120 results about "Cyclobutanes" patented technology

Methods for treating patients with wAIHA comprising administering at least one compound chosen from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (rilzabrutinib) and pharmaceutically acceptable salts thereof are disclosed.

Methods for treating Sickle Cell Disease (SCD) comprising administering a BTKi, such as at least one compound chosen from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (rilzabrutinib) and pharmaceutically acceptable salts thereof, are disclosed.

To provide a type I receptor tyrosine kinase inhibitor.SOLUTION: Or a pharmaceutically acceptable salt thereof. Specific examples thereof include N - (4 - ([1,2,4] triazolo [1, 5-c] pyrimidin-7-yloxy) - 3-methylphenyl) - 5 - (3 - (dimethylamino) azetidin-1-yl) - 6-methoxyquinazolin-4-amine.SELECTED DRAWING: None

The invention belongs to the technical field of medicine synthesis, and particularly relates to a method for efficiently preparing cyclobutane derivatives. Comprising the following steps: dissolving 4-chloro-7H-pyrrolo [2, 3-d] pyrimidine and chloromethyl pivalate in 1, 4-dioxane, and adding an acid binding agent for reaction to obtain a reaction solution; the preparation method comprises the following steps: adding 1-(1-ethoxyethyl)-4-pyrazol boronic acid pinacol ester, purified water, a catalyst and an acid-binding agent into a reaction kettle, carrying out Suzuki reaction, separating liquid, adding activated carbon into an upper organic phase for decoloration, adding an organic solution containing hydrogen chloride for crystallization, and filtering to obtain a wet product; and dissolving the wet product and 2-[1-(ethylsulfonyl)-3-azacyclobutane] acetonitrile in 1, 4-dioxane, and reacting under an alkaline condition to obtain the cyclobutane derivative. According to the preparation method, synthesis is performed through a one-pot four-step reaction, a solvent only relates to 1, 4-dioxane and water, and post-treatment is simple, convenient and efficient.

The application discloses a preparation method of baricitinib, and belongs to the technical field of drug synthesis. The method comprises the following steps: firstly, 2-[1-(ethylsulfonyl)-3-azetidinyl]acetonitrile and 4-pyrazole boron pinacol ester are subjected to a Michael addition reaction to obtain 1-(ethylsulfonyl)-3-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]-3-azetidine acetonitrile as an intermediate I; secondly, a protection group is introduced on the amino group of 4-chloropyrrolopyrimidine to obtain an intermediate II; finally, the intermediate I and the intermediate II are subjected to a Suzuki coupling process by adopting a method of combining a nickel pre-catalyst with a supporting ligand to obtain the baricitinib. The preparation method creatively realizes cross coupling of the baricitinib by adopting the cheap metal nickel as a catalyst, avoids the use of a heavy metal palladium catalyst, and has the advantages of low cost, low toxicity, small pollution, green environmental protection and the like.

Provided are a curable composition, a curable ink composition, and a curable ink composition for inkjet, each of which has low viscosity, low volatility, and curability. And methods of using these compositions are provided. The curable composition contains an epoxy / oxetane compound represented by chemical formula (I). In the formula, n is the same or different and represents an integer of 2-5.

A novel crystalline form of a GLP-1 receptor agonist, its preparation method, its pharmaceutical composition, and its use are provided. The GLP-1 receptor agonist is designated Compound I, i.e., (S)-2-((4-(6-((2-fluoro-4-(oxetan-3-yl)benzyl)oxy)pyridin-2-yl)piperidin-1-yl)methyl)-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid.

