53 results about "Pyrazole Compound" patented technology

The present application relates to a kind of preparation method of trifluoromethyl pyrazole compound, belong to the technical field of organic synthesis.The specific method is: (1) trifluoroacetyl ethyl acetate is first with hydrazine hydrate cyclization reaction and generates compound of formula III;(2) under the catalysis of base, compound of formula III is reacted with difluoromethylation reagent and generates compound of formula II;(3) compound of formula II is reacted with methylating agent and obtains compound of formula I;The difluoromethylation reagent is difluoro-monochloromethane or sodium difluoro-monochloroacetate;The methylating agent is chloromethane, bromomethane, iodomethane, dimethyl sulfate or dimethyl carbonate.The present application is prepared by changing reaction route, and the higher-priced raw material methylhydrazine is replaced, and isomer impurity is no longer generated in the product prepared.Not only raw material cost is reduced, but also the purity of product is improved.

The present application belongs to the field of agricultural fungicides, and particularly relates to a fungicidal composition and application thereof.The composition comprises two active components A and B, the weight ratio of the active component A to the active component B is 1:99-99:1; the active component A is one or more of substituted pyrazole compounds containing pyrimidine or salts thereof, and the active component B is selected from one fungicide.The fungicidal composition is particularly suitable for preventing and treating various plant pathogenic fungi and bacterial diseases.

Disclosed herein are embodiments of a method for treating a disease or condition in a subject, comprising administering to the subject, a pyrazole compound according to formula I.The compound may be administered as a composition, such as a spray-dried formulation. The disease or condition may be hidradenitis suppurativa, or a lymphoid neoplasm, and may be chronic myeloid leukemia or chronic myelomonocytic leukemia.

The application discloses a kind of thieno [2, 3-c] pyrazole compounds in preparation antitumor drug purposes, belong to pharmaceutical chemistry technical field.The application provides a kind of small molecule skeleton thieno [2, 3-c] pyrazole compound I and II, compound I is 2-oxo benzo [d] [1, 3] oxathiole-6-yl 1-(3-fluorophenyl)-3-methyl-1H-thieno [2, 3-c] pyrazole-5-carboxylate.Compound II is 1-(4-chlorophenyl)-N-[4-((4-ethylpiperazine-1-yl)methyl)phenyl]-3-methyl-1H-thieno [2, 3-c] pyrazole-5-formyl.Both have strong antitumor activity.Compound II has strong inhibition to a variety of human tumor cells, such as bone sarcoma MG63, breast cancer HCC1806, liver cancer LM3, lung cancer A549, colorectal cancer HCT-8 and the like, provides new candidate compounds for broad-spectrum antitumor drugs.

The present invention relates to the use of novel nitrification inhibitors of formula I, which are N-functionalized alkoxy pyrazole compounds. Moreover, the invention relates to the use of compounds of formula I as nitrification inhibitors, i.e. for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors of formula I.

This invention discloses a method for preparing 4-(trifluoromethylsulfinyl)pyrazole compounds, comprising: dissolving terminal alkyne in n-hexane under nitrogen atmosphere, adding anhydrous zinc chloride, and reacting trifluoromethylsulfinyl chloride to obtain α-trifluoromethylalkynyl sulfoxide; adding benzoyl chloride dropwise to a CH2Cl2 solution of phenylhydrazine and triethylamine under nitrogen atmosphere to obtain acylhydrazine; adding carbon tetrachloride to a suspension of acylhydrazine and triphenylphosphine in acetonitrile to obtain hydrazone chloride; and reacting α-trifluoromethylalkynyl sulfoxide, hydrazone chloride, potassium carbonate, and anhydrous ethanol at room temperature to obtain 4-(trifluoromethylsulfinyl)pyrazole compounds. This invention uses inexpensive and readily available raw materials, the entire reaction route is mild and simple to operate, does not require stringent reaction conditions, and most of the reaction process is carried out at room temperature. The product yield is high, and the prepared trifluoromethylalkynyl sulfoxide pyrazole structure has multiple derivatization sites, showing good application prospects.

A fluorine-containing pyrazole compound is represented by the following general formula (1):wherein in formula (1) above, R represents a hydrocarbon group having 1 to 12 carbon atoms, and a ring Z represents an aromatic heterocyclic ring containing at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom.

The application discloses a preparation method of an amido pyrazole compound and a method for preparing sildenafil by using the same. The amido pyrazole compound is shown as formula I. The compound of formula I is prepared by using 2-pentanone as an industrial chemical, and can be used for synthesizing sildenafil which is a selective inhibitor of type 5 phosphodiesterase (PDE5). The method has the advantages of easy availability of raw materials, simple operation, avoidance of nitration reaction, avoidance of safety hidden dangers caused by the nitration reaction from a technical source, and avoidance of environmental protection pressure caused by a large amount of nitration waste liquid, and is suitable for development into a green and sustainable production process of sildenafil bulk drug.

