13578 results about "Combinatorial chemistry" patented technology

The invention discloses a novel synthetic method for 5-phenyl tetrazole, which includes the following steps: firstly performing acid neutralization to hydrazine hydrate; then adding mixing solution formed by cyanobenzene, water and ethyl alcohol to generate phenyl aminoguanidine salt; adopting sodium nitrite for diazotization to obtain nitrine amidine under the acidic condition; obtaining 5-phenyl tetrazole crude product through closed loop under the alkaline condition; obtaining 5-phenyl tetrazole acceptable product through adopting ethyl alcohol for refining. The method has the advantages of simple technology, simplicity in operation and high product yield.

The application provides a process method for preparing (2-(3,6-dimethoxy-9H-carbazol-9-yl)ethyl) phosphonic acid, and particularly relates to the technical field of organic synthesis. The process method is that, under alkaline conditions, a halogenated phosphonate compound is added into a 3,6-dimethoxy-9H-carbazole solution to perform a reaction, hydrochloric acid aqueous solution is added after the reaction to perform acidolysis degreasing, and finally (2-(3,6-dimethoxy-9H-carbazol-9-yl)ethyl) phosphonic acid is obtained through extraction, reflux adsorption and beating purification. The process method uses 3,6-dimethoxy-9H-carbazole as a starting material, realizes the synthesis of the target product through one-pot reaction, has mild reaction conditions, uses non-toxic raw materials which are easy to obtain, has simple synthesis process, is convenient to operate, and has high separation yield.

The application discloses a compound and application thereof, and belongs to the technical field of biological pharmacy. The compound has a structure shown in formula (I), or a deuterium compound thereof, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. The compound has good PDE3 and / or PDE4 inhibiting effect, and is of great significance to the preparation of a medicine for PDE3 and / or PDE4 related diseases.

The present disclosure relates to compositions and methods for reversible fixation of biological samples using fixation reagents that form bis-carbamate crosslinks between amine-bearing moieties in biomolecules.

This invention relates to pharmaceutically acceptable tryptamine analogues and salts thereof. In particular, though not exclusively, the invention relates to formulations and uses of the same as a medicament.

The invention discloses a cyclic nonapeptide with repairing and anti-oxidation effects and application of the cyclic nonapeptide, the amino acid sequence of the cyclic nonapeptide is cyclic (arginine-glycine-aspartic acid-serine-arginine-lysine-valine-lysine-serine), the prepared cyclic nonapeptide has the repairing and anti-oxidation effects, and the cyclic nonapeptide has the repairing and anti-oxidation effects. The composition can be applied to preparation of cosmetics with repairing and / or anti-oxidation effects.

The invention discloses a method for synthesizing electronic-grade ethyl acetate through catalytic esterification of acidic ion exchange resin, and belongs to the technical field of ethyl acetate preparation. The method comprises the following steps: mixing crosslinked polystyrene white balls and a swelling agent, and dropwise adding concentrated sulfuric acid for reaction to obtain S-PS resin; mixing an EDTA disodium salt saturated solution and a polyacrylic acid solution, adding a cross-linking agent and an emulsifier, and carrying out a cross-linking curing reaction to obtain EDTA microcapsules; the preparation method comprises the following steps: dispersing S-PS resin in a solvent, adding EDTA microcapsules, a dehydration condensation agent and a catalyst, reacting under the protection of inert gas, and filtering and recovering after the reaction is finished to obtain S-PS-EDTA resin; mixing glacial acetic acid, absolute ethyl alcohol and S-PS (at) EDTA resin for reaction, and filtering and collecting liquid after the reaction is finished; and rectifying the collected liquid to obtain the product. According to the method provided by the invention, metal impurities can be chelated in the synthesis process, and the electronic-grade ethyl acetate with high purity and low impurity content is produced.

The invention discloses a dual-mechanism antibacterial photosensitizer as well as a preparation method and application thereof, and relates to the technical field of biomedical photoelectric functional materials. The invention relates to a triphenylamine derivative, which can realize fluorescence imaging of bacterial or fungal infection by utilizing fluorescence characteristics, can generate active oxygen under illumination to play a photodynamic therapy role, is suitable for preparing photodynamic therapy preparations and developing antibacterial materials, and can also be applied to the fields of environment and public health and tumor treatment. The problems that an existing photosensitizer is insufficient in broad spectrum, different in fungus drug resistance mechanism, limited in single treatment effect and the like can be effectively solved, and the photosensitizer has wide application prospects.

