198 results about "Oxazole" patented technology

The invention relates to the technical field of microbial treatment of antibiotic pollution, and discloses an antibiotic degrading bacterium with salt tolerance and capable of degrading sulfamethoxazole at low temperature and application, the strain degrades SMX in a wide temperature range of 10-40 DEG C, the degradation rate of 20mg / L SMX at 10-35 DEG C within 64 hours is greater than 70%, and the degradation rate of 20mg / L SMX at 20-30 DEG C reaches 100%; at the low temperature of 10 DEG C, low-concentration SMX is obviously degraded, and the SMX with the concentration of 5 mg / L can be completely degraded within 16 hours; the MJ2 can still effectively degrade SMX under the harsh conditions that the temperature is low and SMX serves as the unique carbon and nitrogen source, the degradation rate reaches 100% after 66h at the concentration of 5 mg / L, and it is proved that the MJ2 has the unique oligotrophic adaptability. Salinity tests show that the degradation rate of MJ2 to 20 mg / L SMX within 48 hours under the 0.1-2% NaCl concentration is 100%, the degradation rate is still kept at 50% even under the stress of 3% high salt, and remarkable salt tolerance is also shown. In conclusion, the strain MJ2 integrates wide temperature range adaptability, low-temperature high efficiency, oligotrophic tolerance and high salt stability, and has great application value in sulfonamide antibiotic pollution remediation in a complex environment.

The invention discloses a preparation method of 3-chloro-5, 5-dimethyl-4, 5-dihydroisoxazole, which comprises the following steps: taking a hydroxylamine oxygen sulfonic acid aqueous solution and isopentenal as raw materials, carrying out oximation reaction in an organic solvent under an alkaline condition, then directly adding an acid or an organic base catalyst into the reaction system, and reacting for 2-4 hours to obtain 3-chloro-5, 5-dimethyl-4, 5-dihydroisoxazole, thereby obtaining the 3-chloro-5, 5-dimethyl-4, 5-dihydroisoxazole. Under the catalytic action of the catalyst, a cyclization reaction is carried out, after the reaction is finished, an intermediate solution containing 5, 5-dimethyl-4, 5-dihydroisoxazole is obtained, and the next step is directly carried out; and carrying out a chlorination reaction by taking the intermediate solution as a raw material and sodium hypochloride or chlorine as a chlorination reagent, and after the reaction is finished, carrying out post-treatment to obtain the 3-chloro-5, 5-dimethyl-4, 5-dihydroisoxazole. The hydroxylamine oxygen sulfonic acid is used for enabling the isopentenal to be subjected to oximation reaction under the alkaline condition, then cyclization is carried out under the catalytic action of acid or alkali, the 5, 5-dimethyl-4, 5-dihydroisoxazole is generated, and the process has the advantages that the yield is high, the production steps are simplified, and the production cost is reduced.

The invention belongs to the technical field of organic synthesis, and particularly relates to a synthesis method of an isoxazole compound under a visible light catalysis condition. The method comprises the following steps: dissolving a compound 1 in 1, 2-dichloroethane, then adding tert-butyl nitrite, tribromomethane, alkali and a photocatalyst, in an inert gas environment, irradiating with visible light and stirring at room temperature to react, after the reaction is completed, reducing pressure to remove a solvent, and then performing silica gel column purification on a crude product to obtain a product, namely the isoxazole compound. The brand-new method for preparing the isoxazole compound through visible light catalysis is developed, the conditions of high temperature and high pressure in a traditional synthesis method are avoided, energy consumption and environmental pollution are remarkably reduced, and the yield of the isoxazole compound is effectively increased by regulating and controlling reaction conditions and optimizing raw material selection and proportion.

