, tarsonidae, aleuridae and root-knot nematode, and can be used for controlling pests such as tetranychidae, microcosaridae, gall mite, tarsonidae, aleuridae and the like. # imgabs0 #

The invention relates to a pyrrolo [2, 3-d] pyrimidine-4-amine derivative and application thereof in medicine, in particular to a compound shown in a formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, pharmaceutically acceptable salt or eutectic of the compound, and application of the compound in preparation of medicines for treating sGC-related diseases.

The present application provides a pyrimidineamine compound, characterized in that the pyrimidineamine compound is a compound represented by Formula I, or its stereoisomer, tautomer, isotope derivative, hydrate, solvate, prodrug, and pharmaceutically acceptable salt. The pyrimidineamine compound described in the present application has excellent NUAK1 / NUAK2 kinase inhibitory activity and can be used for preventing or treating the following diseases by inhibiting NUAK1 / NUAK2: neuropsychiatric diseases, metabolic diseases, tumors, visceral fibrosis diseases, and skin fibrosis diseases. #imgabs0#

The present application provides a pyrimidineamine compound, characterized in that the pyrimidineamine compound is a compound represented by Formula I, or its stereoisomers, tautomers, isotopic derivatives, hydrates, solvates, prodrugs, and pharmaceutically acceptable salts. The pyrimidineamine compound described herein has excellent NUAK1 / NUAK2 kinase inhibitory activity and can be used to prevent or treat the following diseases by inhibiting NUAK1 / NUAK2: neuropsychiatric diseases, metabolic diseases, tumors, visceral fibrosis, and skin fibrosis. #imgabs0#

The invention discloses a ceramic coating for a metal door and a preparation method of the ceramic coating, and relates to the technical field of coatings. The prepared ceramic coating is prepared from sodium silicate, methyltrimethoxysilane, modified polyacrylate emulsion, modified silicon dioxide, glass powder, sodium fluosilicate, a dispersing agent, a flatting agent and pure water. The modified polyacrylate emulsion is obtained by polymerizing a phosphorus-containing monomer and a vinyl monomer to generate polyacrylate, carrying out sulfonyl chlorination on the polyacrylate, reacting with 5-chloromethyl-2-pyrimidinamine, and emulsifying; the preparation method comprises the following steps: polymerizing aniline on the surface of pretreated silicon dioxide, reacting with 1-benzothiophene-5-carbonyl chloride, salinizing with diphenyl iodide trifluoromethanesulfonate and copper acetate, and reacting with bis (2-ethynylphenyl) sulfane to obtain the silicon dioxide. The prepared ceramic coating has good corrosion resistance, antibacterial property and ageing resistance, and the performance of the metal door is greatly improved.

The present invention relates to the crystalline form of bipyrimidine compounds, as well as methods for preparing the same and their use. In particular, the present invention relates to crystalline form I of 4'-cyclopropyl-5,6'-dimethoxy-N-((4-(1-methyl-4-(trifluoromethyl)-1H-imidazole-2-yl)bicyclo[2.2.2]octan-1-yl)methyl)-[2,5'-bipyrimidine]-4-amine, wherein the X-ray powder diffraction pattern of crystalline form I includes characteristic peaks at diffraction angles (2θ) of 6.378±0.2°, 9.521±0.2°, 15.721±0.2°, 16.379±0.2°, 16.981±0.2°, 17.560±0.2°, 19.080±0.2° and 22.200±0.2°. Crystal form I possesses high stability, high solubility, high plasma concentration, high bioavailability, and excellent pharmacological activity, making it suitable for pharmaceutical preparations.

The invention relates to a synthesis method of 7H-pyrrolo [2, 3-d] pyrimidine-4-amine, and belongs to the technical field of synthesis of drug intermediates. In order to solve the problems of easy generation of metal residues and low yield in the prior art, the invention provides a synthetic method of 7H-pyrrolo [2, 3-d] pyrimidine-4-amine, which comprises the following steps: in the presence of alkali, reacting aziridine with malononitrile to obtain a compound shown as a formula III; under the action of organic alkali and trichloroisocyanuric acid, the compound shown in the formula III is subjected to oxidative dehydrogenation reaction to be converted into 2-amino-3-cyano-1H-pyrrole; the 2-amino-3-cyano-1H-pyrrole and formamidine acetate are subjected to a reaction, and the 7H-pyrrolo [2, 3-d] pyrimidine-4-amine is obtained. According to the method, the problem of metal residues caused by the adoption of a noble metal catalyst can be effectively avoided, the product yield is better guaranteed, the high-purity quality effect is achieved, and the purity of an intermediate product in each step can reach 99% or above.

