309 results about "Pyrrolidine" patented technology

The invention discloses an indole-benzothiadiazole derivative as well as a preparation method and application thereof. The general structural formula of the indole-benzothiadiazole derivative provided by the invention is shown in the specification, wherein R is selected from one of methyl piperazinyl, diethylamino, azetidinyl and pyrrolidinyl. The derivative can be specifically combined and fluorescently labeled with mitochondrial RNA in cells, and has good selectivity, high fluorescence signal-to-noise ratio and excellent anti-interference capability in a complex biological system. Meanwhile, the indole-benzothiadiazole derivative provided by the invention is simple in synthetic route, easily available in raw materials, good in stability and convenient to store and use, can be specifically combined with RNA and generate strong fluorescence response, is suitable for real-time detection and imaging of in-vitro and in-vivo mitochondrial RNA, and is an efficient mitochondrial RNA micromolecular fluorescent probe.

The present invention relates to pharmaceutical compositions containing N-(1,3-dimethylpyrazol-4-yl)sulfonyl-6-[3-(3,3, 3-trifluoro-2,2-dimethyl-propoxy)pyrazol-1-yl]-2-[(4S)-2,2,4-trimethylpyrrolidin-1-yl]pyridine-3-carboxamide, a solid dispersion of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-7V-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-en indol-5-yl)cyclopropanecarboxamide, and a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-quinoline-3-carboxamide, including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical compositions.

The invention provides a fullerene pyrrolidine enantiomer mediated cholesteric liquid crystal with circular polarization luminescence property and nonlinear anti-saturated absorption property, and a preparation method and application thereof. The method comprises the following steps: dissolving C60, paraformaldehyde and (R / S)-(+ / -)-alpha-methylbenzylamine in an organic solvent, and carrying out heating reflux reaction to obtain fullerene pyrrolidine enantiomer molecules; dissolving in carbon disulfide to obtain an enantiomer solution; dissolving achiral dye molecules in a solvent to obtain a dye solution; and dropwise adding the enantiomer solution and the dye solution into thermotropic liquid crystal molecules, and drying to obtain the thermotropic liquid crystal. The method is simple, the obtained cholesteric liquid crystal system shows a characteristic fingerprint texture and has a periodic spiral structure, and the doping proportion of chiral molecules is easy to adjust; the composite system has good time stability and is not prone to phase separation; the liquid crystal platform shows good circular polarization luminescence performance and third-order nonlinear optical property, and is a cholesteric liquid crystal platform with an integrated function.

The invention discloses an extraction head and a method for detecting organochlorine pesticides in water by using the extraction head. According to the preparation method, 4-hydroxycarbazole is taken as a functional monomer for electro-polymerization, (benzotriazole-1-yloxy) dipyrrolidine carbon hexafluorophosphate ionic liquid (IL) is taken as a doping medium, and the composite extraction coating is obtained in an electrochemical co-deposition mode. The polymerization 4-Hydroxycarbazole-IL (HBPyU) with the ionic liquid concentration of 25 mu g / mL, the salt solution of 35% saturated sodium chloride solution, the stirring rate of 600 r / min, the extraction temperature of 50 DEG C and the extraction time of 30 min is used as an optimal extraction head, and organochlorine pesticides Hepache and Quintozene in water are analyzed and detected. Therefore, according to the technical scheme, compared with an extraction head only provided with a monomer, the coating material added with the ionic liquid has the best extraction capacity on an analyte, and the beneficial effects of high efficiency and high sensitivity are achieved.

The application discloses a kind of ultraviolet absorber with triazine ring as main structure and its preparation method and its application in aramid fiber, the ultraviolet absorber has the following structural formula: Wherein, R1, R2, R3, R4 It is the group containing phenyl or substituted phenyl, R5 It is piperidyl, piperazyl, pyrrolidinyl and one of the following structures:This ultraviolet absorber has good absorption to UVA-UVB band ultraviolet, especially in 290~320 nm range has good ultraviolet absorption, adding the ultraviolet absorber in aramid fiber can significantly improve its weather resistance and service life, keep mechanical property, delay ultraviolet degradation, reduce the direct damage of fiber.

The technology herein provides various embodiments that relate to a method of treating pulmonary hypertension in a subject in need thereof, comprising administering to the subject an effective amount of BX-912 (N-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]-2-pyrimidinyl]amino]phenyl]pyrrolidine-1-carboxamide).

