236 results about "Pyridyne" patented technology

The present application relates to a kind of five-ring thiazole indole ketone piperazine amide derivatives and purposes thereof.The derivatives take ethyl cyanoacetate as starting material, generate hydroxylamine compound (A) under the action of sodium nitrite and phosphoric acid;Obtain 2-amino ethyl cyanoacetate (B) by reduction, in turn with acetic anhydride, lawson reagent is reacted, and 5-amino-4-carboxylate thiazole compound (D) is obtained;After bromination by NBS, under the catalysis of phosphorus oxychloride, react with tetrahydropyridine indole ketone, generate 2-bromo-6,7-dihydrothiazolo [5'',4'':4',5'] pyrimido [1',2':1,2] pyrindo [3,4-b] indole-4 (12H) -ketone (F), again under alkaline condition, first with Boc piperazine, then by Boc treatment and obtain compound (H);Finally, react with acyl chloride, and 28 different substitution structures of five-ring thiazole indole ketone piperazine amide compound (I1-I28) are synthesized.The 28 compounds are tested on three kinds of cancer cells, and the results show that: 28 compounds have significant inhibitory activity on Hela cervical cancer cells, HT-29 human colon cancer cells and HGC-27 human gastric cancer cells.

The present disclosure relates to solid state forms of Compound (1) freebase. The present disclosure also relates to processes for the preparation of the solid state forms, the pharmaceutical compositions comprising the forms, and the use thereof, e.g., in the treatment and prevention of disorders in which NLRP3 activity is implicated.

This invention discloses a method for preparing sulfonamide-modified benzo[a]fluorene-5-one derivatives, using 1,7-enyne and N Using sulfonylaminopyridine salts as raw materials, a series of sulfonated benzo[a]fluorene-5-one compounds were successfully synthesized by catalyzing the sulfonation / cyclization tandem reaction of 1,7-enynes under photocatalytic conditions. This method has excellent functional group tolerance and high economic applicability.

Provided herein are methods for preparing crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate.

The present disclosure provides certain bifunctional compounds that cause degradation of Cyclin-dependent kinase 2 (CDK2) via ubiquitin proteasome pathway and are therefore useful for the treatment of diseases mediated by CDK2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

This utility model relates to the field of reaction vessel technology, specifically to a multi-stage tail gas absorption and anti-clogging reaction vessel for the synthesis of pyridine intermediates. It includes a reaction vessel with a stirring shaft inserted inside. Multiple through-grooves in a ring structure are formed on the inner wall of the reaction vessel, and a filter membrane is disposed inside each through-grooves. It also includes a mounting plate fixedly installed inside the reaction vessel, and a movable component movably connected to the lower end of the reaction vessel, with multiple discharge grooves on the movable component. Through the mounting plate inside the reaction vessel, and the communication between the ring grooves and through-grooves within the mounting plate, effective exhaust gas discharge can be achieved. Furthermore, the rubber layer located on the upper side of the mounting plate and the movable component ensure stable discharge and guarantee synthesis efficiency.

The application discloses application of a pyrimidinotriazine diketone derivative in preparation of a medicine for inhibiting activity of human protease caspase-1, and belongs to the technical field of medicines. In view of defects of existing caspase-1 inhibitors, the compound has the characteristics of high affinity binding to caspase-1 (K D = 8.11 μM; 8.78 μM) and strong inhibition on the activity (IC 50 = 11.90 nM-14.47 nM). The compound is used for preparation of a medicine for inhibiting the activity of caspase-1 and a medicine for treating inflammation-related diseases such as sepsis-related lung injury, acute respiratory distress syndrome or acute pancreatitis.