The present invention relates to a pyrido[2,3-d]pyrimidine-4-amine compound of general formula (I): wherein R 1 、R 2 、R 3 , A, x and y are as defined herein; methods for preparing the compounds; intermediate compounds used to prepare the compounds; pharmaceutical compositions and combinations comprising the compounds; and the use of the compounds as a single agent or in combination with other active ingredients for the preparation of pharmaceutical compositions for treating or preventing diseases, particularly hyperproliferative diseases.

The invention belongs to the technical field of organic synthesis, and particularly relates to a preparation method of a pyrrolopyrimidine-4-amine derivative, which selects methanol, ammonium formate and formic acid as a reaction system to carry out directional reaction, avoids the use of high-pressure hydrogen and a high-pressure kettle, avoids the safety risk caused by high-pressure operation, and improves the yield of the pyrrolopyrimidine-4-amine derivative. And the alcoholic solution solves the problems of low solubility and obvious amplification effect of a starting material when water is used as a solvent in the prior art, and realizes homogeneous reaction. By adopting the fixed bed reaction unit, the problem of pipeline blockage caused by sublimation of ammonium formate is solved, the potential safety hazard in large-scale production is eliminated, the fixed bed reaction unit is used for continuous catalytic reaction to replace the traditional staged reaction, the production period is remarkably shortened, the production efficiency is improved, and the method is suitable for large-scale industrial production.

A pyridin[3,2-d]pyrimidin-2-amine derivative, a preparation method therefor, and a use thereof. The pyridin[3,2-d]pyrimidin-2-amine derivative can be used as a TLR7 / 8 dual agonist, and is used for treating diseases related to TLR activity, such as diseases caused by virus (such as HBV and HIV) infection, tumors, and inflammatory diseases. In particular, the provided pyridin[3,2-d]pyrimidin-2-amine derivative has better physicochemical properties, druggability, cardiac safety and oral bioavailability, and has very good research and application value in the field of medicine.

The invention relates to a preparation method of 4-chloro-5H-pyrrolo [3, 2-D] pyrimidine-2-amine, which comprises the following steps: step 1, synthesizing a compound B from a compound A; 2, synthesizing a compound C from the compound B; 3, synthesizing a compound D from the compound C; wherein the structures of the compound A, the compound B, the compound C and the compound D are respectively as follows: # imgabs0 #. Compared with the prior art, the preparation method disclosed by the invention has the advantages that the process is simple, only three-step reaction is needed, and complicated post-treatment is not needed; the cost is controllable, raw materials are easy to obtain, reagents are cheap, and the prepared compound is a key intermediate of kinase inhibitor drugs, has important application value in research and development of anti-cancer and anti-inflammatory drugs and has high potential economic benefits; the method has no harsh reaction conditions, is simple to operate and is suitable for large-scale production.

The application discloses a ceramic paint for metal doors and a preparation method thereof, and relates to the technical field of paints. The ceramic paint prepared by the application contains sodium silicate, methyltrimethoxysilane, modified polyacrylate emulsion, modified silicon dioxide, glass powder, sodium fluorosilicate, dispersant, leveling agent and pure water. The modified polyacrylate emulsion is obtained by polymerizing phosphorus-containing monomers and vinyl monomers to generate polyacrylate, reacting the polyacrylate with 5-chloromethyl-2-pyrimidine amine after sulfonyl chlorination, and then emulsifying. The silicon dioxide is obtained by polymerizing aniline on the surface of pretreated silicon dioxide, reacting with 1-benzothiophene-5-carbonyl chloride, then salifying with diphenyl iodonium triflate and copper acetate, and then reacting with bis(2-ethynylphenyl) sulfane. The ceramic paint prepared by the application has good corrosion resistance, antibacterial property and anti-aging property, and greatly improves the performance of the metal door.

The invention discloses a method for preparing mesosulfuron, wherein pyrimidine amine and a phosgene compound are reacted to obtain isocyanate, and then the isocyanate is condensed with 5-methylsulfonylaminomethyl-2-methoxycarbonylbenzenesulfonamide to obtain mesosulfuron. The method of the invention has high yield, high purity of the obtained product, and few by-products are generated during the preparation process and are easy to recover.