The invention discloses a synthesis method of an oxazole derivative, and belongs to the technical field of chemical synthesis. The oxazole derivative is synthesized from a ketone ester compound and thiourea through a one-pot method, the required raw materials are cheap and easy to obtain, the experimental operation is simple, the reaction condition is mild, a metal catalyst and other reagents are not needed, and the defects that a metal catalysis synthesis method is used, for example, the catalyst is high in price, the reaction synthesis route steps are many, and the synthesis cost is low are overcome. The method has the advantages of mild reaction conditions, low reaction rate, unstable intermediate, low yield and the like, bypasses most complex synthesis steps of a metal-free catalytic synthesis method, and develops a simple, efficient, green and environment-friendly way for synthesizing the oxazole derivative. Under mild conditions, ketone ester substrates with different substituent groups have very strong compatibility, and a new green synthesis way is provided for synthesis of substituted oxazole.

The invention discloses a blended neutron / gamma discrimination polysiloxane scintillator and a preparation method thereof. The polysiloxane scintillator is composed of a matrix, a primary fluorescent dye, a secondary fluorescent dye and a cross-linking agent. A matrix of the scintillator is a copolymer of methyl phenyl polysiloxane and phenyl methyl siloxane, a main fluorescent dye is 2, 5-diphenyl oxazole (PPO), a secondary fluorescent dye is selected from 7-diethylamino-4-methylcoumarin (MDAC), and a cross-linking agent is 1, 3-divinyl-1, 3-diphenyl-1, 3-dimethyl siloxane. The obtained polysiloxane scintillator has good stability and can be used for neutron detection and neutron / gamma discrimination in a strong irradiation field environment.

The application provides a synthesis process of metrafenone, in which inorganic alkali KOH is used as a catalyst, a key intermediate 4-(((5,5-dimethyl-dihydroisoxazole-4-yl)thio)methyl)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-ol can be obtained at low production cost and high yield, metrafenone is prepared through substitution reaction and oxidation reaction, the reaction yield is high, raw materials are simple and easy to obtain, three-waste emissions are small, and the process is beneficial to industrial mass production.

The application discloses a thiazole / oxazole group-containing 1,2,4-triazole derivative, a preparation method and application thereof, and relates to the technical field of medicinal chemistry.The thiazole / oxazole group-containing 1,2,4-triazole derivative has excellent broad-spectrum antifungal effect and the advantage of a simple synthesis method, and has important reference significance for developing a novel high-efficiency antiplant pathogenic fungus agent.

The invention belongs to the field of medicinal chemistry, and relates to an indole allylamine amide derivative as well as a preparation method and application thereof. Functional activity screening of G protein dependent signaling pathways is carried out on all the synthesized compounds, and it is found that the new derivatives can be used for preparing beta2-adrenergic receptor allosteric antagonism regulator drugs. Trans-indole allylamine is used as a raw material, amide coupling is performed to obtain the novel indole allylamine amide derivative, and R1 is any one of phenyl, m-methylbenzene, m-methoxyphenyl, m-bromophenyl, m-chlorphenyl, m-fluorophenyl, o-methoxyphenyl, p-methoxyphenyl, naphthalene ring, oxazole, cyclohexyl, cyclopentyl, methyl, ethyl and isopropyl. A biological activity test result shows that the indole allylamine amide derivative disclosed by the invention has relatively good antagonistic activity on beta2AR and can be used for carrying out negative allosteric regulation on the functional activity of isoproterenol.

The invention discloses a novel styrene-acrylonitrile neutron / gamma discrimination plastic scintillator and a preparation method and application thereof. The plastic scintillator is composed of a mixed matrix, a main fluorescent dye and a secondary fluorescent dye, the mixed matrix is styrene-acrylonitrile (ABN), the main fluorescent dye is 2, 5-diphenyl oxazole (PPO), and the secondary fluorescent dye is 9, 10-diphenyl anthracene (DPA). The prepared plastic scintillator uses the mixed matrix, the traditional scintillator usually focuses on the influence of the matching of primary and secondary fluorescent dyes on the plastic scintillator, which is only in the transfer direction of debugging matrix excitation energy, and the innovation of the double mixed matrix can explore another way and expand thinking for researching how to improve the light yield of the plastic scintillator. Meanwhile, the addition of acrylonitrile improves the transparency and hardness of the plastic scintillator, and the stability is also greatly improved.