The invention provides a compound of carboplatin and 1, 1-cyclobutane dicarboxylic acid and a detection method of the compound. A nuclear magnetic resonance hydrogen spectrum and a nuclear magnetic resonance carbon spectrum of the carboplatin and 1, 1-cyclobutane dicarboxylic acid eutectic compound in a D-(+)-glucose heavy water solution with the mass fraction of 5%, a nuclear magnetic resonance hydrogen spectrum and a nuclear magnetic resonance carbon spectrum of carboplatin in a 1.2. 3. 4-cyclobutane tetracarboxylic acid heavy water solution with the mass fraction of 2%, and a 1, 1-cyclobutane dicarboxylic acid eutectic compound with the mass fraction of 1, 1-cyclobutane dicarboxylic acid are measured. A nuclear magnetic resonance hydrogen spectrum and a nuclear magnetic resonance carbon spectrum of carboplatin and 1, 1-cyclobutane dicarboxylic acid in a D-(+)-glucose heavy water solution with the mass fraction of 5% are analyzed, and the structure of the carboplatin and 1, 1-cyclobutane dicarboxylic acid eutectic compound in water is determined by analyzing the chemical shift change of characteristic carbon atoms in the nuclear magnetic resonance carbon spectrum.

The invention provides a preparation method of an ivabradine hydrochloride key intermediate (I), the method is characterized in that (1S)-4, 5-dimethoxy-1-(aminomethyl) benzocyclobutane is used as a raw material, and (1S)-4, 5-dimethoxy-1-[(methylamino) methyl] benzocyclobutane hydrochloride (I) is obtained through condensation and reduction reaction, the method is simple to operate, the yield is high, and the method is suitable for industrial production. The method has the advantages of mild conditions, high reaction yield, significantly reduced cost, avoidance of high toxic substances, significantly improved environmental benefits, and suitableness for large-scale industrial production.

The present invention relates to (3)-phenoxyazetidin-(1)-yl-heteroarylpyrrolidine derivatives of general formula (I) that are agonists of GPR52, useful for the treatment of central nervous system disorders and other disorders. The present invention also relates to (3)-phenoxyazetidin-(1)-yl-heteroarylpyrrolidine derivatives of general formula (I) for use as medicines, pharmaceutical compositions comprising at least one compound of general formula (I) and methods for preparing pharmaceutical compositions, as well as methods for preparing the compounds according to the invention.

The application belongs to the field of organic synthesis, and discloses a preparation method of 1-amino cyclobutanecarboxylic acid, which comprises the following steps: S1. 1-cyanocyclobutyl carboxylic acid ethyl ester is reacted under acidic conditions to obtain 1-formylaminocyclobutane carboxylic acid ethyl ester; S2. 1-formylaminocyclobutane carboxylic acid ethyl ester is reacted under the action of sodium hypochlorite to obtain 1-amino cyclobutanecarboxylic acid ethyl ester; S3. 1-amino cyclobutanecarboxylic acid ethyl ester is reacted under the action of a base catalyst and di-tert-butyl dicarbonate to obtain BOC-1-amino cyclobutane carboxylic acid ethyl ester; and S4. BOC-1-amino cyclobutane carboxylic acid ethyl ester is reacted under the action of an acid catalyst to obtain 1-amino cyclobutanecarboxylic acid. The product obtained by the preparation method is pure, has no inorganic salt residue, and is simple to operate, low in cost and suitable for industrialized production.

The application discloses a kind of self-reinforced nylon materials and preparation method thereof, and the self-reinforced nylon material contains the benzocyclobutane structure sensitive to force.By interface polycondensation method, the benzocyclobutane structure is introduced into nylon main chain.When the matrix material is subjected to destructive force, the benzocyclobutane structure unit undergoes ring-opening isomerization, and simultaneously reacts with the bifunctional group crosslinking agent in the matrix material, plays the crosslinking self-reinforcing role.The technical route of the application is simple, the required cost is low, and the prepared nylon material can be used in some engineering plastic application fields with harsh service conditions, and can reduce the risk of component failure.

Provided are: a resin composition which contains a resin having a polymerizable group and a photopolymerization initiator, wherein the resin has at least one partial structure represented by formula (A-1a) or formula (A-1b), and the proportion of the molar amount of a cyclobutane ring having a trans-type steric conformation to the total molar amount of cyclobutane rings contained in the resin is 80% or more; a cured product which is obtained by curing the composition and a method for producing the cured product; a laminate which contains the cured product and a method for producing the laminate; a semiconductor device and a method for producing the semiconductor device; and a novel resin.