The invention discloses weather-resistant and medium-resistant alkyd resin varnish and a preparation method thereof. The varnish is prepared from the following raw materials: modified alkyd resin, a composite drier, zirconium iso-octoate with the purity of 12%, an anti-skinning agent, 200 # solvent oil and xylene. The modified alkyd resin is prepared from the following raw materials: soya oil acid, pentaerythritol, benzoic acid, pyrrolidine-2-one-1-acetic acid, dimethylbenzene and a 200 # solvent. According to the invention, pyrrolidine-2-ketone-1-acetic acid is used as a binary acid component to partially or completely replace traditional phthalic anhydride, so that the reaction efficiency of alkyd resin synthesis can be improved, and the problems of yellowing, pulverization and poor water resistance of traditional alkyd resin can be solved; according to the varnish prepared by the invention, on the basis of maintaining the inherent gloss, flexibility and constructability of alkyd resin, the key properties such as weather resistance, water resistance and acid resistance are improved; the whole preparation process of the varnish continues to use mature alkyd resin production equipment and flow, and has good economical efficiency and industrial popularization prospects.

An aerosol generating material for use in an aerosol delivery device is provided, the aerosol generating material including a fibrous plant material, an aerosol former, and an active agent including at least a substituted 3-(1-methylpyrrolidin-2-yl)pyridine, a 3-(azetidin-2- yl)pyridine, or a 3-(azetidin-2-ylmethoxy)pyridine. The active agent is absorbed or adsorbed in or on the fibrous plant material. The disclosure further provides devices and aerosol provision systems incorporating such aerosol generating material.

This invention discloses a chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups, with the following structural formula: The preparation includes the following steps: 1. Sequentially adding a metal catalyst, a chiral ligand, a base, indigo-derived trifluoromethylimine ylide, and 3-methylene β-lactam, followed by the addition of an organic solvent to obtain a mixture. The mixture is stirred at a reaction temperature of 0℃ to 50℃. 2. After the reaction is complete, the chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups is obtained through post-processing. The chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups prepared in this application lays a material foundation for in-depth drug activity research based on new drug development.

The present invention relates to a new process for the preparation of (3R)-3-fluoropyrrolidine hydrochloride or an acceptable salts thereof via a N-Boc-(3S)-3-hydroxypyrrolidine intermediate. The process is suitable for the synthesis of N-Boc-(3S)-3-hydroxypyrrolidine at technical scale in high, not less than 99.85%-a / a optical purity and a purity of not less than 99.8%-a / a. The high quality N-Boc-(3S)-3-hydroxypyrrolidine can be converted to (3R)-3-fluoropyrrolidine hydrochloride exhibiting an optical purity of not less than 99.95%-a / a and a purity of not less than 99.5%-a / a thus making it a suitable intermediate for manufacturing of pharmaceutical active compounds.

The application discloses a preparation method of 1-(2-aminoethyl) pyrrolidine and belongs to the field of chemical synthesis. The application provides a novel synthesis method of 1-(2-aminoethyl) pyrrolidine, which is prepared from 1,2-dichloroethane and pyrrolidine as raw materials, addition of a solvent and alkali, heating reaction, extraction, acidification and reduced-pressure distillation after the reaction is finished to obtain N-(2-chloroethyl) pyrrolidine solution; N-(2-chloroethyl) pyrrolidine and ammonia water are used as raw materials, high-pressure heating reaction is carried out, extraction and reduced-pressure distillation are carried out after the reaction is finished to generate 1-(2-aminoethyl) pyrrolidine. The application has the advantages of simple operation process, green process synthesis, convenient product purification and high product purity.

Use of a composition containing a 5-oxo-pyrrolidine-2-carboxylic acid derivative with formula IIa for the fixation and optional preservation of biological organs and / or tissues and / or whole body specimens and / or corpses.

The present invention relates to compounds of formula (I) or formula (II) or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein said compound of formula (I) and said compound of formula II each comprises at least one ONO2 or ONO moiety; R1 is C1-C3alkyl; R2 is H, C1-C6alkyl, C3-C6cycloalkyl, C1-C2alkoxy, C2-C4alkenyl; R3 is C1-C4alkyl optionally substituted with C1-C2alkoxy, C3-C4cycloalkyl, C2-C4alkenyl; R4 and R5 are each independently H or C1-C6alkyl optionally substituted with F, OH, ONO, ONO2, COOH, C1-C3alkoxy, C3-C6cycloalkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine, homo-piperazine, 2,5-diazabicyclo[2,2,1]heptane and 3,7-diazabicyclo[3,3,0]octane, wherein said heterocyclic ring is optionally substituted with independently one or more R6; R6 is C1-C6alkyl optionally substituted with independently one or more halogen, OH, ONO, ONO2, C1-C3alkoxy, C1-C3haloalkoxy, COOR7, NR8R9, C═NR10; R7 is H, or C1-C4alkyl optionally substituted with F, OH, ONO, ONO2, NR8R9; R8 and R9 are independently H, or C1-C4alkyl optionally substituted with ONO, ONO2; R10 is C1-C4alkyl optionally substituted with F, ONO, ONO2; C3-C6cycloalkyl; pharmaceutical compositions thereof, and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.