The present application relates to a method for synthesizing leu-enkephalin by Fmoc method, which uses Fmoc-protected amino acid as monomer, and sequentially connects amino acid to resin. In the synthesis of leu-enkephalin, all the amino acids do not have any side chain protection group. The Fmoc protection group is removed by using a solution of 1.00 mol / L imidazole and 0.02 mol / L tricyclohexylphosphine in tetrahydrofuran, and finally leu-enkephalin is obtained by removing the resin with aqueous trifluoroacetic acid. The present application first uses imidazole and tricyclohexylphosphine as components of Fmoc deprotection agent, instead of traditional pyridine. The deprotection agent is not controlled by "controlled chemicals", is cheap and easy to obtain, is stable in nature, and is low in toxicity, volatility and corrosion. The deprotection agent has excellent Fmoc removal ability, does not cause phenolic ring acylation side reaction of tyrosine side chain, does not need any side chain protection, simplifies the production process of polypeptide, reduces the preparation cost of polypeptide, and provides great improvement space for the design of synthesis strategy of polypeptide containing basic sensitive side chain protection group.

The utility model relates to rectifying device technical field especially a kind of pyridine methanol rectifying device of stable assembly type, including base, the top side of base is equipped with support frame, the side of support frame is equipped with several mutually superposed tower tubes, the both ends of each tower tube are equipped with flange, two adjacent flanges are connected by bolt, the side of support frame is equipped with several fixed plates, the one end of each fixed plate is arc-shaped setting, and the one end of each fixed plate is stretched to the both sides of tower tube, the side of each fixed plate is connected with first arc-shaped connecting plate and second arc-shaped connecting plate. First arc-shaped connecting plate and second arc-shaped connecting plate can be connected with the flange on each tower tube in the application, and first arc-shaped connecting plate and second arc-shaped connecting plate are also connected on support frame by fixed plate, so that each tower tube can be supported by support frame, so that the pressure received by each tower tube is same, and assembly stability is improved.

The application belongs to the field of organic material preparation, and particularly relates to a kind of poly-metal phthalocyanine-based porous organic material based on 4-dimethylamino pyridine hot melt method and preparation method and application.The method for preparing poly-metal phthalocyanine-based porous organic material based on 4-dimethylamino pyridine hot melt method comprises the following steps: mixing cyano-containing aromatic monomer, metal element and 4-dimethylamino pyridine, placing in a closed reaction container, heating to a temperature above the melting point of 4-dimethylamino pyridine under the condition of no additional solvent, and then reacting; after the reaction is completed, the product is washed and purified to obtain poly-metal phthalocyanine-based porous organic material. The application utilizes 4-dimethylamino pyridine as a reaction medium and an efficient nucleophilic catalyst, and establishes a general synthesis platform for synthesizing polyphthalocyanine porous material from cyano monomers.

The present application relates to the technical field of surface modification materials, and particularly relates to a perfluoroalkyl silane coupling agent for material surface modification and a preparation method thereof. The coupling agent comprises synergistically modified perfluoroalkyl triethoxysilane, an organic small-molecule functional regulator, an acid catalyst, a surfactant, a stabilizer, ethanol and deionized water. The synergistically modified perfluoroalkyl triethoxysilane is prepared by synergistic modification of perfluoroalkyl triethoxysilane, monohydroxyl column [5] arene, octakis(glycidyl ether propyl) silsesquioxane, N-(2-aminoethyl)-3-aminopropyl trimethoxysilane and 2,6-pyridine dimethyl formaldehyde through host-guest inclusion, epoxy-amine ring-opening reaction and Schiff base condensation reaction, and the organic small-molecule functional regulator is 9,10-dihydroxyanthracene. The preparation method is simple and suitable for surface modification of various substrates such as glass, metal, ceramic and polymer materials.