The invention provides a catalyst, a preparation method and application thereof, and a method for preparing primary amine by catalyzing nitrile compound hydrogenation, and particularly relates to the technical field of catalyst synthesis. The catalyst comprises a nickel / cobalt-based catalyst and a metal salt; wherein the nickel / cobalt-based catalyst is selected from any one of a supported nickel / cobalt-based catalyst, a Raney nickel / cobalt catalyst or a nickel / cobalt nanocrystal; the metal salt comprises any one or a combination of at least two of tungsten salt, molybdenum salt, vanadium salt, aluminum salt and cerium salt. The metal salt and the nickel / cobalt main catalyst have a synergistic effect: the surface electron density is adjusted through electron transfer, the hydrogen dissociation and cyano adsorption activation capacities are enhanced, the hydrogenation activity is improved, and the mild condition reaction is assisted; the surface chemical environment is changed or steric hindrance is borrowed, the primary amine selectivity is improved, and byproducts are inhibited; aluminum salt, cerium salt and the like inhibit nickel / cobalt agglomeration, increase active sites, enhance stability, prolong the service life and reduce the dosage.

The invention relates to the field of organic chemical synthesis, in particular to a synthetic method and application of pyrimidone compounds. The invention provides a synthesis method, reactants are o-amino heterocyclic formamide and triethyl orthoformate respectively, a solvent system is a hexafluoroisopropanol solvent, and a product is a heterocyclic pyrimidone compound. The reaction does not need strong acid or strong alkali conditions, does not need additional reducing agents or oxidizing agents, does not need transition metal catalysis, is economical and practical, the reaction conditions are relatively mild, and the synthesized pyrimidone compound has a good antibacterial effect.

The invention provides a substituted amino bipyridine derivative as well as a preparation method and application thereof, the structure of the substituted amino bipyridine derivative is as shown in formula I. In the formula, R1, R2, R3 and R4 are independently selected from any one of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C20 alkynyl, C3-C6 cycloalkyl, C5-C20 aryl or C5-C20 heterocyclic radical; when R1, R2, R3 and R4 are not methyl, no more than one of R1, R2, R3 and R4 is H; and when any one of R1, R2, R3 and R4 is methyl, the rest groups are independently selected from H or methyl. When the substituted amino dipyridyl derivative provided by the invention is used as a blue dye, the dyed blue dye is bright in color, deep in dyeing and comprehensive in dyeing fastness; the preparation process is simple, convenient to purify, safe, simple, convenient and energy-saving, the product quality is stable, the reproducibility is good, the yield is high, and the method is suitable for industrial production.

Provided are an antibacterial peptide and the use thereof. The antibacterial peptide has a structure represented by formula (I), wherein Z1 is selected from tetrapeptides, the tetrapeptides being optionally modified by -OH, -CHO, -COOH, -NH2, -SO3H or -C=O; S1 and S2 are each independently selected from amino acids having the structure of (I); Q1 and Q2 are each independently selected from dipeptides or tripeptides; and n is independently selected from any integer between 1 and 6. (Q2)4-(S2-Q1)2-S1-Z1

The invention discloses a temperature-sensitive hydrogel based on Chinese prickly ash alkaloid. The temperature-sensitive hydrogel is prepared from poloxamer 407, poloxamer 188 and Chinese prickly ash alkaloid powder. The temperature-sensitive hydrogel based on the pepper alkaloid prepared by the invention has three characteristics of biological adhesion, self-healing property and slow release property, and solves the technical problems that the pepper alkaloid is poor in stability and uncontrollable in drug release.

The invention discloses an omariglitazone intermediate as well as a synthesis method and application thereof, and belongs to the technical field of pharmaceutical chemistry synthesis. The invention provides a synthesis method of an omarigliflozin intermediate and application of the intermediate in synthesis of omarigliflozin. The key of the synthesis method provided by the invention lies in the deprotection process of polycyclic indole amide, nitrile groups are not hydrolyzed, indole carboxylic acid is generated with high selectivity, molecular lactamization is avoided in the condensation process with polycyclic imine B, and expensive amidation reagents such as HATU are not needed in the process, so that the synthesis method is simple and easy to implement. And the purpose of preparing omariglitazone with low cost and high yield is achieved. The synthesis method has the advantages of easily available raw materials, mild reaction conditions, small side reaction influence, simplicity and convenience in operation and high yield, improves the yield, is easy to purify, and is suitable for industrial production of omariglitazone.