The utility model discloses a production system of 1-cyclopropyl-3-(2-methylthio-4-trifluoromethylphenyl) propyl-1, 3-diketone, which comprises an esterification unit and a condensation unit, and is characterized in that the esterification unit is connected with the condensation unit; the production system has the advantages that the production system is simple in connection structure and easy to implement, methyl 2-methylthio-4-trifluoromethyl benzoate is prepared from 2-methylthio-4-trifluoromethyl benzoic acid and the like through an esterification unit and then reacts with cyclopropyl ketone and other raw materials to prepare 1-cyclopropyl-3-(2-(methylthio)-4-(trifluoromethyl) phenyl) propyl-1, 3-diketone, and the production system has the advantages that the production system is simple in connection structure and easy to implement. The generation of three wastes is reduced, and the production cost is reduced; moreover, in the reaction process, the reaction temperature is not high, the reaction condition is mild, the yield is high, the production cost is low, the content of impurities in the product 1-cyclopropyl-3-(2-(methylthio)-4-(trifluoromethyl) phenyl) propyl-1, 3-diketone can be reduced, a high-quality reaction raw material is provided for subsequent industrial production of isoxaflutole, and the method is suitable for large-scale industrial production.

The invention discloses a benzoxphosphine ligand and a complex and application thereof. The structure of the benzoxphosphine ligand is shown as a formula (I), in the formula (I), R1 is alkyl or aryl substituted oxazolidinyl or imidazoline, R2 is alkyl and / or aryl, and R3 is at least one of fluorine, carbazolyl and 2, 6-dimethoxyphenyl. According to the benzoxphosphine ligand disclosed by the invention, the metal iridium complex can be used as a catalyst to be applied to an asymmetric hydrogenation reaction of alpha-phenyl vinyl diethyl phosphate, and has excellent activity and relatively high enantioselectivity; moreover, the benzoxphosphine ligand disclosed by the invention can be directly synthesized from simple and easily available chiral aldehyde, and the preparation method is simple and easy to operate.

Disclosed are an anthracycline compound, a preparation method therefor, an intermediate, and a use thereof. The present invention provides an anthracycline compound as shown in formula I or a pharmaceutically acceptable salt thereof. The anthracycline compound provided by the present invention has antitumor activity comparable to existing anthracycline drugs (such as nemorubicin) or greater than that of existing anthracycline drugs doxorubicin and daunorubicin, and does not form an oxazole ring structure during metabolism, thereby improving the clinical safety of such drugs.

One aspect of the present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is a phenyl group or a 5- or 6-membered heteroaryl group; Ring B is absent or is phenyl, pyridinyl, pyrazidinyl, pyrazinyl, pyrimidinyl, oxazolyl, isoxazolyl, thiadiazolyl, pyrazolyl, isothiazolyl or thiazolyl; Ring C is a fused bicyclic group of formula: (AA), wherein X1 to X9 form a substituted heteroaryl group containing at least one N and at least one NH; X-Y is -(CH2) m NR 21 CO; L is a direct bond or a linker group; Z is selected from alkyl, cycloalkyl, aryl, heteroaryl and heterocycloalkyl, each of which may be substituted; each R a and each R b is independently selected from alkyl, halo, haloalkyl, alkoxy, cycloalkoxy, haloalkoxy, cyano, NR 23 COR 25 、NR 24 -SO2R 26 、(CH2) q SR 27 、(CH2) q SOR 28 、(CH2) q SO2R 29 、SO2NR 30 R 31 、(CH2) q OH、(CH2) q OR 32 、NR 33 R 34 、CONR 35 R 36 、cycloalkyl and (CH q 2)-heterocycloalkyl; R 10 、R 11 、R 21 、R 22 、R 23 and R 24 are each independently selected from H and alkyl; R 12 ~R 20 、and R 25 ~R36 Each of the following is independently selected from H, alkyl, aralkyl, alkoxy, alkoxyalkyl, hydroxyalkyl, and cycloalkyl; each of m, n, and p is independently an integer from 0 to 4; and each of q is independently an integer from 0 to 4. Further aspects of the present invention relate to pharmaceutical compositions comprising the compounds according to the present invention and the use of the compounds in the treatment of various GPR35-related disorders. [Formula 1] TIFF2026510355000540.tif56170

