179 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.

The invention discloses an aryl oxadiazole compound with a chemical structural formula as shown in the specification or pharmaceutically acceptable salt thereof. In-vitro experiment results show that the compound has a remarkable inhibition effect on DENV, the therapeutic index (TI) of the compound is far higher than that of a clinical reference substance ribavirin, the TI value of a preferred compound such as I-29 exceeds 1131.86, and the TI value of the preferred compound is far higher than that of the clinical reference substance ribavirin. The characteristics of high efficiency and low toxicity are highlighted. In addition, the preparation method is simple in process, high in yield, mild in reaction condition and suitable for large-scale production and clinical popularization.

The application discloses a blue fluorescent molecule, which has a D-pi-A structure, contains an oxadiazole as an acceptor group and a phenyl carbazole as a donor group, and connects the acceptor group and the donor group with an aromatic ring having a thermal excitation energy level arrangement characteristic as a pi bridge. The application also provides a preparation method and application of the blue fluorescent molecule. The application uses the aromatic ring having the thermal excitation energy level arrangement characteristic as the pi bridge, reasonably regulates a high-energy excited state of the acceptor by introducing the donor, activates a thermal excitation channel of the molecule, breaks through a limitation of 25% of an excitation utilization rate of a fluorescent material, and thus improves the excitation utilization rate.

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.

The present application relates to a kind of aromatic oxadiazole polymer modified membrane and its preparation method.The preparation method of the modified membrane includes the following steps: step (1) with terephthalic dihydrazide as raw material, with polyphosphoric acid as solvent and dehydrating agent, polymerization is carried out to obtain prepolymer solution, wherein ternary acid and polyol are added during polymerization reaction;Step (2) the prepolymer solution obtained in step (1) is made into film, dried, to obtain modified membrane.The present application constructs the new network structure of aromatic oxadiazole polymer, and the modified membrane prepared has good film-forming property, is soft and transparent, has good mechanical property, has high thermal stability and chemical stability.

The invention discloses a 1, 2, 4-oxadiazole compound and a preparation method and application thereof.The preparation method comprises the steps that 1, 2, 4-oxadiazole serves as a parent nucleus structure and reacts with aromatic amine intermediates containing different substituent groups, structures such as alkyl, halogen, alkoxy and trifluoromethyl are introduced, oxalyl chloride serves as an acylating agent, a condensation reaction is conducted in THF and other solvents, and the 1, 2, 4-oxadiazole compound is obtained; a series of target compounds are synthesized. The structure of the obtained compound is confirmed by NMR, the compound has clear and controllable hydrogen spectrum and fluorine spectrum signals, the synthesis process is simple, the raw materials are easy to obtain, the reaction condition is mild, the yield is good (most yield is more than 65%), and the developed 1, 2, 4-oxadiazole compound not only has clear structure and stable physicochemical properties, but also has wide application prospects. Good sterilization performance and structure regulation and control space are also shown, and high further research and development value is achieved.

The application provides a palladium ion extractant material and a preparation method thereof, and the pyridine-oxadiazole ligand is used as the extractant, most Pd 2+ in the aqueous phase can be extracted into the organic phase in a short time, and has a very high extraction rate; selective extraction separation of Pd 2+ under acidic conditions can be realized, the applicable range of acidity is wide, and excellent extraction capacity is achieved in the range of 0.2-4M nitric acid concentration; the extractant has excellent selectivity to Pd 2+ in the aqueous phase containing various metal ions; the pyridine-oxadiazole extractant has a good application prospect in the separation and recovery of Pd 2+ in high-level radioactive waste; the m-nitro-trifluorotoluene is used as a diluent of the extraction system, has good solubility to the organic ligand and the extractant, and the 2-bromohexanoic acid can increase the lipophilicity of the extractant.

N-[(S)-[3-[1-(2,2-difluoropropylcarbamoyl)-3-hydroxy-3-methyl- cyclobutyl]imidazo[1,2-b][1,2,4]triazin-6-yl]-[4-(trifluoromethyl)cyclohexyl]methyl]-4-5 methyl-1,2,5-oxadiazole-3-carboxamide, or a pharmaceutically acceptable salt and / or solvate thereof, being a potent modulator of human IL-17 activity, is accordingly of benefit in the treatment and / or prevention of various human ailments, including inflammatory and autoimmune disorders.

Embodiments of the present disclosure are directed towards spray-dried compositions including a Zr phenol-oxadiazole complex and methods utilizing these spray-dried compositions.

The present application relates to a kind of 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative purposes, 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative structure as shown in formula I, this 3-(2H-benzopyran-3-yl)-5-phenyl-1,2,4-oxadiazole derivative has the potential to be developed as anti-radiation drug and antitumor drug.