To provide pharmaceutical compositions for use in treatment of a subject having or at risk of having cancer.SOLUTION: A pharmaceutical composition is provided which comprises a compound (2) represented by a chemical formula in the figure and a pharmaceutically acceptable carrier. The compound (2) is formulated into a dosage form for administration of a unit dose in a range from about 100 mg to about 200 mg each time.SELECTED DRAWING: None

This invention discloses a method for preparing and applying a gold cluster scintillator protected by a stable luminescent free radical ligand. The scintillator material uses (3,5-dichloro-4-pyridine)bis(2,4,6-trichlorobenzene)methyl free radical (PyBTM) as a ligand, and a chain-like tetranuclear free radical cluster is constructed using a one-pot method. The chemical formula of the compound is [Au4(PNP)2(PyBTM)2](SbF6)4, belonging to the triclinic crystal system, space group R-3. This free radical cluster scintillator achieves 100% theoretical exciton utilization and a short radiation decay lifetime due to its unique doublet emission mechanism. These properties make it an ideal candidate material for overcoming the contradiction between high luminous yield and fast response in traditional scintillators. Due to the excellent thermal and water-oxygen stability of this system, it can be fabricated into a scintillator screen to further achieve high-quality X-ray imaging with a spatial resolution of up to 31 LP·mm. ‑1 This provides a general design strategy for high-performance radiation detection materials.

A pyrrolopyrimidine or pyrrolopyridine derivative and its medical use. Specifically, the compound has the structure shown in formula I, has good inhibitory effect on focal adhesion kinase (FAK), and can inhibit its related signal pathways, and can be prepared for treating or preventing diseases related to cancer, pulmonary arterial hypertension, pathological angiogenesis, etc., and can be particularly used for treating diseases caused by excessive or abnormal cell proliferation, such as tumors or cancers.

The present invention relates to compounds of formula (I) wherein A is a 3-10 membered carbocyclic ring or a 4-12 membered heterocyclic ring containing 1-4 heteroatoms selected from O, N or S; B is any one of the following groups (1), (2) or (3); C is any one of the following groups (1'), (2'), (3') or (4'); G1 is CH2, NH or O; G2 and G3 are independently of each other CH or N; Z is -C(O)-, -SO2-, -C 1‑3 alkyl- or -CH2-C(O)-; L is a bond, -C 1‑7 alkyl- or -C 1‑7 alkenyl-. The compounds of formula (I) are inhibitors of cytochrome P450 monooxygenase 11A1 (CYP11A1). The compounds are useful as medicaments for the treatment of steroid receptor, e.g. androgen receptor or estrogen receptor dependent diseases and disorders such as cancer including prostate cancer and estrogen cancer.

The application discloses a bisoxazoline pyridine functionalized porous organic polymer and preparation and application thereof; firstly, a styryl functionalized PyBox monomer (VPyBox) is designed and synthesized, and VPyBox, styrene and divinylbenzene are subjected to free radical polymerization under initiation of azobisisobutyronitrile in a certain proportion to obtain a series of porous organic polymers (POP-PyBox); the POP-PyBox can be used as a solid N , N , N tridentate ligand for Co-catalyzed hydrosilylation of arylalkynes with diphenylsilane; the heterogeneous catalyst system developed by the application has a catalytic activity comparable to that of a homogeneous catalyst reported in the literature, and the catalyst is easy to separate and recover; the recovered catalyst can be recycled for more than 6 times, which can not only greatly reduce the preparation cost of vinylsilane, but also simplify the post-treatment process and reduce the three wastes, and has a good practical application prospect.

To provide pyridopyrimidinone derivatives as AHR antagonists.SOLUTION: The present disclosure relates to compounds of formula (Ia) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same, intermediate compounds useful for preparing the same, and methods for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling. These compounds may also be useful in treating cancer when administered in combination with at least one additional therapy.SELECTED DRAWING: None

This invention provides an ultramicroporous porous coordination polymer, its preparation method, and its application in the adsorption and separation of carbon dioxide, relating to the field of novel materials for gas-phase adsorption and separation. The material is named TCE-NH2ipa, with the chemical formula [Co2(bpt)2(NH2ipa)2]. n In this method, Co represents the metal center cobalt, bpt represents the organic ligand 4-(3-pyridin-4-yl-1H-1,2,4-triazol-5-yl)pyridine, and NH2ipa represents the organic ligand 3-aminoisophthalic acid. The method involves fully dissolving bpt, NH2ipa, and Co(NO3)2·6H2O, transferring the solution to a pressure-resistant sealed container, and heating it for reaction. After the reaction is complete, solvent exchange and heating activation steps are performed to finally obtain a homogeneous powdered material. The TCE-NH2ipa material of this invention exhibits good adsorption capacity for carbon dioxide, hardly adsorbs nitrogen at room temperature and pressure, and can selectively adsorb carbon dioxide in an acetylene / carbon dioxide mixture, demonstrating excellent selectivity and scalability.

