217 results about "Cyclopentanes" patented technology

The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-TH-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

The invention belongs to the technical field of drug synthesis, and particularly relates to an adamantane derivative as well as a synthesis method and application thereof. The adamantane derivative comprises an intermediate structural formula I, an intermediate structural formula II and an intermediate structural formula III, and the structural general formula is as follows: Linker is substituted or unsubstituted C6-C10 aroyl, R1 is hydrogen or C1-C6 alkyl, R2 is hydrogen, C1-C6 alkyl or a nitrogen-containing or nitrogen-free structural fragment, or the integral structure of R1R2 is N-substituted heterocyclic pentyl or heterocyclic cyclohexyl. According to the adamantane derivative provided by the invention, an adamantane structure is combined with part of groups of OAB-14, and a parent nucleus structure is changed, so that the drug activity is improved. The invention also provides a synthesis method of the compound, the obtained compound is screened through cell viability research, and the compound has a potential synergistic effect in the aspects of preventing influenza and treating Alzheimer's disease.

The invention provides a cationic conjugated polymer as well as a preparation method and application thereof. The structural formula of the cationic conjugated polymer is shown in the specification. The preparation method comprises the following steps: reacting tris (4-bromophenyl) amine and N, N-dimethyl-4-(4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolane-2-yl) aniline in an organic solvent under the action of a catalyst and an initiator to obtain a first intermediate; the cationic conjugated polymer is prepared from the first intermediate, the second intermediate and the third intermediate under the action of a catalyst and an initiator. The cationic conjugated polymer shows good photo-thermal and photodynamic performance under the irradiation of near-infrared light with the wavelength of 980 nm, so that the effect of inhibiting the growth of bacteria is realized. # imgabs0 #

Disclosed herein are compositions and formulations of 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)benzonitrile (Compound (I)), wherein Compound (I) has the structure (I) and methods of making and using such compositions and formulations.

The invention discloses a series of recombinant bacteria for expressing a steroid compound taking a cyclopentane multi-hydrogen phenanthrene structure as a structural mother nucleus, such as recombinant strains for expressing cholesterol, 22-hydroxycholesterol, diosgenin or polyphyllin II, and construction and application of the strains. The invention provides a recombinant bacterium which can efficiently express a steroid compound taking cyclopentane multi-hydrogen phenanthrene as a structural mother nucleus, for example, the yield of diosgenin can be increased to the level of 40 mg / L or above, heterologous synthesis of the polyphyllin II is also realized to obtain a polyphyllin II synthetic strain, the yield of the polyphyllin II in a shake flask reaches 0.13 mg / L, and the yield of the polyphyllin II in the shake flask reaches 0.13 mg / L. The strain is the first strain for heterologous synthesis of the polyphyllin II at present.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a memantine derivative and a synthesis method and application thereof. The memantine derivative comprises an intermediate structural formula I, an intermediate structural formula II, an intermediate structural formula III and a structural general formula, Linker is substituted or unsubstituted C6-C10 aroyl, R1 is hydrogen or C1-C6 alkyl, R2 is hydrogen, C1-C6 alkyl or a nitrogen-containing or nitrogen-free structural fragment, or the integral structure of R1 and R2 is N-substituted heterocyclic pentyl or heterocyclic cyclohexyl. According to the memantine derivative provided by the invention, a memantine group is combined with an OAB-14 partial structure to change a parent nucleus structure, so that the drug activity is improved. The invention also provides a synthesis method of the compound, and the obtained compound is used for treating Alzheimer's disease and Parkinson's disease.

The invention relates to the technical field of organic synthesis, in particular to a method for synthesizing cyclopentane compounds through [3 + 2] cycloaddition reaction of aryl cyclopropane and olefin under the synergistic catalysis of bromide ions / visible light. The method comprises the following steps: in a nitrogen atmosphere, sequentially adding aryl cyclopropane, a benzyl malononitrile derivative, pyridine tribromide and a photocatalyst into a reaction solvent to obtain a mixture, stirring the mixture at the temperature of 40 DEG C under the irradiation of a 12W blue light LED lamp until the reaction is complete, and performing concentration and column chromatography purification to obtain the cyclopentane compound. The method has the advantages of mild reaction conditions, simple operation, simple and easily available raw materials and low cost.