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 application discloses a preparation method and product of a myrtenyl-1,3,4-oxadiazole formylhydrazine compound and application of the compound, and synthesizes myrtenic acid by oxidizing myrtenal; myrtenyl hydrazine is generated by reacting the myrtenic acid with hydrazine hydrate; myrtenyl-1,3,4-oxadiazole methyl ester is generated by reacting the myrtenyl hydrazine with oxalyl chloride methyl ester; the myrtenyl-1,3,4-oxadiazole formylhydrazine compound is generated by reacting the myrtenyl-1,3,4-oxadiazole methyl ester with each substituted phenylhydrazine; the compound has a general formula I: wherein R is H, 4-F, 4-Cl, 4-Br, 4-I, 4-CH3, 2-CH3, 2-F, 3-F, 2-Cl, 3-Cl, 2-Br, 3-Br or 4-OCH3; the compound has good prevention effects on sclerotinia sclerotiorum, botryosphaeria dothidea and fusarium graminearum under an in-vitro condition, and can be used for preventing and treating fungal diseases of agricultural or forestry plants. The preparation method of the compound is simple, the yield is high, and the product is stable in property.

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.

N-[(S)-(4, 4-difluorocyclohexyl) {3-[1-(2, 2-difluoropropylcarbamoyl)-3-hydroxy-3-methylcyclobutyl] imidazo [1, 2-b] [1, 2, 4] triazin-6-yl} methyl]-4-methyl-1, 2, 5-oxadiazole-3-carboxamide, or a pharmaceutically acceptable salt thereof, is a potent modulator of human IL-17 activity, and is therefore of benefit in the treatment and / or prevention of a variety of human diseases, such as, for example, human IL-17. Inflammatory and autoimmune disorders are included.

This invention belongs to the field of polymer material modification. Addressing the problem of unifying the functionality and mechanical properties of existing nylon, this invention provides a flame-retardant, antistatic, and high-temperature resistant nylon and its preparation method. The method includes the following steps: Under a protective atmosphere, 2,5-bis(4-aminophenyl)oxadiazole, a diamine, a diacid, a flame-retardant monomer, an antistatic agent, a catalyst, an antioxidant, and water are mixed and subjected to a pre-condensation reaction; then, a condensation reaction is carried out to obtain the flame-retardant, antistatic, and high-temperature resistant nylon. The nylon prepared by this method has the characteristics of high molecular weight, high temperature resistance, antistatic properties, and mechanical properties comparable to unmodified nylon. Furthermore, this method is simple to operate, easy to control, and readily achievable for large-scale production.

The invention discloses a [1, 2, 5] oxadiazole-bis [1, 2, 4] triazole explosive, which is N3, N4 bis (5-nitro-1H-1, 2, 4-triazole-3-yl)-1, 2, 5-oxadiazole-3, 4-diamine, and a preparation method of the [1, 2, 5] oxadiazole-bis [1, 2, 4] triazole explosive. The invention also discloses a preparation method of the [1, 2, 5] oxadiazole-bis [1, 2, 4] triazole explosive. The invention discloses a [1, 2, 5] oxadiazole-[1, 2, 4] triazole explosive with high-energy low-sensitivity flexible imino characteristics, which is structurally characterized in that a five-membered azole ring ([1, 2, 5] oxadiazole and [1, 2, 4] triazole) is used as a basic skeleton, a flexible imino group is used as a bridging center, and an amino group and a nitro group are used as substituent groups. The invention provides a synthesis method of the compound. The compound disclosed by the invention has the characteristics of high energy, low sensitivity, excellent detonation performance, simple synthesis method and the like, and has application potential in the aspect of linked ring explosives.

The invention relates to the field of organic synthesis, in particular to equipment and a method for preparing fluorine-containing oxadiazole. The equipment is a rotary evaporator, a hollow pipe, used for steam circulation, of the rotary evaporator is connected with an evaporation bottle, the hollow pipe rotates to drive the evaporation bottle to rotate, and the evaporation bottle is partially arranged in a water bath kettle; a bottle retreating mechanism is arranged on the rotary evaporator and can drive the evaporation bottle to rotate and push the evaporation bottle to move in the axis direction of the hollow pipe. According to the rotary evaporation device, the evaporation bottle can be rapidly fixed in the mode that the rotating ring b extrudes the rotating frame, follow-up rotary evaporation work can be conveniently carried out, after rotary evaporation is finished, the seizure state of the evaporation bottle can be rapidly broken through the bottle retreating mechanism, in the whole operation process, an operator does not need to hold the evaporation bottle to forcefully rotate and pull the evaporation bottle, and operation is convenient. The evaporation flask can be indirectly protected only by rotating the rotating deflector rod a and the rotating deflector rod b, so that the operation is more labor-saving, and collision between the evaporation flask and the water bath kettle due to overexertion is avoided.