The present application relates to a kind of porous coordination polymers with interpenetrating framework, preparation method and application in ethane / ethylene high temperature separation, belong to coordination chemistry material technical field.Porous coordination polymers are Cu-based coordination polymers, its chemical formula is [Cu2 (BDC) 2L2] n (solvent) x , belong to C2 / c space group, L2 is 4,6-di (1H-1,2,4-triazole-1-yl) pyrimidine-2-amine, NH2 Group is again with adjacent framework forms single hydrogen bond;It is obtained by adding regulating ligand during solvothermal reaction of ligand and metal salt.The present application proposes a new method to regulate temperature-dependent dynamic characteristics in hydrogen-bonded interpenetrating framework, with the weakening of hydrogen bond, porous coordination polymers with one-dimensional narrow-neck channel exhibit promising structural response to ethane / ethylene at high temperature, so that it shows significant ability to directly obtain polymerization grade ethylene.

The present invention belongs to the technical field of drug synthesis, and in particular to a method for preparing ibrutinib. The present invention uses 3-bromo-1H-pyrazolo[3,4-D]pyrimidine-4-amine as a raw material, and reacts with 4-phenoxyphenylboronic acid under amine catalysis to obtain 4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine; 4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine is reacted with 1-[(S)-3-hydroxy-1-piperidinyl]-2-propylene-1-one under the catalysis of phosphine oxide to obtain ibrutinib through Mitsunobu reaction. This process uses amine catalysts instead of precious metal palladium to catalyze the Suzuki coupling reaction, which solves the problems of low yield and expensive catalysts in traditional reactions of this type. It uses phosphine oxide as a catalyst to catalyze the Mitsunobu reaction, avoiding the use of equivalent triphenylphosphine in the Mitsunobu reaction, and solves the harsh conditions of the reaction itself that require the acidity of the nucleophilic reagent. The process is simple to operate, and the target product obtained is of high purity, which is suitable for industrial production.

The invention relates to a crystal form of a bipyrimidine compound as well as a preparation method and application thereof. In particular, the present invention relates to a crystalline form I of 4 '-cyclopropyl-5, 6'-dimethoxy-N-((4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl) bicyclo [2.2. 2] oct-1-yl) methyl)-[2, 5 '-bipyrimidinyl]-4-amine, a crystalline form II of 4'-cyclopropyl-5, 6 '-dimethoxy-N-((4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl) bicyclo [2.2. 2] oct-1-yl) methyl)-[2 An X-ray powder diffraction pattern of the compound comprises characteristic peaks at diffraction angles (2 theta) of 6.378 + / -0.2 degrees, 9.521 + / -0.2 degrees, 15.721 + / -0.2 degrees, 16.379 + / -0.2 degrees, 16.981 + / -0.2 degrees, 17.560 + / -0.2 degrees, 19.080 + / -0.2 degrees and 22.200 + / -0.2 degrees. The crystal form I is high in stability, high in solubility, high in blood concentration, high in bioavailability and excellent in pharmacological action, so that the crystal form I is suitable for pharmaceutical preparations.

The present application provides a pyrimidineamine compound, which is characterized in that the pyrimidineamine compound is a compound represented by Formula I, or its stereoisomer, tautomer, isotope derivative, hydrate, solvate, prodrug and pharmaceutically acceptable salt. The pyrimidineamine compound described in the present application has excellent NUAK1 / NUAK2 kinase inhibitory activity and can be used for preventing or treating the following diseases by inhibiting NUAK1 or NUAK2: neuropsychiatric diseases, metabolic diseases, tumors, visceral fibrosis diseases, and skin fibrosis diseases.

The present application provides imidazolyl pyrimidinylamine inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

Disclosed in the present invention are 6-arylquinazolin-4-amine and 6-arylpyridopyrimidin-4-amine derivatives, and the use thereof as PI3Kδ covalent inhibitors. Said derivatives disclosed by the present invention are compounds capable of being used as PI3Kδ inhibitors. PI3Kδ kinase activity and PI3K selectivity tests verify that the compounds disclosed in the present invention exhibit an obvious inhibition effect on PI3Kδ kinase activity and have obvious selectivity on the activity of PI3Kδ. In-vitro cell anti-proliferative activity tests by means of using various blood tumor cell lines exhibit that the compounds disclosed in the present invention have different inhibition effects on various blood tumor cells.

