23 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 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.

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.

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)

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.

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 provides a pyrazole compound represented by a formula (1) or a salt thereof, and a novel fungicide, in particular, agricultural-horticultural fungicide that contains it as an active ingredient. The formula indicates a structure in which G represents G-1, G1 represents C1-C6 haloalkyl, etc., T represents an oxygen atom, etc., RX represents C1-C6 alkyl, etc., RY represents a hydrogen atom, etc., R1 represents a hydrogen atom, etc., R2 represents a hydrogen atom, etc., R3 represents a hydrogen atom, etc., Ra represents a hydrogen atom, etc., Z represents Z-1, etc., Z1 represents C1-C6 alkyl, etc., m5 and n5 each represent an integer of 0, 1, 2, 3, 4, or 5, and p represents an integer of 0 or 1.

This invention discloses a 3-trifluoromethyl-substituted pyrazole compound or a pharmaceutically acceptable salt thereof and its application. The 3-trifluoromethyl-substituted pyrazole compound or its pharmaceutically acceptable salt has the structure shown in formula (I). The 3-trifluoromethyl-substituted pyrazole compound or its pharmaceutically acceptable salt of this invention exhibits excellent inhibitory activity against PDE10A (phosphodiesterase type 10A), and compared to other phosphodiesterase subtypes, it shows high selectivity for phosphodiesterase type 10A, making it a specific drug for inhibiting phosphodiesterase type 10A activity. It also exhibits good metabolic stability, with a half-life of up to 239 min after metabolism by rat liver microsomes, solving the problem of excessively rapid metabolism of pyrazole PDE10A inhibitors such as MP-10.

The present disclosure relates to methods of making N2-(3-(2-(2H-1, 2, 3-triazol-2-yl)propan-2-yl)-1-cyclopropyl-1H-pyrazol-5-yl)-N4-ethyl-5-(trifluoromethyl)pyrimidine-2,4-diamine and intermediates thereof.

Disclosed herein is a compound. Also disclosed are compositions comprising the compound and a pharmaceutically acceptable excipient, methods for making the compound, and methods of using the compound as a therapy for subjects suffering from, or susceptible to, a disease involving a vascular pathology.

Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formulaein which R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.

This invention relates to an electrochemical synthesis method for fully substituted sulfonated pyrazole compounds. The method includes the following steps: mixing acetylacetone, substituted arylsulfonyl hydrazides, and an electrolyte, adding the mixture to a mixed solvent to obtain a mixed solution; subjecting the mixed solution to an electrochemical reaction to obtain a reaction mixture; and separating and purifying the reaction mixture to obtain the fully substituted sulfonated pyrazole compounds. Compared with existing technologies, this invention uses an electrochemical method to prepare fully substituted sulfonated pyrazole compounds. During the reaction, an iodine-containing electrolyte undergoes an oxidation reaction at the anode to generate iodine free radicals. These iodine free radicals then react with arylsulfonyl hydrazides and acetylacetone with different substituents to form the fully substituted sulfonated pyrazole compounds. This method has advantages such as simple preparation, convenient operation, high atom utilization, and mild reaction conditions.

The present disclosure addresses the problem of providing a novel compound or a novel agrochemical. Provided is a pyrazole compound represented by general formula (1) (where: A represents iodine, optionally substituted alkynyl, or the like; Z represents an optionally substituted divalent carbocyclic ring or the like; X represents an oxygen atom or carbonyl (C=O); T represents an oxygen atom or a sulfur atom; L represents optionally substituted alkyl or the like; R1 represents a hydrogen atom or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom or the like). Also provided is a structural isomer of the pyrazole compound, or a salt of the pyrazole compound or of the structural isomer.

Crystalline forms of compounds represented by formula (II)-formula (VIII) and formula (I)-formula (VIII-1) are provided, along with a method of preparing the same and an application of the compounds and crystalline forms in the preparation of a drug for the treatment of a related disease.

The present invention provides a process for preparing substituted pyrazole compounds of Formula II, which are useful as intermediates for preparing substituted piperidine urea compounds useful for treating dilated cardiomyopathy (DCM).R 2 is independently selected from F, C1-C4 alkyl, C1-C4 haloalkyl,R 3 is independently selected from H, F, C1-C4 alkyl, C1-C4 haloalkyl,R 4 is C1-C4 alkyl,R 6 is H or a protecting group, andR 7 is selected from H, CI or trialkylsilyl.

The present invention relates to a pyrazole compound and a preparation method therefor and a use thereof. In particular, the present invention relates to a compound shown in Formula I, a pharmaceutical composition containing same or a pharmaceutically acceptable form thereof, a pharmaceutical composition thereof, a preparation method therefor, and a use thereof. The compound can be used as a drug for treating cancer or fibrosis disease,

A novel fungicide, particularly for agricultural and horticultural use, is provided. A pyrazole compound or a salt thereof, as shown in formula (1), is provided. In the formula, G represents G-1, etc. 1 Indicates C1-C6 haloalkyl groups, etc., R X Indicates C1-C6 alkyl groups, etc., R Y W represents hydrogen atoms, etc., and W represents -O- or -C(R) a (R) 2 )-, R 1 R represents hydrogen atoms, etc. 2 R represents hydrogen atoms, etc. 3 R represents hydrogen atoms, etc. 4 R represents hydrogen atoms, etc. a Z represents hydrogen atoms, etc., and Z represents Z⁻¹, etc. 1 The symbols represent C1 to C6 alkyl groups, m5 and n5 represent integers 0, 1, 2, 3, 4 or 5, and p represents structures expressed as integers 0 or 1.