The invention relates to a preparation method of a dimer-mediated organic polymer single crystal, and belongs to the technical field of organic polymer single crystals. The preparation method comprises the following steps: S1, carrying out coordination self-assembly on a metal salt, an alkenyl pyridine ligand and an auxiliary ligand in a solvent, and washing and drying to obtain a coordination polymer single crystal reaction template; s2, under irradiation of ultraviolet light or visible light, the coordination polymer single-crystal reaction template is subjected to a [2 + 2] light ring addition reaction, and a coordination polymer containing a cyclobutane dimer is obtained; s3, under the action of alkali liquor or acid liquor, dissociating the coordination polymer containing the cyclobutane dimer, extracting, concentrating and recrystallizing to obtain dimer single crystals; s4, under the irradiation of ultraviolet light or visible light, carrying out topological chemical polymerization reaction on the dimer single crystal to obtain an organic polymer single crystal; accurate and controllable preparation from the alkenyl pyridine ligand to the high-quality polymer single crystal with the self-supporting long-range ordered structure is successfully realized.

A method for treating pruritus in patients with atopic dermatitis (AD) and / or nodular prurigo (PN) is disclosed, comprising administering a therapeutically effective amount of at least one compound selected from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-carbonyl]-4-methyl-4-[4-(oxecyclobutane-3-yl)piperazin-1-yl]pent-2-enonitrile (rezabrutinib) and pharmaceutically acceptable salts thereof.

The invention discloses a synthetic method of a 3-spirobutyl oxoindole compound containing trifluoromethyl, and belongs to the technical field of organic synthesis. According to the invention, under the action of visible light induction, a photocatalyst and alkali, CF3Br and N-aryl bicyclo [1.1. 0] butane-1-formamide are subjected to a free radical tandem cyclization reaction in an organic solvent, so that the 3-spirobutyl oxoindole compound containing trifluoromethyl is prepared. According to the invention, free radical series cyclization reaction of CF3Br and saturated carbon atoms, namely sp3 hybrid carbon atoms, is realized for the first time, and the variety of organic matters reacting with CF3Br is enriched. The preparation method provided by the invention provides a new path for synthesis of 3-spirobutyl oxindole containing trifluoromethyl, has the advantages of cheap and easily available raw materials, mild reaction conditions, simple operation, high product yield and the like, and accords with the concept of green synthesis.

This invention relates to a method for preparing a bimetallic cyanide (DMC) catalyst, comprising a reaction of an aqueous solution of a cyanide-free metal salt, an aqueous solution of a basic metal cyanide salt, an organic complexing ligand, and optionally a component forming a complex, wherein the metal cyanide salt is one or more compounds selected from potassium hexacyanocobalt(III), potassium hexacyanoferrate(II), potassium hexacyanoferrate(III), calcium hexacyanocobalt(III), and lithium hexacyanocobalt(III), wherein the organic complexing ligand is one or more compounds selected from dimethoxyethane, tert-butanol, 2-methyl-3-buten-2-ol, 2-methyl-3-butyn-2-ol, ethylene glycol mono-tert-butyl ether, and 3-methyl-3-oxetane-methanol, and wherein the basic metal cyanide salt used has an alkalinity between 0.700 wt% and 3.000 wt% sodium hydroxide (NaOH) based on the total weight of the basic metal cyanide salt used, determined by titration as disclosed in the experimental section. Another subject of the invention includes a bimetallic cyanide catalyst (DMC) obtainable by the method according to the invention, and the use of said DMC catalyst in the preparation of polyoxyethylene polyols.

To provide a method for producing hexafluoropropene in which the formation of octafluorocyclobutane, a by-product, is suppressed, and a composition obtained by the said production method. [Solution] A method for producing hexafluoropropene, comprising preheating trifluoromethane at a first preheating temperature of 350 to 700°C, then contacting it with tetrafluoroethylene to obtain a product containing hexafluoropropene.

Disclosed herein are crystalline forms of ((2-Ethylbutanoyl)oxy)methyl(R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate. Also disclosed herein are methods of treating a bacterial with a crystalline form of ((2-Ethylbutanoyl)oxy)methyl(R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate.