The application provides a system and method for integrated acetaldehyde distillation and recovery, which comprises a vertically arranged main tower, the main tower is sequentially divided into a distillation section, a catalytic reaction section, a stripping section and a stripping section from top to bottom, the top of the distillation section is provided with a self-adaptive distributor and a tower top pressure controller, the catalytic reaction section comprises catalytic filler plates and a transverse liquid redistributor, and the catalytic filler plates are loaded with catalysts. The four sections of stripping, stripping, catalytic reaction and distillation are integrated in the vertical main tower, the intermediate cooling and conveying equipment are cancelled, and the investment and energy consumption are significantly reduced. The catalytic reaction section adopts the corrugated filler loaded with catalysts and cooperates with the transverse liquid redistributor, so that the liquid forms thin layer flow, the reaction residence time is effectively prolonged, and the hydrolysis decomposition rate of 2-methyl-1,3-dioxolane (MD) and the acetaldehyde recovery rate are improved.

The invention provides a cycloalkane separation method, a computer program product and a cycloalkane detection system. The method comprises the steps that a detection device is controlled to separate compounds, the one-dimensional retention time of all the compounds in a one-dimensional chromatographic column is obtained, the two-dimensional retention time of all the compounds in a two-dimensional chromatographic column is obtained, the one-dimensional retention time is the time needed for separating out the compounds through the one-dimensional chromatographic column, and the two-dimensional retention time is the time needed for separating out the compounds through the two-dimensional chromatographic column. The two-dimensional retention time is the time required for separating the compound by the two-dimensional chromatographic column; a target compound in the separated compounds is determined according to the one-dimensional retention time and the two-dimensional retention time of the separated compounds, and the target compound is cyclohexane or cyclopentane; the content of the target compound is obtained, the content is sent to target equipment, and the target equipment is equipment used by the target object, so that the target object is guided to improve the catalyst. According to the scheme, the problem that cycloalkanes (cyclohexane or cyclopentane) cannot be rapidly measured in the prior art is solved.

The invention relates to a pharmaceutical salt of a quinoline amine compound, a crystal form and a preparation method of the pharmaceutical salt. Specifically, the invention provides a pharmaceutically acceptable salt of 8-chloro-N-(2, 2-difluorobenzo [d] [1, 3] dioxacyclopentane-5-yl) quinoline-2-amine, a crystal form and a preparation method thereof, and the corresponding salt has good stability and can be better used for clinical treatment.

The invention relates to a quinoline amine compound crystal form and a preparation method thereof. Specifically, the invention provides a crystal form of 8-chloro-N-(2, 2-difluorobenzo [d] [1, 3] dioxacyclopentane-5-yl) quinoline-2-amine and a preparation method thereof, and the corresponding crystal form has good stability and can be better used for clinical treatment.

The invention discloses a composite foaming agent, rigid polyurethane foam, a preparation method and application, and belongs to the technical field of rigid polyurethane materials. According to the technical scheme, the foaming agent comprises a first physical foaming agent, a second physical foaming agent, a chemical foaming agent and silanized cellulose nanocrystals, the first physical foaming agent is cyclopentane, the second physical foaming agent is a low-boiling-point foaming agent, and the chemical foaming agent comprises an organic amine salt compound. The foaming agent is applied to thermal insulation materials, and the problem that an existing foaming agent system cannot give consideration to heat conduction and foam strength well is solved.

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.

The invention provides a crystal form VI of an acrylamide compound, and the acrylamide compound is (S)-N-(5-((6-(2-(7, 7-dimethyl-1-oxo-1, 3, 4, 6, 7, 8-hexahydro-2H-cyclopentane [4, 5] pyrrolo [1, 2-a] pyrazine-2-yl)-3-(hydroxymethyl) pyridine-4-yl)-4-methyl-3-oxo-3, 3, 4-triazolo [1, 2-a] pyrazine-2-yl)-3-(hydroxymethyl) pyridine-4-yl)-4-methyl-3-oxo-3, 3, 4-triazolo [1, 2-a] pyrazine-2-yl)-3-(2, 3, 4-triazolo [1, 2-a] pyrazine-2-yl)-4- The crystal form VI is a 2-(2, 4-dihydropyrazine-2-yl) amino)-2-(2-methyl-4-(tetrahydro-2H-pyran-4-yl) piperazine-1-yl) 5phenyl) acrylamide compound, and an X-ray powder diffraction pattern of the crystal form VI comprises diffraction peaks with the following 2 theta angle values: 8-3 + / -0.2 degrees, 13.2 + / -0.2 degrees and 18.9 + / -0.2 degrees. The crystal form VI has the advantages of good stability and low hygroscopicity, and is suitable for industrial production of bulk drugs and development of preparation prescriptions.

The invention provides a preparation method and application of lipid nanoparticles based on lipoic acid derivatives. The lipoic acid derivative provided by the invention depends on a cyclopentane structure and a disulfide bond of lipoic acid, so that a lipid compound is more easily internalized by cells, and the effectiveness of nucleic acid delivery is improved. The lipid nanoparticles have excellent spleen targeting performance, and drugs are preferentially delivered to the spleen.