The present application relates to the technical field of display, in particular to an organic compound and application thereof. The organic compound provided by the present application is connected with arylamine containing a benzoxazole structure by limiting the structure of the parent nucleus of formula (1), and the overall compound shows high stability and high hole transport performance by matching different substituent groups, the matching degree of HOMO and LUMO energy levels and adjacent energy levels is high, and then the carrier mobility of the organic compound with the specific structure is more balanced, so that the organic electroluminescent device containing the organic compound has low driving voltage, high luminous efficiency and long service life.

The invention discloses a self-repairing mute tire and a preparation method thereof, and relates to the technical field of tires, the self-repairing mute tire comprises a tire body, and a self-repairing rubber layer and a mute material which are sequentially attached to the inner wall of the tire body from inside to outside; the self-repairing adhesive layer is prepared from the following components: epichlorohydrin rubber, acrylate rubber, a rosinyl phenyl phosphine oxide isoxazolyl functional polymer, 4, 4-chloroformyl phenyl ether, a catalyst, 2, 2-bis [4-(4-aminophenoxy) phenyl]-1, 1, 1, 3, 3, 3-hexafluoropropane, trithiocyanuric acid, a filler, an accelerant TMTD (Tetramethylthiuram Disulfide) and an auxiliary agent; the rosinyl phenyl phosphine oxide isoxazolyl functional polymer comprises structural units introduced through a condensation polymerization reaction of the following monomers: glycerol triabietate, bis (4-carboxyl phenyl) phenyl phosphine oxide and 3, 5-isoxazoledicarboxylic acid. The tire is remarkable in self-repairing effect, good in mute performance, sufficient in performance stability and long in service life.

The application belongs to the technical field of microbial application, and specifically discloses application of roseofungin Streptomyces roseofunginus in plant disease prevention and treatment. The application finds that after R&M synthesis genes in roseofungin Streptomyces roseofunginus are knocked out, the strain can still synthesize oxazolomycin A. Further finding is that oxazolomycin A shows good inhibitory effect on pepper Phytophthora capsici and Phytophthora sansomei, wherein the EC 50 value of pepper Phytophthora capsici PC35 is 2.95 μg / mL, and the EC 50 value of atractylodes Phytophthora sansomei AMPH-1 is 2.39 μg / mL. The oxazolomycin A prepared by the application can be developed into a biological pesticide that can effectively meet the agricultural development demand of "green ecology", and provides key biocontrol resource support for green prevention and control of plant diseases.

The present invention relates to benzoxazole and benzothiazole compounds or pharmaceutically acceptable salts thereof which are useful for the treatment of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (Exon19 deletion, L858R and the Del 19 / T790M and L858R / T790M resistance mutation). The compounds of the present invention and salts thereof are useful in the treatment or prevention of different types of cancers. The present invention also relates to methods of preparation for benzoxazole and benzothiazole compounds and pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof; a pharmaceutical composition containing the compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and / or solvates thereof particularly useful polymorphs of the compounds and salts thereof. The invention also relates to use of the compounds and pharmaceutically acceptable salts, prodrugs, stereoisomers, and solvates thereof in the preparation of a medicament for treating diseases associated with various forms of EGFR. The definitions of 'A', 'X', R1, R2, R3, and 'm' are as defined herein. Formula (I)

