36 results about "Oxadiazole" patented technology

The application discloses a continuous synthesis method of an amicarbazone intermediate 5-isopropyl-1,3,4-oxadiazole-2(3H)-ketone. The method comprises two continuous processes of hydrazinolysis and phosgenation: continuously feeding a mixture of isobutyric acid and a solvent, a mixture of hydrazine hydrate and a catalyst into a hydrazinolysis continuous reactor respectively, carrying out a warming reflux dehydration reaction, and obtaining an isobutyryl hydrazine solution shown in formula I; continuously feeding the isobutyryl hydrazine solution and phosgene into a phosgenation continuous reactor, carrying out a phosgenation reaction, and after distillation and desolventizing treatment of a reaction solution, obtaining 5-isopropyl-1,3,4-oxadiazole-2(3H)-ketone shown in formula II. The application has the advantages of simple reaction flow, high product yield, and significant production efficiency improvement, and is suitable for industrial large-scale production.

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I)In the formula Q is O, R1 is the side chain of Ser, R2 is —CO-Thr, R3 is the side chain of Asn or Glu, and R4, R5 and R6 are each H.

This invention relates to a compound containing trifluoromethyloxadiazole and a spirocyclic structure, or a pesticide-acceptable salt, hydrate, or solvate thereof, characterized in that the structure of the compound containing trifluoromethyloxadiazole and a spirocyclic structure is shown in general formula I. Compared with the prior art, the compound provided by this invention can be used to prepare histone deacetylase inhibitors, effectively inhibiting the growth and reproduction of various rust fungal spores, with effects comparable to fluopyram.

This invention discloses a high-fire-resistant concrete, characterized by being composed of the following components in parts by weight: 20-25 parts cement, 30-35 parts crushed stone, 10-25 parts river sand, 10-12 parts volcanic ash, 10-20 parts water, 1-3 parts epoxy-propionic acid modified octa-tetramethylcyclotetrasilazane, 0.3-0.6 parts guanidine carbonate, 1-3 parts calcium borate, 0.5-1 part waste polyarylene diazole fiber, and 0.1-0.3 parts 3-chloro-2-hydroxypropanesulfonic acid modified 2,5-bis(diethylamino)phenyl-1,3,4-diazole. This invention also discloses a method for preparing the aforementioned high-fire-resistant concrete. The high-fire-resistant concrete disclosed in this invention exhibits high fire resistance, good workability, excellent comprehensive performance, impermeability and crack resistance, durability, and high compressive strength.

The disclosure provide compounds of Formula I and the pharmaceutically acceptable salts thereof. The variables, R1, R2, R3, X1, X2, and Z are defined herein. Certain compounds of Formula I act as selective mitochondrial protonophore uncouplers that do not affect the plasma membrane potential. Compounds and salts of Formula I are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as cancer, obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, compounds of Formula I are useful for increasing lifespan. Compounds and salts of Formula I are also useful for regulating glucose homeostasis or insulin action in a patient.

The present invention provides, inter alia, a process for the preparation of substituted oxadiazole derivatives of formula (I), which can be obtained through reaction of amidoximes of formula (II) in the presence of an organic guanidine base, wherein the substituents are as defined in the claims. The present invention further provides intermediate compounds utilized in said process, and methods for producing said intermediate compounds.

The present application relates to the field of organic chemistry, in particular to the use of silicon compounds in cyclization reactions, and provides a preparation method of 5-chloromethyl-2-trifluoromethyl-1,3,4-oxadiazole, which comprises: subjecting 1-(chloroacetyl)-2-(trifluoroacetyl)hydrazine to a cyclization reaction in the presence of a silicon compound and an amide compound to provide 5-chloromethyl-2-trifluoromethyl-1,3,4-oxadiazole. The silicon compound or / and the amide provided by the present application can be used as a cyclization reagent to efficiently perform cyclization synthesis, and has higher comprehensive benefits compared with other methods in the prior art.