The application discloses a kind of benzofuran pyrazole compounds or its pharmaceutically acceptable salt or deuteride and preparation method and application thereof.A variety of biological experiments confirm that the compound prepared in the application has MYC inhibitory activity, and has significant antitumor activity and can enhance the response of tumor to immunotherapy, and can be used as MYC inhibitor for the treatment of tumor and other MYC related diseases, and has good application prospect.

The application belongs to the technical field of organic synthesis, and particularly relates to a 1,3,5-trisubstituted pyrazole compound and a preparation method thereof. The preparation method of the 1,3,5-trisubstituted pyrazole compound provided by the application comprises the following steps: mixing a hydrazine compound, an alpha-bromoketone compound, a photocatalyst, an alkaline compound, an additive and a polar organic solvent, and performing an addition cyclization reaction under light irradiation to obtain the 1,3,5-trisubstituted pyrazole compound. The preparation method has the advantages of mild conditions, easy control, high reaction efficiency, economical steps, cheap and easily available raw materials, no use of oxidants, good functional group tolerance and the like, and the prepared 1,3,5-trisubstituted pyrazole compound has high purity, the purity is 98.5-99.9%, and has great market promotion value.

The invention discloses application of a thieno [2, 3-c] pyrazole compound in preparation of antitumor drugs, and belongs to the technical field of medical chemistry. The invention provides a small molecular skeleton thieno [2, 3-c] pyrazole compound I and a small molecular skeleton thieno [2, 3-c] pyrazole compound II, and the compound I is 2-oxobenzo [d] [1, 3] oxathiacyclopentane-6-yl 1-(3-fluorophenyl)-3-methyl-1H-thieno [2, 3-c] pyrazole-5-formate. And the compound II is 1-(4-chlorphenyl)-N-[4-((4-ethyl piperazine-1-yl) methyl) phenyl]-3-methyl-1H-thieno [2, 3-c] pyrazole-5-formyl. The two compounds have relatively strong anti-tumor activity. Wherein the compound II has a relatively strong inhibition effect on various human tumor cells such as osteosarcoma MG63, breast cancer HCC1806, liver cancer LM3, lung cancer A549, colorectal cancer HCT-8 and the like, and a new candidate compound is provided for broad-spectrum antitumor drugs.

The application belongs to the technical field of chemical drugs, and particularly relates to a pyrazole compound and a preparation method and application thereof. The application provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, which not only has good myeloperoxidase (MPO) inhibitory activity, but also can be used for treating and / or preventing cardiovascular diseases. (I)

Provided is a radioactive triphenylpyrazole compound that is useful as an active ingredient of a pharmaceutical composition, particularly an imaging agent, and is stable in vivo. 4-(4-[18F]fluoro-2-(1-phenyl-5-(2-(trifluoromethyl)phenyl)-1H-pyrazole-3-yl)phenoxy)butanoic acid or a salt thereof can be used as a radioactive triphenylpyrazole compound according to the present invention.

The present application relates to the technical field of organic synthesis, in particular to a synthesis method of polysubstituted pyrazole compounds, which comprises adding aryl diazonium salt 0.6 mmol, enone 0.9 mmol, 0.5 ml of acid and 0.3 mmol of electrolyte into a 10 ml three-necked bottle, and then adding 6 ml of solvent to dissolve; using a carbon rod as an anode and a platinum plate as a cathode, stirring the reaction, monitoring the reaction process by using thin layer chromatography, after the reaction is completed, extracting the mixture with ethyl acetate; drying the organic layer of the mixture with anhydrous sodium sulfate, rotary evaporating the solvent under reduced pressure, purifying the residue by column chromatography, and obtaining the target product; the method uses aryl diazonium salt as a double synthetic substrate under mild electrochemical conditions, continuously generates two free radicals by electrochemical reduction of aryl diazonium salt, directly synthesizes a series of polysubstituted pyrazole compounds, directly and orderly constructs polysubstituted pyrazole compounds without transition metal or external redox agent, is environment-friendly, efficient and high in atom economy.