The present invention relates to (i) an azeotropic or azeotrope-like composition comprising (a) cis-1,2-dichloroethylene and cis-1H,2H-octafluorocyclopentane or comprising (b) trans-1,2-dichloroethylene and trans-1H,2H-octafluorocyclopentane, (ii) a spin fluid for flash spinning comprising these azeotropic or azeotrope-like compositions and a polyolefin, and (iii) a process for the preparation of plexifilamentary fibrils of polyolefin using the spin fluid.

Methods of treating tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction with (1S,3S)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid or a pharmaceutically acceptable salt thereof are provided. Methods of treating tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction with (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid are provided. Also provided are therapeutic compositions that may be used to improve one or more symptoms of tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction.

A preparation process of 5-ethylidene-2-norbornene, including: introducing dicyclopentadiene into a dicyclopentadiene decomposition reactor to thermally decompose the dicyclopentadiene; introducing a product of the above step into a cyclopentadiene purification tower; introducing 1,3-butadiene, a solvent, and cyclopentadiene separated from the top of the cyclopentadiene purification tower into a Diels-Alder reactor to react the same; introducing a product of the immediate above step into a 1,3-butadiene removal tower to recover 1,3-butadiene from the top; introducing a mixture at the bottom of the 1,3-butadiene removal tower into a desolvation tower, and recycling a solvent and unreacted raw materials recovered from the top of the desolvation tower to the dicyclopentadiene decomposition reactor; introducing a mixture at the bottom of the desolvation tower into a 5-vinyl-2-norbornene separation tower to separate 5-vinyl-2-norbornene; and introducing the 5-vinyl-2-norbornene into an isomerization reactor to react the same.

This invention discloses a high-strength and tough PET foam sheet and its preparation method, belonging to the field of foam material technology. It comprises the following raw materials in parts by weight: 100 parts food-grade PET resin, 3-7 parts melt reinforcing agent, 3-5 parts crystallization toughening agent, 1-3 parts in-situ fiber-forming reinforcing agent, 1-5 parts compatibility dispersant, and 8-10 parts cyclopentane. The preparation method includes: S1, mixing dried food-grade PET resin with melt reinforcing agent, crystallization toughening agent, in-situ fiber-forming reinforcing agent, and compatibility dispersant to obtain a premix; S2, melting and plasticizing the premix, injecting liquid cyclopentane for blending, and then extruding to a normal pressure environment to obtain a foam sheet blank; S3, cooling and shaping the foam sheet blank, drawing, trimming, and winding to obtain a high-strength and tough PET foam sheet. The foam sheet obtained by this invention has fine and uniform pores, possessing high flexural strength, high modulus, and high impact toughness, with comprehensive performance far exceeding that of traditional PET foam materials.

The invention discloses a diamine cyclopentane compound, a composition and application of the diamine cyclopentane compound, and belongs to the field of chemical medicines. The invention provides a diamine cyclopentane compound as shown in formula (I), or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvent compound, a crystal form, a stereoisomer or an isotope variant thereof, and the diamine cyclopentane compound can be used for preventing and inhibiting neurogenic inflammation, and is used for treating and / or preventing urticaria itching, angioedema and other related diseases. # imgabs0 #

The preparation method comprises the following steps: 1, adding tartaric acid, an acid-binding agent and a first organic solvent into a reaction container, uniformly mixing, cooling, dropwise adding a mixed solution of triphosgene and the first solvent into the reaction container under the condition that the temperature does not exceed 10 DEG C, and reacting for 1-2 hours at the temperature of 20-30 DEG C, so as to obtain 5-(methoxycarbonyl)-2-oxo-1, 3-dioxolane-4-methyl formate, namely the 5-(methoxycarbonyl)-2-oxo-1, 3-dioxolane-4-methyl formate, namely the 5-(methoxycarbonyl)-2-oxo-1, 3-dioxolane-4-methyl formate. After dropwise adding, heating to room temperature, stirring, and concentrating filtrate to obtain an intermediate; and 2, adding the intermediate, a second organic solvent, a catalyst and methanol into a reflux reaction container with a water knockout drum and a condenser, carrying out heating reflux reaction to separate water, concentrating the reaction liquid after the reaction is finished to obtain a crude product, adding the crude product into a first organic solvent, carrying out heating reflux, filtering to remove insoluble substances while the crude product is hot, cooling and crystallizing the filtrate, carrying out suction filtration, and drying to obtain the target product. The method has the advantages that the synthesis method is simple and easy to implement, the post-treatment method is easy to operate, and the product is high in purity and good in yield.