The utility model discloses a perovskite solar cell relates to the technical field of solar cell, perovskite solar cell includes first electrode layer, hole transport layer, perovskite layer, passivation layer, electron transport layer and second electrode layer who sets gradually, wherein, passivation layer includes 2-(4'-tert butyl phenyl)-5-(4'-diphenyl)-1,3,4-oxadiazole layer. Through setting 2-(4'-tert butyl phenyl)-5-(4'-diphenyl)-1,3,4-oxadiazole layer between perovskite layer and electron transport layer, make up the defect site of perovskite layer, reduce charge recombination, can also adjust the energy level structure of electron transport layer, optimize the charge transport between perovskite layer and electron transport layer, thereby improve the separation and transport efficiency of photoinduced carrier.

The present invention discloses two novel synthetic methods for preparing monothiol-labeled mesylphenyl oxadiazole active esters. These methods use inexpensive commercial raw materials to prepare two kinds of mesylphenyl oxadiazole active esters for thiol labeling of antibodies, polypeptides, hydrogels, etc. through conventional transformations such as condensation and coupling. The preparation method of the present invention has a simple process, easily available raw materials, high product added value, and has good economic benefits and market prospects.

The present application relates to the technical field of agrochemicals and fungicides, and discloses a benzoic acid sulfide compound containing a trifluoromethyl oxadiazole fragment as well as a preparation method and application thereof.The compound has a structure shown in formula I, wherein R 1 ‑R 5 Each is independently selected from one of a 1-6-membered heterocyclic ring, an alkyl group containing 1-12 carbon atoms, an alkoxy group containing 1-12 carbon atoms, hydrogen, halogen, amino, nitro, cyano, trifluoromethyl, and trifluoromethoxy.In the presence of a first solvent and a first base, 4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzoyl chloride is subjected to a condensation reaction with a compound of formula II to obtain the benzoic acid sulfide compound containing a trifluoromethyl oxadiazole fragment.The benzoic acid sulfide compound containing a trifluoromethyl oxadiazole fragment provided by the present application has a novel structure, and the bioactivity determination result shows that the compound has good fungicidal activity on soybean rust and wheat scab, and is suitable for wide range of popularization and application.

The application discloses a 1,3,4-oxadiazole sulfide compound containing an isopropanolamine structure and a preparation method and application thereof. The preparation method of the 1,3,4-oxadiazole sulfide compound containing the isopropanolamine structure is simple in operation, does not involve a noble metal in the reaction, and is efficient. The 1,3,4-oxadiazole sulfide compound containing the isopropanolamine structure has good bactericidal activity, and the 1,3,4-oxadiazole sulfide compound containing the isopropanolamine structure shows efficient and / or broad-spectrum bacteriostatic activity, and can be effectively used in the prevention and treatment of crop pathogenic bacteria.

The present invention relates to a process for the preparation of aromatic carboxyamides of formula I, which can be obtained by a palladium-catalyzed carbonylation reaction of aromatic chlorides of formula II, amines of formula III and carbon monoxide in the presence of 1,5,7-triazabi-cyclo[4.4.0]dec-5-ene. The invention further relates to a process for the preparation of aryl-5-trifluoromethyl-1,2,4-oxadiazoles, which are known for controlling phytopathogenic fungi.

The present application relates to the preparation method of 3-phenyl-5-aryl-1,2,4-oxadiazole by electro-oxidation, and the preparation reaction is as follows: wherein R is selected from hydrogen, 4-fluoro, 4-chloro, 2-bromo, 4-tert-butyl, 3-methyl or 3,4-dimethyl; Ar is selected from phenyl, 2-thiophenyl, 2-fluorophenyl, 4-chlorophenyl, 2-bromophenyl, 4-fluorophenyl or 4-methylphenyl. The preparation method of electro-oxidation is that (Z)-N'-hydroxy-N-(arylmethyl) benzamidine, organic solvent, base and electrolyte are used as electrolyte in a non-membrane electrolytic cell, and then constant voltage electrolysis is carried out at a certain temperature for a certain time, so that 3-phenyl-5-aryl-1,2,4-oxadiazole (I) is obtained by electro-oxidation reaction. The preparation method of electro-oxidation can be used for preparing line thiophene and ataluren.