The invention relates to a compound of formula (I) wherein n = 1 or 2, A and A'are independently selected from the group consisting of the following substituents (II-a) and (II-b), R and R 'are independently selected from H and a linear or branched C1-C3 alkyl group, Z is selected from a linear or branched C1-C4 alkyl group and an aryl group optionally substituted by a linear or branched C1-C3 alkyl group and / or by a hydroxyl group, and the structural unit of formula (N) is selected from the following structural units (III-a), (III-b), (III-c), (III-d) and (III-e) wherein for each structural unit (III-a), (III-b), (III-c), (III-d) and (III-e), Ra, Rb, Rc and Rd are independently selected from a linear or branched C1-C4 alkyl group. .

Aerosol generating articles adapted for use in an aerosol delivery device are provided. The aerosol generating articles include an aerosol generating material and an aerosol-modifying agent, wherein the aerosol-modifying agent includes a substituted 3-(1-methylpyrrolidin-2- yl)pyridine, a 3-(azetidin-2-yl)pyridine, or a 3-(azetidin-2-ylmethoxy)pyridine. The disclosure further provides devices incorporating such aerosol generating articles.

The invention discloses a battery monomer, an isolating membrane, a preparation method of the isolating membrane, a battery device and a power utilization device, the battery monomer comprises the isolating membrane and electrolyte, and the isolating membrane comprises a porous base membrane; the coating is arranged on at least one side of the porous base membrane and comprises a polymer additive, and the polymer additive comprises a first functional group and a second functional group; the first functional group comprises one or more of bis (fluorosulfonyl) imino group, bis (trifluoromethyl) sulfonyl imino group, trifluoroboric acid group, hexafluorophosphoric acid group, sulfonic acid group, hexafluoroarsenate group, trifluoromethanesulfonic acid group, difluorophosphoric acid group, bis (oxalato) boric acid group, difluoro (oxalato) boric acid group, difluoro (oxalato) phosphoric acid group, tetrafluoro (oxalato) phosphoric acid group and imidazolyl; the second functional group comprises one or more of quaternary ammonium ions, pyrrolidinyl, pyrrolyl, piperidinyl, pyridyl and imidazolyl. The battery monomer has good dynamic performance; the invention provides the isolating membrane for realizing the beneficial effects of the battery monomer, the preparation method of the isolating membrane, the battery device and the power utilization device.

The invention belongs to the field of organic chemical synthesis, and relates to a method for preparing butanediamine and co-producing pyrrolidine by using butanedinitrile, which comprises the following steps: S1, reacting acrylonitrile with hydrocyanic acid in a fixed bed reactor filled with a first catalyst to obtain butanedinitrile; the first catalyst is filled in a fixed bed reactor in a solid form, and the first catalyst comprises a carrier and an active component loaded on the carrier. And S2, dissolving the butanedinitrile obtained in the step S1 into a pyrrolidine ionic liquid solvent, then adding a second catalyst and alkali, then introducing hydrogen, and reacting to obtain butanediamine and pyrrolidine. According to the method, continuous and easy-to-separate production of butanedinitrile is realized, a by-product is directionally converted into tetrahydropyrrole with a high added value through a specific reaction system, and the safety, the economical efficiency and the resource utilization rate of the process are remarkably improved.

The present disclosure provides a novel solid crystalline form of isopropyl ((11S,12S,13S,9S,12S)-9-amino-12-((1-(6-aminohexyl)-5-fluoro-1H-indol-3-yl)methyl)-4,10,13-trioxo-2-oxa-5,11-diaza-1(3,1)-pyrrolidina-7(1,3)-benzenacyclotridecaphane-12-carbonyl)-L-threoninate (Compound 1), or pharmaceutically acceptable salt thereof, compositions comprising Compound 1 (Form 1A and / or Form 2) synthesis thereof, and an improved crystallization process using Form 2 to prepare Form 1. Novel compositions also include Compound 1 solid Form 1, Form 2 and / or other crystalline and amorphous solid forms of Compound 1.