The invention discloses a preparation method of dicyclopentyl methacrylate, which comprises the following steps: carrying out hydration reaction on dicyclopentadiene serving as a starting raw material to obtain an intermediate I, carrying out hydrogenation reaction to obtain an intermediate II, and carrying out esterification reaction to obtain the dicyclopentyl methacrylate. The reaction temperature is 40-60 DEG C, and the mass ratio of dicyclopentadiene to phosphoric acid is (1.1-1.3): 1; the hydrogenation reaction takes palladium on carbon as a catalyst, the reaction temperature is 38-48 DEG C, and the mass ratio of the intermediate I to the palladium on carbon is 1: (0.001-0.01); the esterification reaction is carried out on the intermediate II and methacryloyl chloride under the catalytic action of an acid-binding agent triethyl diamine, the reaction temperature is-2 DEG C to 5 DEG C, and the molar ratio of the intermediate II to the methacryloyl chloride to the triethyl diamine is 1: (1.2-1.8): (2-3); the product purity reaches 99.80% or above, the total amount of metal impurities is lower than 70 ppb, the quality of the product is far higher than that of commercially available products, and the product meets the quality requirement of a resist raw material for photoresist.

The present invention discloses a method for preparing 1-aryl-3-arylsulfinylbicyclo[1.1.1]pentane. Under inert gas protection, an aryl Grignard reagent is reacted with [1.1.1] propeller alkane, and the resulting intermediate solution is reacted with an SO2 source. After the reaction is completed, 1-aryl-3-arylsulfinylbicyclo[1.1.1]pentane is obtained by post-processing. The present invention achieves efficient preparation of 1-aryl-3-arylsulfinylbicyclo[1.1.1]pentane without adding any catalyst, and has low raw material cost, easy operation, mild conditions, and high reaction yield, and has broad application value.

The present invention relates to the field of organic synthesis, and more particularly to a process for the preparation of cycloethers of formula (I) comprising the cyclization of compounds of formula (II) in the presence of a Lewis acid, a protic acid having a pKa of 2 or less, or a mixture thereof.

The invention relates to the technical field of chemical synthesis, in particular to a preparation method of 1-benzyl alcohol-3-alkyl bicyclo [1.1. 1] pentane, which comprises the following steps: by taking aromatic aldehyde, [1.1. 1] propeller alkane and 4-alkyl substituted Hanss ester synthesized by aldehyde as initial raw materials and dichloroethane and the like as a solvent, carrying out a reaction under the protection of inert gas to obtain 1-benzyl alcohol-3-alkyl bicyclo [1.1. 1] pentane, and separating the 1-benzyl alcohol-3-alkyl bicyclo [1.1. 1] pentane from the 1-benzyl alcohol-3-alkyl bicyclo [1.1. 1] pentane. A three-component free radical coupling reaction is carried out under the illumination condition, and a 1-benzyl alcohol-3-alkyl bicyclo [1.1. 1] pentane product is synthesized in one step. The method has the advantages of mild reaction conditions, high reaction efficiency, low cost, simplicity and convenience in operation and the like, and a new method is provided for later structural modification of diaryl methanol drug molecules.

The invention provides a foaming agent composition, premixed polyether polyol, a polyurethane composition, polyurethane foam and refrigeration equipment. The foaming agent composition comprises a foaming agent and a foam stabilizer, the foaming agent comprises bio-based cyclopentane and a CO2-based foaming agent, and the foam stabilizer comprises a bio-based siloxane-polyether copolymer. The environment-friendly property of the polyurethane foam can be improved.

This invention belongs to the technical field of drug synthesis, specifically relating to memantine derivatives, their synthetic methods, and applications. The memantine derivatives include intermediate structural formulas I, II, and III, as well as a general structural formula. The linker is a substituted or unsubstituted C6-C10 aryl group, R1 is hydrogen or a C1-C6 alkyl group, and R2 is hydrogen, a C1-C6 alkyl group, or a nitrogen-containing or nitrogen-free structural fragment, or the overall structure of R1 and R2 is an N-substituted heterocyclopentyl or heterocyclohexyl group. The memantine derivatives provided by this invention improve drug activity by combining the memantine group with the OAB-14 partial structure, thereby altering the core structure. This invention also provides a synthetic method for the obtained compounds used in the treatment of Alzheimer's disease and Parkinson's disease.

The present invention relates to methods, compositions, and combinations for inhibiting the NLRP3 inflammasome and / or LON protease as well as methods, compositions, and combinations for treating cancer, particularly blood cancer or brain cancer. In certain aspects, the compositions and combinations include a synthetic triterpenoid, such as 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-2-yl)-1H-imidazole (“CDDO-2P-Im”) and 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-3-yl)-1H-imidazole (“CDDO-3P-Im”).