Disclosed is an application of a compound based on a 3-phenyl-1,2,4-oxadiazole-5-carboxamide scaffold in the preparation of a drug for treating tumor diseases. The compound of the 3-phenyl-1,2,4-oxadiazole-5-carboxamide scaffold regulates the level of Cofilin1 palmitoylation modification by inhibiting the activity of PPT2, and finally achieves an anticancer effect.

The invention discloses a nylon composite material with high performance, high weather resistance and good appearance and a preparation method thereof, and belongs to the technical field of polymer composite materials. A functional metal organic framework layer is constructed on the surface of glass fiber, Zr < 4 + > ions and a 2, 5-bis (2-carboxyphenyl)-1, 3, 4-oxadiazole ligand form a three-dimensional network structure, Ce ions are doped, and a slow-release benzotriazole corrosion inhibitor is loaded. The composite material is prepared from 20 to 60 parts of PA6, 15 to 45 parts of modified glass fiber, 1 to 5 parts of titanium dioxide, 0.3 to 1 part of a light stabilizer, 0.3 to 1 part of a pH regulator, 0.3 to 1 part of a coupling agent, 0.2 to 0.9 part of an antioxidant and 0.3 to 1 part of a lubricant. The color difference of the material is only 0.8 after a xenon lamp is aged for 500 hours, the tensile strength retention rate reaches 85%, the tensile strength retention rate reaches 82% after the material is subjected to damp-heat aging for 1000 hours, and the phenomenon of floating fibers on the appearance is eliminated.

The application discloses a method for synthesizing 1,3,4-oxadiazole compounds from 1,2-dihydrazide compounds, and the specific implementation process is as follows: taking 1,2-dihydrazide compounds as shown in formula (I) as raw materials, adding alkali and a solvent into a reactor in sequence, and reacting in the atmosphere of a cyclization agent gas SO2F2, and after the reaction is completed, post-treatment is carried out to obtain 1,3,4-oxadiazole compounds as shown in formula (II), and the reaction process is as follows: in the formula, the substituent R1 on the benzene ring is substituted or not substituted, when the substituent R1 is substituted, the substituent R1 is fluorine, chlorine, bromine, a methyl group or a methoxy group, and the substituent R2 is a methyl group, an isopropyl group, a tert-butyl group or a phenyl group. The application has mild reaction conditions, uses a cheap and easily obtained cyclization agent, and efficiently promotes the preparation of 1,3,4-oxadiazole compounds.

The application discloses a method for identifying Fe by using 2-amino-5-substituted-1, 3, 4-oxadiazole. 3+ The method comprises the following steps: firstly, preparing a 2-amino-5-substituted-1, 3, 4-oxadiazole solution to be detected; secondly, adding a metal cation solution into the solution to be detected; and thirdly, identifying Fe by naked eye observation and ultraviolet-visible absorption spectrum. 3+ The method has good selectivity for Fe 3+ , is not interfered by other ions, and can better identify and detect Fe in the environment. 3+ ​

Oxadiazole antibiotics that exhibit bactericidal activity against C. difficile vegetative cells. We screened a library of 75 oxadiazoles against C. difficile ATCC 43255. The findings from this collection served as the basis for the syntheses of an additional 58 analogs, which were tested against the same strain. We discovered a potent (MIC50=0.5 μg / mL, MIC90=1 μg / mL for 101 C. difficile strains) and narrow-spectrum oxadiazole (3-(4-(cyclopentyloxy)phenyl)-5-(4-nitro-1H-imidazol-2-yl)-1,2,4-oxadiazole; compound 57) that is not active against common gut bacteria or other tested organisms, but is selectively bactericidal against C. difficile and targets cell-wall synthesis. Other similarly effective oxadiazole antibiotics of formula I and II are described herein, several of which inhibit or prevent C. difficile spore germination.

The invention discloses a multi-azido substituted biheterocyclic energetic compound which has high nitrogen content, and multiple properties of the compound are superior to those of a traditional initiating explosive lead azide. The invention also provides a synthesis method of the multi-azido substituted biheterocyclic energetic compound, which comprises the following steps: by taking 1, 2, 5-oxadiazole-3, 4-diamine as an initial raw material, carrying out three-step reaction of oxidation, chlorination and azidation to obtain the energetic compound. The synthesis method has the advantages of easily available raw materials, simplicity and convenience in operation, high total yield and the like.

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.