The invention discloses a high-regeneration-performance absorption liquid for capturing carbon dioxide and a preparation method and application thereof, and relates to the technical field of gas separation and purification, the high-regeneration-performance absorption liquid comprises a main absorption component, an auxiliary absorption component, an active component, an antioxidant, an auxiliary agent and water. According to the absorption liquid provided by the invention, the antioxidant 2, 6-di-tert-butyl-4-methoxyphenol with a specific structure and the auxiliary agent 1-isopropyl-3-pyrrolidinol are introduced and are synergistically combined with the main absorption component, the auxiliary absorption component, the activation component and the solvent water, so that the absorption liquid shows excellent absorption and desorption rate and low-temperature capture performance in a CO2 capture process; the method can obviously reduce the trapping energy consumption and improve the trapping efficiency, so that the operation cost is reduced, and the method is suitable for trapping treatment of CO2-containing waste gas.

This invention relates to the field of organic synthesis technology, specifically to a polyhydroxypyrrolidone ether compound, its preparation method, and its application. The structure of the polyhydroxypyrrolidone ether compound is shown in formula (1), and each group in formula (1) has a specific selection; the stereoconfiguration of the carbon atoms at positions 2, 3, and 4 in formula (1) is "2R,3R,4R" or "2S,3S,4S". The polyhydroxypyrrolidone ether compound of this invention and its pharmaceutically acceptable salts exhibit excellent selectivity and strong inhibitory effects on β-glucosidase, and are suitable for the prevention or treatment of Gaucher's disease and Parkinson's syndrome. Formula (1), Formula (2).

The presently claimed invention relates to an alkaline composition for cleaning a substrate comprising i) copper or copper alloy and ii) cobalt or cobalt alloy, the composition comprising: a) at least one pH adjustor selected from diglycolamine, 4,4-diethoxy-N,N-dimethyl-1-butanamine, 3-dimethylaminopropan-1-ol, dimethylaminoethoxyethanol, N,N-dimethylisopropanolamine, ethylethanolamine, N-methyldiethanolamine, 2-(2-(methylamino)ethoxy)ethanol, 3-(methylamino)propane-1,2-diol, 2-[2-[2-(2-methoxy- ethoxy)ethoxy]ethoxy]ethylamine, 2-[2-(2-aminoethoxy)-ethoxy]-ethanol, N-butyldiethanolamine, diisopropanolamine, N-methyldiisopropanolamine, monoethanolamine, 3-dimethylamino-1,2-propandiol, 2- amino-1-butanol, 2-(2-(2-(2-aminoethoxy)ethoxy)ethoxy)ethanol, prolinol, 1-methyl-2-pyrrolidinemethanol, 1-methyl-2-pyrrolidinemethanol, 1-methyl-3-pyrrolidinol, 2-amino-2-methyl-1-propanol, N,N-dimethylethanolamine, butylethanolamine, diethylethanolamine, 3-methoxypropylamine, 4-(2-hydroxyethyl)morpholine, 4-(dimethylamino)cyclohexanol, 2-amino-2-methyl-1, 3-propanediol, or diisopropylamine; b) at least one complexing agent selected from C2 to C12 hydrocarbon having at least two sulfonic acid or carboxylic acid groups; c) at least one polymeric dispersing agent having a weight average molecular weight ≥ 1000 g / mol; and d) a solvent comprising water.

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 discloses a pyrrole polymer electrolyte film in an energy storage lithium battery and a preparation method and application thereof, and belongs to the polymer electrolyte field. The method comprises the following steps: reacting 1-methyl pyrrolidine and bromine n-butane to prepare 1-methyl-1-butyl pyrrolidine bromide; preparing 1-methyl-1-butyl pyrrolidine difluoromethane sulfonimide salt ionic liquid by mixing the 1-methyl-1-butyl pyrrolidine bromide and lithium difluoromethane sulfonimide; mixing 1-methyl-1-butyl pyrrolidine difluoromethane sulfonimide salt ionic liquid, polyethylene glycol methyl ether methacrylate, acrylonitrile, lithium bistrifluoromethanesulfonimide, divinylbenzene and benzoin ethyl ether uniformly, coating and curing to obtain a pyrrole ionic liquid polymer electrolyte film. The application combines the molecular configuration of the pyrrolidine-based ionic liquid and the topological structure of the polymer network, realizes triple optimization of ion transmission-mechanical strength-interface stability.