The invention relates to compounds of Formula (I) as described herein, useful as histone deacetylase 6 (HDAC6) inhibitors. The invention also relates to pharmaceutical compositions comprising these compounds and to their use in therapy.

The present application relates to 5-[1,2,4-oxadiazole]-6-oxygen-pyrazolopyridine derivatives and preparation method and application thereof, and the 5-[1,2,4-oxadiazole]-6-oxygen-pyrazolopyridine derivatives and pharmaceutically acceptable salts thereof, the general formula is as shown in formula (II): wherein, the definition of substituent group is described in the specification. The 5-[1,2,4-oxadiazole]-6-oxygen-pyrazolopyridine derivatives and pharmaceutically acceptable salts thereof of the present application have the functions of inhibiting Hsp110-STAT3 interaction, thereby down-regulating p-STAT3 and c-Myc levels, inhibiting pulmonary arterial endothelial cell proliferation, migration and apoptosis resistance, reducing pulmonary arterial pressure and improving the degree of pulmonary vascular remodeling, and further playing the role of anti-pulmonary arterial hypertension.

The objective is to provide a method for producing 1,2,4-oxadiazole-5(4H)-one derivatives that have pest control properties, which offers excellent yield and is advantageous for industrial-scale production. [Solution] We have discovered a method for producing 1,2,4-oxadiazole-5(4H)-one derivatives in high yield and on an industrial scale by reacting hydroxyimidamide derivatives with halogenated carbamate compounds in the presence of a base selected from carbonates, hydroxides, metal alkoxides, and metal hydrides.

Preparation of aromatic carboxyamides by palladium-catalyzed carbonylation reaction The present invention relates to a process for the preparation of aromatic carboxyamides of formula I, which can be obtained by palladium-catalyzed carbonylation reaction of aromatic chlorides of formula II, amines of formula III and carbon monoxide in the presence of a base. The invention further relates to a process for the preparation of aryl-5-trifluoromethyl-1,2,4-oxadiazoles, which are known for controlling phytopathogenic fungi.

This invention discloses two novel methods for synthesizing dithiol-bridged labeled bis(methylsulfonyl)phenyloxadiazole. These methods utilize inexpensive, commercially available raw materials and conventional transformations such as condensation and coupling to prepare two bis(methylsulfonyl)phenyloxadiazoles suitable for dithiol-bridged labeling of antibodies, peptides, and hydrogels. The preparation methods of this invention are simple, use readily available raw materials, and produce high-value-added products, demonstrating significant economic benefits and market potential.

The invention relates to a novel 1, 2, 4-oxadiazole compound (I) as a fungicide, in which A1, R1, R2, R3, R4 and R5 are defined in the specification. The invention also discloses a preparation method of the compound of the formula (I) and application of the compound as a fungicide. (I)

This invention discloses a difluoromethylpyrimidine-substituted 1,3,4-oxadiazole derivative for the prevention and control of pathogenic fungi in edible fungi, its preparation method, and its application. It relates to the field of biochemistry, and the key technical points are: through rational molecular design, a class of thioether derivatives (6a-6t) with difluoromethylpyrimidine as the parent nucleus and 1,3,4-oxadiazole as the active terminal group were constructed, and their inhibitory activity against *Trichoderma* and *Mucor* was systematically studied. The results show that some compounds exhibit superior EC50 activity compared to the commercially available fungicide pyrimethanil. 50 It has high value, and the synthesis process is simple and controllable, showing good development prospects.