This invention belongs to the field of liquid crystal displays and discloses a liquid crystal alignment agent for forming liquid crystal alignment films and a liquid crystal display element. The aim is to provide a liquid crystal alignment agent that, when using negative liquid crystals, can achieve photoalignment films with excellent light spots and image retention characteristics. Furthermore, the alignment agent exhibits excellent viscosity stability during storage, while simultaneously protecting the liquid crystal alignment film obtained from this alignment agent and the liquid crystal display element containing this film. This invention utilizes a modified benzidine reacted with a tetracarboxylic acid dianhydride containing a cyclobutane structure to prepare a polyamic acid coating solution. The resulting photoalignment agent exhibits good storage stability, high compatibility with negative liquid crystal materials, avoids bright spot defects, and possesses excellent image retention characteristics. It can be applied to FFS-driven liquid crystal display elements and other applications requiring high display quality.

The invention discloses a photocatalysis method for [2 + 2] cycloaddition reaction of indole and imine, and belongs to the field of organic synthesis. The problem that the reaction condition of the [2 + 2] cycloaddition reaction of the existing indole compounds is harsh is solved. The method comprises the following steps: carrying out photocatalytic reaction on 1-(3-oxocyclobutane-1-carbonyl)-1H-indole-3-carboxylic acid ethyl ester, ethyl (E)-2-((benzyloxy) amino) acetate, a catalyst, inorganic alkali and an organic solvent, carrying out reduced pressure distillation to remove the solvent after the reaction, and carrying out silica gel column chromatography separation and purification. The method is used for photocatalysis of [2 + 2] cycloaddition reaction of indole and imine.

The invention discloses a synthesis method of 1-(t-butyloxycarboryl)-3-ethoxy azetidine-3-carboxylic acid, and the synthesis route is as follows: the invention discloses a preparation method of 1-(t-butyloxycarboryl)-3-ethoxy azetidine-3-carboxylic acid, which comprises the following steps: by taking 3-oxo azetidine-1-carboxylic acid tert-butyl ester as a raw material, reacting at the temperature of 60-80 DEG C for 2-4 hours, and then adding a catalyst, thereby obtaining the 1-(t-butyloxycarboryl)-3-ethoxy azetidine-3-carboxylic acid. Under an alkaline condition, chloroform and ethanol are mediated, so that a keto carbonyl group of the 3-oxo-azetidine-1-carboxylic acid tert-butyl ester is converted into an ethyoxyl carboxylic acid group, and the target compound 1-(t-butyloxycarbonyl)-3-ethyoxyl azetidine-3-carboxylic acid is obtained. The synthesis method is low in cost, mild in reaction condition, low in potential safety hazard, ideal in yield and simple and efficient in operation, and a potential route is provided for large-scale production of the compound 1-(t-butyloxycarbonyl)-3-ethoxyazetidine-3-carboxylic acid.

This invention discloses a method for synthesizing a dipeptide linker for antibody-coupled degradation, relating to the field of organic synthesis. 1-[(3S)-3-{[(4-{[(2-bromophenyl)oxy]methyl}phenyl)amino]carbonyl}-8-methyl-1-oxoylide-2,8-diazanon-1-yl]cyclobutane-1-carboxylic acid ethyl ester (CAS: 2760139-12-4) is a cleavable dipeptide linker for antibody-coupled degradation, which can be used to synthesize antibody-coupled active molecules. This invention uses readily available and inexpensive commercial raw material p-aminobenzyl alcohol as a starting material, and through seven conventional steps, obtains the target product with high purity and high yield. The starting material is inexpensive, the operation is simple, the reaction conditions are mild, and it can be prepared in large quantities at the hundred-gram scale, representing a completely new synthetic route.