A chemical synthesis method for the Klebsiella toxin Tilimycin relates to the field of biomedical chemical analysis and synthesis technology. The method includes the following steps: (1) mixing bis(trichloromethyl) carbonate dissolved in a polar aprotic solvent with 3-hydroxy-an-aminobenzoic acid in a certain proportion to undergo a substitution reaction, heating and stirring to obtain intermediate product 1; (2) mixing intermediate product 1 with (S)-2-pyrrolidone dissolved in a polar aprotic solvent in a certain proportion to undergo ammonolysis and hydrolysis reactions, heating and stirring, filtering, and purifying by prep-HPLC to obtain intermediate product 2; (3) mixing intermediate product 2 with pyridine sulfur trioxide dissolved in a polar aprotic solvent and DCM in a certain proportion under alkaline conditions to undergo oxidation and amination reactions, stirring at low temperature, vacuum drying, and purifying by prep-HPLC to obtain the target compound Tilimycin. This invention enables the efficient synthesis of the Klebsiella toxin Tilimycin with high purity and good stability, thus providing a material basis and technical method for scientific research related to this toxin.

This invention relates to the prevention and / or treatment of protein tyrosine kinase-mediated diseases, particularly phosphatidylinositol 3-kinase (PI3Ks)-mediated diseases. PI3Ks are well known as oncological targets, and several PI3K inhibitors have been developed that inhibit numerous class 1A PI3K isoforms. The development of selective inhibitors of PI3K-α may enable sufficient targeted inhibition while avoiding some of the known toxic drawbacks of pan-PI3K inhibitors. The inventors have discovered that a novel carbamoti-oil-pyrrolidine-carboxamide compound of formula (I) exhibits advantageous PI3K inhibitory activity, particularly with high selectivity for the isoform PI3K-α. In particular, this invention relates to the compound of formula (I), or deuterated or tritiated forms of the compound of formula (I), and pharmaceutically acceptable salts thereof. [Formula 1] The present invention also relates to pharmaceutical compositions containing a compound of formula (I) for use in the treatment and / or prevention of protein tyrosine kinase-mediated diseases, and to a compound of formula (I).

This invention provides an N,N-diethylpyrrolidine difluorosulfonylimide salt, its preparation method, and its applications, belonging to the field of ionic liquid materials technology. The preparation method of the N,N-diethylpyrrolidine difluorosulfonylimide salt of this invention includes the following steps: reacting potassium carbonate solution, tetrahydropyrrole, and bromoethane in an inert atmosphere; then dissolving the reaction product in an organic solvent, filtering, and evaporating to obtain N,N-diethylpyrrolidine bromide; dissolving the N,N-diethylpyrrolidine bromide in water, adding activated carbon for decolorization treatment, to obtain an aqueous solution of N,N-diethylpyrrolidine bromide; and subjecting the aqueous solution of N,N-diethylpyrrolidine bromide to an ion exchange reaction with lithium difluorosulfonylimide in an organic solvent to obtain the final product. The preparation method of this invention separates the reaction product and byproduct into liquid and solid phases, and the reaction does not introduce other impurity ions, greatly improving the purity of the product.

The present invention provides solid forms of (3R)-N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide, salts and solvates thereof, as well as therapeutic uses thereof and pharmaceutical compostion comprising them.

This invention relates to a pyrrolidine derivative and its pharmaceutical use, and more particularly to a pyrrolidine derivative as shown in general formula (I), or its stereoisomers, solvates, metabolites, prodrugs, pharmaceutically acceptable salts or cocrystals, pharmaceutical compositions comprising the thereof, and the use of the compounds or compositions of this application in the preparation of medicaments for autoimmune diseases.

This invention discloses a method for preparing raloxifene EP impurity B, comprising the following steps: dissolving 6-methoxy-2-(4-methoxyphenyl)benzothiophene (Ⅰ) as a raw material in solvent one, adding NIS, and then adding a free radical initiator to react and obtain intermediate III; dissolving 4-[2-(1-pyrrolidinyl)ethoxy]benzoate salt (II) in solvent two, adding solvent two or not, and then adding a chlorinating agent to react and generate intermediate IV; dissolving intermediate III in solvent three, adding a Lewis acid, and then adding intermediate IV, and performing a Friedel-Crafts acylation reaction to generate intermediate V; dissolving intermediate V in solvent four, adding a demethylating agent, and generating bisphenol hydroxyl intermediate VI under demethylation conditions; dissolving intermediate VI in solvent five, adding a reducing agent, and generating intermediate VII through a reduction reaction; dissolving intermediate VII in formic acid, stirring, evaporating, and finally lyophilizing to generate the formate target product VIII.

The present application provides a new crystalline form of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and a method for preparing the same. The new crystalline form is a hydrate, designated as Form H, which has better solubility and thermal stability. These properties can improve the crystal form stability of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide under high temperature granulation conditions in its formulation process, and can improve its bioavailability in the human body to some extent.