This invention relates to a method for preparing compound (I) or a pharmaceutically acceptable salt or solvate thereof. In particular, such a method comprises the dehydration cyclization of a 1,2-diacylhydrazine intermediate to form the corresponding 1,3,4-oxadiazole, wherein the dehydration cyclizing agent may be N,N-dimethylaminosulfonyl chloride, N-(triethylammonium sulfonyl)carbamate, phosphorus trichloride, or phosphorus pentachloride, resulting in increased product yield and purity compared to known methods. Compound (I) and pharmaceutical compositions thereof can be used as respiratory syncytial virus (RSV) inhibitors.

This invention discloses an acrylonitrile-functionalized covalent organic framework material, its preparation method, and its applications. The material framework contains both acrylonitrile and benzoxoxadiazole groups, and is prepared through stepwise synthesis of amine monomer QA and aldehyde monomer OA, followed by solvothermal condensation of the two. During the preparation process, parameters such as the raw material ratio, reaction temperature, and time are precisely controlled. The material obtained by this invention exhibits good crystallinity, high photogenerated carrier separation efficiency, and, without sacrificial agents, a photocatalytic synthesis yield of over-H₂O₂ of no less than 3500 μmol / g under visible light irradiation. ‑1 h ‑1 In a seawater system with 0.5~1.0 mol / L chloride ions, the activity retention rate is not less than 85% after continuous catalysis for 4~5 days. The preparation process is mild, environmentally friendly, and easy to scale up. It can be efficiently applied to the photocatalytic synthesis of H2O2 in high-salt environments such as pure water and seawater.

The application belongs to the field of plant protection, and specifically provides application of a thiazole compound in preparation of a medicine for preventing and treating plant nematode diseases. The thiazole compound includes 5-(chloromethyl)-3-(2,4-dichlorothiazol-5-yl)-1,2,4-oxadiazole, 5-(bromomethyl)-3-(2,4-dichlorothiazol-5-yl)-1,2,4-oxadiazole and the like. Through nematode-killing activity tests on Bursaphelenchus xylophilus, Meloidogyne incognita and Aphelenchoides besseyi, it is found that the compounds have good and broad-spectrum nematode-killing activity.

The present disclosure provides a fluorescently-traceable amino acid derivative and a preparation method and use thereof, and belongs to the technical field of biomedicine. In the present disclosure, an amino acid skeleton of the amino acid derivative is modified mainly by a fluorescently-traceable functional group. 4-chloro-7-nitro-2,1,3-benzoxadiazole (NBD-Cl) has low polarity and strong fluorescence, and can be used to modify an N-terminal of the amino acid skeleton to conduct subcellular imaging. Moreover, the NBD-Cl has a relatively small volume, lacks reaction orthogonality, and causes little interference with biochemical reactions of the organism itself. The results of examples show that the fluorescently-traceable amino acid derivative has a desirable biological activity and can be fluorescently traced in vivo and in vitro.

The present invention provides modified catalytic antibody 38C2 with arylation of the reactive lysine residue (Lys99). The Lys99 residue is arylated with a heteroaryl methyl sulfonyl compound such as methylsulfone phenyl oxadiazole (MS-PODA). The invention also provides antibody conjugated agents (e.g., antibody drug conjugates) that contain an agent moiety that is site-specifically conjugated to 38C2 via a methyl sulfonyl compound. Further provided in the invention are methods of making the antibody conjugated agents and therapeutic applications of the antibody conjugated agents.

The present invention relates to salt derivatives of (R)-6-(5-fluoropyridine-2-yl)-8-methoxy-N-(1-(5-methyl-1,2,4-oxadiazole-3-yl)ethyl)quinazoline-4-amine, and more particularly to mesylates and esylates of (R)-6-(5-fluoropyridine-2-yl)-8-methoxy-N-(1-(5-methyl-1,2,4-oxadiazole-3-yl)ethyl)quinazoline-4-amine, pharmaceutical compositions containing them, and their therapeutic uses. The salts of the present invention may be useful in the treatment of respiratory diseases, particularly diseases or conditions associated with chronic cough.