The invention discloses a preparation method of an azacyclo-bis (fluorosulfonyl) imide salt derivative, which comprises the following steps of: 1, mixing an azacyclo-compound, a methylation reagent, an ethylation reagent, bis (fluorosulfonyl) imide salt and inorganic alkali in a polar organic solvent, heating, and filtering after complete reaction to obtain crude filtrate containing the azacyclo-bis (fluorosulfonyl) imide salt; the nitrogen heterocyclic compound is selected from one of oxazolidine, 4-cyano piperidine, 4-fluoro piperidine, 4, 4-difluoro piperidine and 3-cyano piperidine; the bis (fluorosulfonyl) imide salt is selected from one of lithium bis (fluorosulfonyl) imide and potassium bis (fluorosulfonyl) imide; and 2, adding an inert organic solvent into the crude product filtrate for crystallization, and performing vacuum drying to obtain a finished product. The method has the advantages that the operation steps are few, the synthesis efficiency is greatly high, the process is greatly simplified, and the preparation cost is effectively reduced.

A novel preventive and / or therapeutic agent useful in the prevention and / or treatment of a disease whose symptom is alleviated or improved by the inhibition of myostatin. The present invention relates to an agent for preventing and / or treating a disease whose symptom is alleviated or improved by the inhibition of myostatin, the agent including a therapeutically effective dose of (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy]butyric acid, a salt thereof, or a solvate thereof.

The present invention relates to a 6-Aryl imidazo[2,1-b]thi / oxazole-2-carboxilic acid derivative, and the compound according to the present invention is useful as a JNK3 inhibitor capable of acting specifically against JNK3. The inhibitory activity of the compound according to the present invention against JNK3 is relatively higher than that against JNK1 and JNK2, and thus it can be used as an Alzheimer's disease therapeutic agent with a low risk of side effects.

The invention discloses a hydrogen phagocystis strain SNF1, which belongs to the field of wastewater treatment, the hydrogen phagocystis strain SNF1 is preserved in China General Microbiological Culture Collection Center (CGMCC), the preservation number is CGMCC No.35006, and the preservation date is June 25, 2025; the invention further discloses a fermentation compound, the fermentation compound is used for removing sulfamethoxazole in wastewater, and the compound comprises the hydrogen phagocystis strain SNF1 and microalgae; the invention further discloses a method for removing sulfamethoxazole in wastewater, and the hydrophage strain SNF1 is used in the method.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

The application provides a low-refractive-index cover layer material, which is a carbazolyl-oxazole derivative and benzene as a mother nucleus, and a plurality of steric groups and electron-withdrawing groups are introduced to regulate the packing density and electron density of the molecule to adjust the polarizability of the molecule, so as to obtain a low-refractive-index cover layer material with a chemical structure shown in formula 1. By matching the low-refractive-index cover layer material with a high-refractive-index material, the light interference effect can be utilized to further improve the light extraction efficiency of an organic electroluminescent device. The refractive index of the compounds in examples 1-155 is 1.411-1.519 in each color gamut, which is lower than the refractive index of the comparative examples Ref1-Ref11, and the extinction coefficient k value is almost 0 in each color gamut, which does not affect the light emission of the light-emitting layer. The device performance of the device examples 1-155 prepared by combining the compounds prepared in examples 1-155 with the high-refractive-index CPL is better than the device performance of the device prepared by only containing the high-refractive-index CPL.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

Described herein is a small molecule splicing modulator compound that modulates splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.

A composition including a fluorine-containing polymer, at least one carboxylic acid compound selected from a dicarboxylic acid compound having a specific structure and a monocarboxylic acid compound having a specific structure; and at least one cross-linking compounding agent selected from a primary amine compound, a secondary amine compound, an inorganic nitride, an organic tin compound, a peroxide cross-linking agent, a polyol cross-linking agent, a polyamine cross-linking agent, an oxazole cross-linking agent, an imidazole cross-linking agent, and a thiazole cross-linking agent. Also disclosed is a molded article obtained from the composition.