The application discloses a kind of 3-(cholic acid pentanoyl amide) cyclobutane-1,1-dicarboxylic acid purification method, belong to the technical field of pharmaceutical chemistry intermediate purification.The method includes: (1) its precursor diethyl ester is hydrolyzed in methanol and / or acetonitrile, concentrated after dissolving with water, with organic solvent extraction is discarded organic phase, water phase is adjusted to 2-4 to pH, again with organic solvent extraction, concentrated and obtained crude product;(2) the crude product is dissolved in alcohol solvent, after filtration, ester solvent is added to crystallize, alcohol ester volume ratio 1:2-1:10, filtration, washing, drying.The application removes unreacted ester, monocarboxylic acid byproduct and cholic acid analogue amide and other impurities by alkaline hydrolysis combined with "alkali dissolving acid extracting" and "alcohol dissolving-ester crystallizing" recrystallization.The product obtained by the method has HPLC purity ≥98.2%, yield ≥80%, and the process is stable, simple to operate, suitable for large-scale production.

This invention discloses a ribonuclease derived from tartary buckwheat. FtRNH Genes, their expression vectors, and applications. This invention isolates ribonuclease from tartary buckwheat through gene cloning. FtRNH The gene, whose CDS sequence is shown in SEQ ID No. 1, and whose encoded protein amino acid sequence is shown in SEQ ID No. 2, is described in this invention. FtRNH Transgenic lines were obtained by genetic transformation into cultivated tartary buckwheat (ZK3) and subjected to ultraviolet stress treatment. Compared with wild-type materials, the transgenic lines showed increased expression. FtRNH The positive lines of tartary buckwheat exhibited stronger tolerance to ultraviolet radiation and less accumulation of UV-B-induced R-loops and cyclobutanepyrimidine dimers. This invention has significant application prospects in improving the tolerance of cultivated tartary buckwheat to ultraviolet stress or in breeding tartary buckwheat varieties resistant to ultraviolet stress.

High temperature lubricants for magnetic media include a plurality of segments according to general formula (I):where Rd is any linker chemistry and each Re may be a reactive end-group and anchoring group containing at least one constituent configured for at least one of tribochemical, thermochemical, or optochemical bonding. The at least one constituent can be cyclopropane or cyclobutane.

This invention provides a photosensitive polyurethane film with a surface grating, its preparation method, and its applications. The photosensitive polyurethane film with a surface grating exhibits well-defined and controllable photoresponse characteristics. Its core mechanism lies in the photosensitive monomer responding to light stimulation of a specific wavelength through a dimerization reaction: under ultraviolet light irradiation, the photosensitive monomer in the film undergoes a [2+2] cycloaddition to generate a four-membered cyclobutane dimer. This response mechanism is clear, the triggering path is independent, and the response efficiency is high. It effectively overcomes the limitations of existing coumarin derivatives, which can only achieve self-healing technology. By controlling parameters such as irradiation time and number of irradiations, multi-dimensional information storage can be achieved, significantly improving information storage capacity and stability. This effectively solves the urgent problem of high-capacity information storage in the current field of optical encryption materials, providing a feasible technical path for improving the performance and expanding the practical applications of optical encryption materials.

Provided herein are methods of treating and / or managing non-Hodgkin lymphoma, which comprise administering to a patient 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3- morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione ("Compound A, A-S, or A- R"), or an enantiomer or mixture of enantiomers, a tautomer, an isotopolog, a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof, in combination with glofitamab or mosunetuzumab.

The present invention provides a hard coat layer-forming composition from which it is possible to form a hard coat layer that exhibits excellent adhesiveness. A hard coat layer-forming composition according to the present invention comprises: at least one selected from the group consisting of hydrolyzable silicon compounds, hydrolysates thereof, and hydrolysis condensates thereof; a silsesquioxane compound having an oxetanyl group; a cationic polymerization initiator; and two or more hydroxybenzophenone compounds having different numbers of hydroxy groups.

The invention belongs to the field of chemical synthesis, and particularly relates to a synthetic method of azetidine-2-yl (methyl) benzyl carbamate hydrochloride. According to the invention, 1-benzyl azetidine-3-alcohol is used as a basic raw material, and a series of reactions such as substitution reaction and the like are carried out to obtain the high-yield and high-purity azetidine-2-yl (methyl) benzyl carbamate hydrochloride, and the method is suitable for industrial production.