The invention belongs to the technical field of oil and gas development, and particularly relates to a sterilization defoaming agent for foam drainage and a preparation method thereof. The cleaning agent is prepared from the following components: alkynediol polyether modified silicone oil, polyoxyethylene polyoxypropylene pentaerythritol ether, modified nano silicon dioxide, an emulsifier, a mutual solvent, a benzyl quaternary ammonium salt disinfectant, a pyrilamine bactericide and water. The preparation method comprises the following steps: heating and stirring the alkynediol polyether modified silicone oil, adding the modified nano silicon dioxide, stirring, cooling, reducing the stirring speed, adding the polyoxyethylene polyoxypropylene pentaerythritol ether, and continuously stirring to obtain an intermediate product A; adding water into another reaction kettle, heating and stirring, then adding an emulsifier, a mutual solvent, a benzyl quaternary ammonium salt disinfectant and a pyrilamine bactericide, stirring to obtain an intermediate product B, and then heating; and adding the intermediate product A into the intermediate product B, and stirring. The sterilizing and defoaming agent for foam drainage has multiple functions of sterilizing and defoaming, and realizes multiple effects by one agent.

The invention belongs to the technical field of medicine detection, and particularly relates to a method for detecting related impurities of an imatinib mesylate intermediate. In particular to a method for detecting related substances in N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl) pyrimidine-2-amine. The related substances in N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl) pyrimidine-2-amine are detected by high performance liquid chromatography, and the content of each impurity in N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl) pyrimidine-2-amine is calculated by a main component external standard method with correction factors. The methodology verification shows that the detection method provided by the invention is good in specificity and high in accuracy and sensitivity, and can be used for quality control of related substances in N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl) pyrimidine-2-amine, so that the product quality is effectively controlled, and the medication safety of imatinib mesylate is improved.

Crystalline and amorphous forms of N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl-5-fluoro-4-(3-iso-propyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-amine (Compound 1) and various salts thereof, preparation methods of these crystalline and amorphous forms, pharmaceutical compositions containing these crystalline or amorphous forms, and use of these crystalline and amorphous forms, or pharmaceutical compositions thereof, for treatment of diseases or disorders associated with cyclin-dependent kinase (CDK), especially CDK4 and CDK6, activities, such as various cancers, are disclosed.

The present invention generally relates to compounds of formula (I) inhibiting 3- phosphoglycerate dehydrogenase (PHGDH) activity; particularly, the invention relates to compounds that are thienopyrimidylamine derivatives, including pharmaceutically acceptable salts thereof, methods of preparing such compounds, and therapeutic use thereof. The compounds of the invention may be useful for instance in the treatment of many disorders associated with PHGDH, for instance in the treatment of many disorders associated with fibrosis, such as idiopathic pulmonary fibrosis (IPF).

Provided herein are solid dispersions of 5-chloro-N-(3-cyclopropyl-5-{[(3R, 5S)-dimethylpiperazine-1-yl] methyl} phenyl)-4-(6-methyl-1H-indol-3-yl) pyrimidine-2-amine and methods for preparing the solid dispersions. The solid dispersions of 5-chloro-N-(3-cyclopropyl-5-{[(3R, 5S)-dimethylpiperazine-1-yl] methyl} phenyl)-4-(6-methyl-1H-indol-3-yl) pyrimidine-2 Also provided herein is a pharmaceutical composition comprising a solid dispersion of 5-chloro-N-(3-cyclopropyl-5-{[(3R, 5S)-dimethylpiperazin-1-yl] methyl} phenyl)-4-(6-methyl-1H-indol-3-yl) pyrimidine-2-amine, and a use thereof. The invention also provides a pharmaceutical composition comprising a solid dispersion of 5-chloro-N-(3-cyclopropyl-5-{[(3R, 5S)-dimethylpiperazin-1-yl] methyl} phenyl)-4-(6-methyl-1H-indol-3-yl) pyrimidine-2-amine.