The application discloses a new method for synthesizing 3-acyl imidazo[1,5-a]pyridine compounds. The method comprises the following steps: adding 2-pyridyl-p-methanequinone (2-Py-p-QMs), terminal alkyne and p-toluenesulfonyl azide (TsN3), catalyst CuI, organic solvent and alkali into a reaction container under the condition of RT and O2 atmosphere, stirring the reaction for 4 hours, and then separating and purifying 3-acyl imidazo[1,5-a]pyridine compounds after the reaction is completed. The method expands the structure range of 3-acyl imidazo[1,5-a]pyridine products, and more compounds with rich structures can be obtained. Compared with the previous method for synthesizing the target product, the method is efficient, the reaction reagent is non-corrosive, the method design is novel, the raw material is cheap, the operation method is simple, and the product can be directly obtained under mild conditions.

The application belongs to the technical field of extraction separation, and particularly relates to a 3N-PTD ligand and a preparation method and application thereof. The preparation method provided by the application comprises the following steps: mixing 3-chloropropylamine hydrochloride, sodium azide and deionized water, and performing a reflux reaction to obtain 3-azidopropylamine; dissolving 2,6-diethynylpyridine, 3-azidopropylamine, sodium ascorbate and CuSO4.5H2O, and performing a click reaction to obtain the 3N-PTD ligand. The yield of the 3N-PTD ligand obtained by the preparation method is high.

This invention relates to the field of bionanomaterials technology, and particularly to mitochondrial-targeting nanomaterials based on ZnO quantum dots, their preparation methods, and applications. The preparation method of mitochondrial-targeting nanomaterials based on ZnO quantum dots includes the following steps: synthesis of silanized HNO donor: hydroxylamine hydrochloride is dissolved in a mixed solvent of anhydrous tetrahydrofuran and anhydrous pyridine, and a dichloromethane solution of 2-(4-chlorosulfonylphenyl)ethyltrimethoxysilane is added. The reaction is carried out with stirring at room temperature, and after post-treatment, silanized HNO donor is obtained; synthesis of zinc oxide quantum dots: zinc acetate dihydrate is dissolved in anhydrous ethanol, diethanolamine is added, the reaction is carried out, and after post-treatment, zinc oxide quantum dots are obtained. The preparation method can prepare mitochondrial-targeting nanomaterials that achieve precise delivery, controlled release, and visual tracking of HNO into cardiac mitochondria, solving the technical problems of traditional HNO donors' inability to achieve stable loading on a carrier and lack of targeting ability to mitochondria.

This invention belongs to the field of MOF mixed matrix membrane technology, and discloses a MOF mixed matrix membrane for ion sieving and its preparation method. The preparation method includes dissolving an organic ligand and a metal source in an organic compound, ultrasonically treating it to obtain a precursor solution, subjecting the precursor solution to a hydrothermal reaction to obtain a first intermediate product, washing and vacuum drying the first intermediate product to obtain MOF-808 powder; dissolving 8-hydroxyquinoline in anhydrous ethanol, adding the MOF-808 powder, and sealing and stirring to obtain 8-Hq@MOF-808 powder; filtering the 8-Hq@MOF-808 powder onto a substrate, spin-coating an epoxy resin solution onto the substrate containing the 8-Hq@MOF-808 powder, and drying at room temperature to obtain the MOF mixed matrix membrane. The phenolic hydroxyl oxygen atom and pyridine ring nitrogen atom of 8-hydroxyquinoline act as bidentate ligands, forming a stable five-membered chelate ring with metal ions, exhibiting high coordination efficiency.