Provided in the present invention are compounds as VAV1 degradation agents and the use thereof. Specifically provided are compounds represented by formula (II), and tautomers, stereoisomers, pharmaceutically acceptable salts or prodrugs thereof. The compounds provided by the present invention have good efficacy, and can be used for preparing drugs for treating or preventing VAV1-related diseases.

The invention relates to the field of organic synthesis, in particular to a synthetic method of 1-(2, 6, 6-trimethyl-1, 3-cyclohexadiene-1-yl) ethanone, and particularly relates to a synthetic method of 1-(2, 6, 6-trimethyl-1, 3-cyclohexadiene-1-yl) ethanone by taking 4-acetyl-3, 5, 5-trimethylcyclohexene as a raw material and carrying out bromination and elimination steps to synthesize the 1-(2, 6, 6-trimethyl-1, 3-cyclohexadiene-1-yl) ethanone. The method has the advantages of easily available raw materials and high reaction yield, and can be industrially implemented on a large scale.

The invention discloses a preparation method of 5-hydroxy-3-iminopyridine-2, 6-diketone, and relates to the technical field of compound preparation. The invention provides a preparation method of 5-hydroxy-3-iminopyridine-2, 6-diketone, which comprises the following steps: uniformly mixing observation blue with at least one oxidant of sodium hypochlorite, potassium permanganate and hydrogen peroxide according to a molar ratio of 1: (0.5-1.5) under a solution condition, reacting for 5-120 minutes, and adding a reducing agent to finish the reaction, thereby obtaining a target product. According to the preparation method provided by the invention, on the basis of the amide structure of the ornamental blue, 'endogenous catalysis' of the reaction can be realized, no additional catalyst needs to be introduced, and the 5-hydroxy-3-iminopyridine-2, 6-diketone with the yield of more than 60.53% and the purity of more than 60.2% can be prepared through a simple and convenient one-step reaction.

The invention discloses a mucosal epithelial cell targeted oral ROS response type nano-enzyme as well as a preparation method and application thereof, and relates to the technical field of biological medicines. The oral ROS response type nano-enzyme comprises Ce-CDs carbon dots and a betaine polymer, and the betaine polymer is coated on the surfaces of the Ce-CDs carbon dots to form nano-particles; the Ce-CCDs carbon dots are prepared by taking a metal cerium source and chlorogenic acid as raw materials through a pyrolysis method. Through structural innovation and function integration, the prepared nano-enzyme shows outstanding advantages in the aspects of catalytic activity, targeted delivery, collaborative treatment, industrial application and the like, a new technical scheme is provided for efficient and safe treatment of inflammatory bowel diseases, and the nano-enzyme has remarkable technical innovation and clinical application value.

Disclosed in the present invention is a novel substituted heterocyclic compound having VAV1 target degradation activity. Specifically disclosed is a compound serving as a VAV1 target degradation agent and having the structure of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, isotopic substituent or isomer of the compound. The compound can be used for preventing or treating diseases related to VAV1 targets or signaling pathways.

The invention discloses a DNA synthesis method which comprises the following steps: processing an initial substrate according to a preset strategy to obtain a target substrate with a Mark pattern and a plurality of reaction sites, and adjusting the positions of the target substrate and an ink-jet printing device through the Mark pattern, so that the working directions of a reaction unit array and the device are consistent, and the subsequent operation accuracy is ensured; deprotecting the reaction sites to generate active groups; sequentially spraying a target monomer solution and an activator solution into the reaction sites of the preset area after deprotection treatment through an ink-jet printing device, and carrying out a coupling reaction with the active groups to obtain a mixed solution containing a nucleotide chain; carrying out cleaning, oxidation, capping and deprotection treatment on the mixed solution to obtain a single-layer base product; according to the target base sequence, determining a corresponding target monomer solution, and circularly carrying out a reaction to obtain a mixed solution containing a nucleotide chain; and obtaining the synthesized DNA according to the mixed solution. According to the method, high-throughput, high-quality and high-efficiency DNA synthesis can be realized.