The application discloses a one-pot method for preparing a medicine building block 5-bromo-4-fluoropyrimidine-2-amine, and relates to the field of organic chemical synthesis.The specific steps of the synthesis route are as follows: step one, 2-amino-4-chloropyrimidine and a bromination reagent are added into a solvent, and stirring reaction is carried out;step two, a fluorination reagent is added into the reaction solution, and heat preservation reaction is carried out;step three, water is added to precipitate, and the filter cake is dried and filtered.The 5-bromo-4-fluoropyrimidine-2-amine is prepared by the one-pot method, and the problems of low yield, complex operation, much waste, existence of isomers, and difficult purification in the existing synthesis preparation route of the 5-bromo-4-fluoropyrimidine-2-amine are solved successfully, and the method does not cause environmental pollution, and is beneficial to the green and environment-friendly industrial production of the 5-bromo-4-fluoropyrimidine-2-amine.

The present invention belongs to the technical field of oil and gas development, and particularly relates to a bactericidal defoaming agent for foam drainage and a preparation method thereof. Its components include: alkynediol polyether modified silicone oil, polyoxyethylene polyoxypropylene pentaerythritol ether, modified nano-silica, emulsifier, co-solvent, benzyl quaternary ammonium salt disinfectant, pyrimidineamine bactericide and water. The preparation method includes: heating and stirring the alkynediol polyether modified silicone oil, adding the modified nano-silica and stirring, cooling and reducing the stirring speed, adding the polyoxyethylene polyoxypropylene pentaerythritol ether, and continuing to stir to obtain intermediate product A; adding water to another reaction kettle, heating and stirring, then adding the emulsifier, co-solvent, benzyl quaternary ammonium salt disinfectant, pyrimidineamine bactericide, stirring to obtain intermediate product B and then heating up; adding intermediate product A to intermediate product B and stirring to obtain the product. This bactericidal defoaming agent for foam drainage has multiple functions of sterilization and defoaming, achieving multiple effects with one agent.

To provide a solid pharmaceutical composition excellent in stability and elution properties comprising a TLR7 agonist (2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine).SOLUTION: A solid pharmaceutical composition comprises a TLR7 agonist (2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine), a diluent, a binder, a disintegrant, and a lubricant. The diluent is selected from among microcrystalline cellulose and the like. The disintegrant is selected from among sodium carboxymethyl starch and the like. The binder is selected from among hydroxypropyl methylcellulose and the like. The lubricant is selected from among magnesium stearate and the like.SELECTED DRAWING: None

Provided in the present invention are an oxazolone-substituted pyrimidinamine compound, a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Specifically, provided in the present invention are a compound having a structure as shown in general formula (I), and a racemate, R-isomer, S-isomer, pharmaceutically acceptable salt thereof, or a mixture thereof. The compound has good IDH1 inhibitory activity, and therefore can be used for treating, preventing and relieving diseases related to IDH1 enzyme, especially for treating malignant tumors or other related diseases caused by IDH1 enzyme mutation.

The present application relates to a synergistic composition containing a biologically effective amount of compound A and component B, wherein the component B is one of thiazide ketone, avermectin, spirotetramat, pyridalyl, emamectin benzoate, azamethiphos, azocyclotin, pyridaben, quimacryd thiocyl, pyrimidifen, tebufenpyrad, flufenoxuron, chlorfenapyr, cyromazine, and halofenozide, and a method thereof for controlling pests in agronomic and non-agronomic environments. The compound A has a synergistic effect with the component B, which can improve the pest control effect, reduce the application amount, reduce the use frequency, and reduce the use cost.

The invention belongs to the technical field of organic chemistry, and particularly relates to a nitration method of 5-phenylpyrazolo [1, 5-a] pyrimidine-7-amine, which comprises the following steps: adding 5-phenylpyrazolo [1, 5-a] pyrimidine-7-amine and Fe (NO3) 3.9 H2O into a reaction tube, adding a solvent, and after the reaction is completed, separating and purifying the reaction liquid to obtain the final product 3-nitro-5-phenylpyrazolo [1, 5-a] pyrimidine-7-amine. The invention relates to a pyrimidine-7-amine compound. The efficient selective C3 nitration method of 5-phenylpyrazolo [1, 5-a] pyrimidine-7-amine and iron nitrate nonahydrate is realized at room temperature under the action of a solvent by taking non-toxic, cheap and easily available Fe (NO3) 3.9 H2O as a nitro source without additionally adding a metal catalyst, an organic ligand and alkali, a corresponding nitration product is obtained, and the highest yield can reach 94%.