The present invention relates to combinations of a compound of formula (A-1) with a compound selected from the group consisting of dimpropyridaz, emamectin and isocycloseram, bentioflumin, pioxaniliprole, isoflualanam, cybenzoxasulfyl, vinylfluthrin, cyclobunofen, flupymezotiaz, fentiazoluron, 1-(1,2-dimethylpropyl)-5-methyl-N-prop-2-ynyl-N-(3-pyridyl)pyrazole-4-carboxamide, 1 -[4- [5-ethylsulfonyl-1-methyl-4-[3-methyl-6-(trifluoromethyl)imidazo[4,5-b]pyridin-2-yl]imidazol-2- yl]phenyl]cyclopropanecarbonitrile, [(Z)-[[3-ethylsulfonyl-5-[4-(trifluoromethoxy)phenyl]-2-pyridyl]-[[5- (trifluoromethyl)-2-pyridyl]amino]methylene]amino] acetate, 3-[3-ethylsulfonyl-5-[4- (trifluoromethoxy)phenyl]-2-pyridyl]-4-[5-(trifluoromethyl)-2-pyridyl]-1,2,4-oxadiazol-5-one, 1-(4- chlorophenyl)-2-fluoro-4-methyl-5-(2,2,2-trifluoroethylsulfanyl)benzene, and emamectin benzoate; and to methods of controlling or preventing damage to plants using such combinations; and to formulations, concentrates and seed treatments comprising such combinations.

This invention relates to a chiral preparation method for irushlstat. Specifically, the method uses 2,3-dihydro-1,4-benzodioxyl-6-aldehyde and 2-amino-1-(pyrrolidine-1-yl)ethyl ketone as starting materials, and carries out an asymmetric aldol reaction in the presence of a pyridinium salt carbonyl catalyst. Following reduction and amidation reactions, chiral irushlstat is obtained. Compared with existing technologies, this invention utilizes the strong catalytic ability of small-molecule pyridinium salt carbonyl catalysts, starting from inexpensive and readily available raw materials, to rapidly construct the two key chiral centers of the irushlstat structure with high diastereoselectivity and high enantioselectivity, shortening the synthetic steps of irushlstat. Furthermore, the reaction conditions of this invention are mild and the operation is simple.

The present invention provides compounds of formula (I) and / or salts thereof and / or biologically active metabolites thereof and / or prodrugs thereof and / or solvates thereof and / or hydrates thereof and / or polymorphs thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA α5 positive allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA α5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

This invention discloses an iron complex with a triazacyclic nonane macrocyclic skeleton, its preparation method, and its applications, belonging to the field of coordination chemistry. The iron complex has a triazacyclic nonane macrocyclic skeleton with two acetate side groups and one pyridine-N derivative side group. The iron complex exhibits excellent catalytic activity in the aerobic oxidation of N-aryltetrahydroisoquinoline, while also possessing good stability. The solvents for the catalytic reaction are water and acetonitrile, resulting in low pollution. This invention features mild reaction conditions, simple synthesis operations, and straightforward post-processing, meeting the requirements of environmental friendliness and clean production.

The present application relates to a kind of valsartan-2-amino pyridine co-amorphous and preparation method, the co-amorphous of valsartan-2-amino pyridine of the present application is with 2-amino pyridine according to specific proportion mixed, using solvent evaporation method to prepare single-phase amorphous binary system, the present application uses the interaction between 2-amino pyridine and valsartan, forms ternary hydrogen bond connection mode, greatly improves the solubility and dissolution of valsartan, improves bioavailability, and cost is low, energy consumption is low, can large-scale industrial production.

The application relates to the technical field of chemical synthesis, and particularly discloses a production method of 2-amino-5-methylpyridine. The production method obtains 2-amino-5-methylpyridine with high yield and high selectivity through (1) an amination reaction and (2) post-treatment, and has the advantages of short cycle, high equipment utilization, large batch yield, low total production cost, less waste and the like.