The invention discloses a chiral alpha-aryloxy benzoxazole acetate compound and a synthesis method thereof, and the chiral alpha-aryloxy benzoxazole acetate compound is an optically active compound with a structure as shown in the following formula I, and comprises a stereoisomer with the same chemical general formula. According to the method, a complex formed by a chiral ligand and metal is used as a catalyst, an electrochemical catalysis asymmetric aryloxylation reaction is used as a key step, and the target chiral compound is accurately and efficiently synthesized with high yield and high stereoselectivity. The preparation method is simple, reaction conditions are mild, atom economy is excellent, and the prepared chiral alpha-aryloxy benzoxazole acetate compound has good biological activity potential, can be widely applied to the field of drug intermediate synthesis and has remarkable biomedical practicability and industrial large-scale production prospects.

The application relates to a transition metal-catalyzed N-(1-arylvinyl)amide for constructing a fully substituted 5,5'-oxazole compound through a multiple cross-dehydrogenative coupling strategy. Specifically, under the condition of an inert solvent, through the joint promotion of a transition metal catalyst and a silver salt oxidant, multiple dehydrogenation 1,1-bifunctionalization of olefins is realized. The method has good regioselectivity and chemical selectivity. Notably, the application reports the first case of a transition metal-catalyzed simple construction of a fully substituted 5,5'-oxazole compound skeleton based on a multiple dehydrogenation cyclization strategy. The substrate of the conversion has a wide application range and strong functional group tolerance. The applicant also realizes the modification of drug molecules such as propyl sulfone. Further, the obtained 5,5'-oxazole molecules are subjected to fluorescence testing, and the fluorescence quantum yield reaches 83.14%, indicating that the novel skeleton has great application potential in luminescent materials.

The invention relates to the technical field of shoe materials, in particular to shoe material sponge applied to shoes easy to wear and take off and a preparation method of the shoe material sponge. The shoe material sponge is prepared from the following raw materials in parts by weight: 70 to 80 parts of polyether polyol, 10 to 17 parts of polyester polyol, 3 to 8 parts of a chain extender, 5 to 12 parts of thiolated nano silicon dioxide, 0.3 to 0.8 part of a Grubbs catalyst, 3 to 10 parts of self-repairing microcapsules, 1 to 3 parts of an oxazolidine crosslinking agent, 1 to 2.5 parts of a foaming agent, 0.05 to 0.2 part of a catalyst, 1 to 2 parts of a foam stabilizer and 40 to 60 parts of isocyanate. The core material of the self-repairing microcapsule is dicyclopentadiene; the method has the advantage that the fatigue resistance of the sponge for the shoe material is improved.

This invention provides a class of general-purpose chiral catalysts containing a cinchona primary amine arylformamide skeleton, along with their preparation methods and applications, belonging to the field of catalytic materials technology. The chiral catalysts provided by this invention link cinchona primary amine with oxazole / thiazole / imidazolium formamide structural units capable of coordination. Through the coordination of the oxazole / thiazole / imidazolium and amide coordinating groups with the central metal, they act as chiral ligands to catalyze a wider range of asymmetric reactions. They can also be used alone as chiral small-molecule catalysts for cinchona-like tertiary amine (thiourea) and square amides to catalyze asymmetric organic reactions. Furthermore, they can achieve synergistic (co-catalytic) catalysis of small molecules and metals in the same reaction system through different combinations. These chiral catalysts can be widely used as Lewis bases, Lewis acids, or small-molecule chiral catalysts and chiral ligands, possessing potential scientific and applied value in chiral sciences such as asymmetric catalysis, chiral synthesis, and chiral resolution.