This invention relates to the field of pharmaceutical technology, specifically to a substituted pyridotriazole compound, its preparation method, and its uses. This specification discloses a substituted pyridotriazole compound that inhibits RIPK1 and / or MLK, as well as its pharmaceutically acceptable salts, stereoisomers, solvent compounds, or prodrugs. The compound is shown in formula (I), where the definitions of each group are detailed in the specification. Furthermore, this invention also discloses pharmaceutical compositions comprising this compound and their use in the preparation of medicaments for treating RIPK1-related diseases or conditions.

The invention discloses an AIE imitated antibacterial peptide material and a preparation method and application thereof, and belongs to the technical field of polymer materials, the AIE imitated antibacterial peptide material takes an alkyl chain as a main chain, the position of a cation primitive is regulated, and AIE primitives with different D-A structures are combined as side chains, so that the AIE imitated antibacterial peptide material is prepared. Through the D-A structure in the AIE element, the molecular can be used for the performance regulation and control of generating ROS or photo-thermal through illumination response, so that the growth and proliferation of microorganisms can be inhibited, and the damage to a biofilm is further inhibited. The AIE imitated antibacterial peptide material is good in biocompatibility and has a wide application prospect in the field of antibacterial agents.

The invention relates to application of a heterocyclic compound as a fluorescent probe. The structural formula of the heterocyclic compound is shown as a general formula I, and R1, R2, R3, R4, R5, R6, R7 and R8 are independently one of hydrogen, alkyl, hydroxyl, phenyl, hydroxyphenyl, indole and oxymethyl. According to the present invention, the heterocyclic compounds represented by the general formula I can be specifically positioned in mitochondria, and have long fluorescence lifetime, such that the heterocyclic compounds are suitable for being used as mitochondria fluorescence probes.

The present disclosure relates to a polycyclic compound, a preparation method therefor, and the pharmaceutical use thereof. Specifically, the present disclosure relates to a polycyclic compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and the use thereof as a therapeutic agent, in particular, the use as an RAS inhibitor and the use in the preparation of a drug for treating and / or preventing RAS-mediated or dependent diseases or conditions, wherein each group in general formula (I) is as defined in the description.

The invention discloses a compound as shown in a formula (I), and / or pharmaceutically acceptable salts thereof, and / or a raceme mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, and belongs to the technical field of medicines. The invention also discloses a pharmaceutical composition containing the compound as shown in the formula (I), and the compound as shown in the formula (I) and / or a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof, and / or the pharmaceutical composition, a pharmaceutically acceptable salt thereof, and / or a racemic mixture, a hydrate, a solvate, a prodrug, an enantiomer, a diastereoisomer and a tautomer thereof. The invention further discloses application of the cGAS agonist in preparation of the cGAS agonist and a medicament for treating diseases responding to activation of the cGAS-STING signal channel.

The invention discloses a phenanthridine-6-formaldehyde derivative and a preparation method and application thereof.The preparation method comprises the steps that 2, 4, 5, 6-tetra (9-carbazolyl)-isophthalonitrile serves as a photocatalyst, 1-azabicyclo [2.2. 2] octane serves as a hydrogen atom transfer catalyst, a biphenyl isocyanide compound, the photocatalyst, the hydrogen atom transfer catalyst and an alkali additive are jointly dissolved in 1, 3-dioxolane, the mixture is stirred to be uniform, and the phenanthridine-6-formaldehyde derivative is obtained. And carrying out free radical tandem cyclization and acid-catalyzed hydrolysis reaction to obtain the phenanthridine-6-formaldehyde derivative. The invention also provides a specific reaction equation. According to the developed synthesis method of the phenanthridine-6-formaldehyde derivative, the compound can be efficiently and conveniently prepared, the technical bottlenecks of harsh reaction conditions and tedious steps in a traditional process are successfully overcome, raw materials which are low in price and easy to obtain are adopted, operation is carried out under mild conditions, the synthesis method has the outstanding advantages of being high in yield, safe and simple to operate, environmentally friendly and the like, and the method is suitable for industrial production. Good industrial application potential is shown.

The present invention relates to a heterocyclic compound capable of inhibiting IL-17A, a preparation method therefor, an intermediate, and a use thereof. In particular, the present invention relates to the compound shown in general formula (I), a preparation method therefor, an intermediate, a pharmaceutical composition including the compound shown in general formula (I), and a use of the compound shown in general formula (I) or the pharmaceutical composition thereof in preparing a drug which treats / prevents IL-17A-mediated diseases. The substituents in general formula (I) have the same definitions as in the description.