The application belongs to the technical field of organic compounds and agricultural fungicides, and particularly relates to the antifungal application of a novel pyrazole compound. The application provides a novel pyrazole compound, which has a structure shown in formula (a). The pyrazole derivative has good antibacterial activity on various fungi and can be used for preparing an agricultural fungicide. Moreover, the pyrazole compound in the application has the advantages of simple synthesis and high yield, and overcomes the problems of complex synthesis and low yield of current pyrazole fungicides. The application has important significance for promoting the application of pyrazole fungicides in the disease control of crops, fruits and vegetables. The application not only provides a new control drug for crop fungi and fungal diseases caused by the fungi, but also enriches the resource library of pyrazole fungicides, and provides more choices for the application of pyrazole derivatives in the fields of medicine and agricultural research.

This invention provides an asymmetric o-phenanthroline amide pyrazole compound, its preparation method, and its applications, belonging to the field of nuclear fuel cycle and high-level radioactive waste treatment technology. The asymmetric o-phenanthroline amide pyrazole compound provided by this invention has the structure shown in Formula I. The asymmetric o-phenanthroline amide pyrazole compound provided by this invention exhibits good performance against Am under high acidity conditions. 3+ The extraction partition ratio is high, and the separation effect is excellent. Under 3 mol / L nitric acid conditions, the asymmetric o-phenanthroline amide pyrazole compound provided by this invention has a high separation efficiency for Am. 3+ and Eu 3+ Extraction partition ratio ( D The separation factors were 3.32 and 0.09, respectively. SF Am / Eu It is 36.9, for Am 3+ It has a good separation effect.

The invention discloses a phenyl pyrazole compound and application thereof. The structure of the compound is shown as a general formula I, wherein the definition of each substituent group in the formula is shown in the specification. Also disclosed in the specification are their use as insecticidal and acaricidal agents and animal parasite control agents.

A pharmaceutical composition of pyrazole compound and a surfactant and a method of using the same to treat atopic dermatitis.

The present invention relates to benzopyrazole compounds and analogs thereof. Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of Formula (I), and methods relating to the use of the compounds and compositions to treat and prevent diseases and conditions characterized by aberrant complement system activity.

The present invention is in the field of nitrification inhibitor compositions and fertilizer formulations and, in one aspect, relates to a composition for reducing nitrification comprising (a) at least one specific alkoxypyrazole compound of formula (I), (b) at least one solvent wherein the solvent comprises at least one monomeric alcohol (b1) and optionally at least one specific N, N-dimethylpyrazole compound of formula (II), an N, N-dialkylamide (b2); wherein the composition comprises compound (a) in an amount of up to 47 wt.-% and at least one solvent (b) in an amount of at least 53 wt.-%, relative to the total weight of (a) and (b). Furthermore, the present invention relates to a solid fertilizer composition comprising such a composition; a method for producing a solid nitrogen-containing fertilizer composition according to the invention; use of a solvent composition comprising at least one monomeric alcohol and optionally at least one N, N-dialkylamide of formula (II) for stabilizing an alkoxypyrazole compound of formula (I) in a solid fertilizer composition; and a use of the composition or solid fertilizer composition or a method for reducing nitrification.

The application discloses a mixed acid nitration organic wastewater treatment method and system and belongs to the technical field of organic chemical wastewater treatment. ‑ The application can effectively degrade toxic and harmful pollutants in wastewater and meets the subsequent biochemical treatment demand, and provides practical value for effective treatment of wastewater in the production process of nitryl pyrazole compounds.

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, which are capable of modulating the GLP-1 receptor; the invention also relates to salts, solvates, stereoisomers or tautomers thereof, pharmaceutical compositions, processes for their preparation and therapeutic uses.

Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitor compounds and compositions comprising such compounds. The compounds may have a structure according to Formula I (I) Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and / or compositions may be used to treat or prevent an IRAK-associated disease or condition.

The present invention relates to a compound having formula (I) or an agronomically acceptable salt of said compound, wherein Q, U, R2 and R3 are as defined herein. The invention further relates to herbicidal compositions comprising compounds of formula (I) and to the use of compounds of formula (I) for controlling weeds, in particular in crops of useful plants.

Providing a novel agent having an excellent control effect. 【Solution means】Provided are a pyrazole compound represented by formula (1) or a salt thereof, and a novel fungicide containing the same as an active ingredient, particularly a fungicide for agricultural and horticultural use. In the formula, G represents G-1, and G 1 represents C1-C6 alkyl or the like, and R X represents C1-C6 alkyl or the like, and R Y represents a hydrogen atom or the like, and R 2 represents a hydrogen atom or the like, and R 3 represents a hydrogen atom or the like, Z 1 represents E-1 or the like, Z a represents C1-C6 alkyl or the like, Z 2 represents C1-C6 alkyl or the like, m5 represents an integer of 0, 1, 2, 3, 4 or 5, n4 represents an integer of 0, 1, 2, 3 or 4, and v2 represents an integer of 0, 1 or 2. JPEG2026069209000025.jpg24104