31 results about "Cyclopentamine" patented technology

The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and / or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

The invention discloses a ruthenium polypyridyl complex using quinolones compound as ligand, a preparation method and application thereof. The constitutional formula of the complex is as shown in a formula (I), wherein R1 denotes alkyl, substituted alkyl, naphthenic base, substituted naphthenic base, aryl or substituted aryl; R2 denotes ethyl or cyclopropyl; R3 denotes hydrogen or amido; R4 denotes hydrogen, fluorine, chlorine, cyan or amido; R5 denotes methyl, piperazinyl, cyclopentylamino, dimethylamino, methyl, halogen or hydrogen; R6 denotes hydrogen, fluorine or forms a hexatomic ring together with R1 through carbon atoms and oxygen atoms in a bonding way; R7 denotes hydrogen or methyl; R8 and R9 denote hydrogen or form a benzene ring through carbon atoms in a bonding way; and X and Y denote carbon atoms or nitrogen atoms. The invention uses quinolones compound as ligand and ruthenium polypyridyl group as active group to prepare medicine for curing tumors or antibacterial medicine, and has good antibacterial effect and bacteriostatic effect. Formula (1) is shown as the accompanying drawing.

An anticancer sustained-release gel injection sustained-release microspheres containing platinum-based compound, amphiphilic block copolymer, solvent and release regulator, the mixture of amphiphilic block copolymer and solvent has a temperature sensitive gelatinization characteristic, and can automatically become non-flowing degradable water insoluble gel, which can locally and slowly release drug at tumor foci for several weeks to several months, after injection into body. The adjuvant in the sustained-release microspheres is poly(lactic acid)-glycollic acid copolymer; and the amphiphilic block copolymer is PLGA-PEG-PLGA copolymer. The preparation can be injected into artery, inside a tumor or around a tumor with remarkably reduced systemic toxicity of drug, and can be used for solid tumors at different stages. The platinum-based compound is selected from nedaplatin, carboplatin, cisplatin, enloplatin, ormaplatin, sulfato-1,2-diaminocyclohezane-platinum (SHP), picoplatin, cyclopentylamine platium, zeniplatin, spiroplatin, lobaplatin, iproplatin, oxaliplatin, cycloplatin, and dexormaplatin. The preparation can be used with radioactive particles and can enhance chemotherapy effect.

The invention relates to the fields of pharmaceutical chemistry and pharmaceutical therapeutics, and provides an amino-substituted rutaecarpin analog, and a synthesis method and application thereof in the preparation of anti-obesity medicaments. Experiments prove that the amino-substituted rutaecarpin analog provided by the invention can obviously reduce the lipopexia of 3T3-L1 fat cells, and can reduce the high levulose-induced lipopexia of FAO rat liver cells. Cellular level tests show that the compound can reduce lipopexia and has an effect of relieving obesity and alleviating fatty liver. The chemical formula of the amino-substituted rutaecarpin analog is shown in the specification. In the chemical formula, R0 is -NH(CH2)nR2, n is 1, 2, 3, 4 or 5, and R2 is -N(CH3)2, -N(CH2CH3)2, cyclopentylamino or cyclohexylamino; or R0 is morpholinyl, piperazinyl or methylpiperazinyl.

The invention relates to platinum (IV) anticancer compounds with a dihydrogen phosphate radical as an axial ligand. The chemical structure of the compounds is shown in the description. In the structure, a carrier group 2A is an ammonia / amine liand, and comprises 2NH3, 1R,2R-cyclohexanediamin, 1,2-bis(aminomethyl)cyclobutane, NH3 / cyclopentamine and NH3 / cyclohexylamine; and leaving groups 2X are the leaving groups of platinum (II) anticancer compounds existing at present, and comprise 2Cl<->, an oxalate radical, a 1,1-cyclobutanedicarboxylate radical and a propane dicarboxylate radical. Phosphoric acid bonding is helpful for running of compounds to cancer cell nuclei, improving the selectivity of cancer cells, and makes the compounds mediate compound targeting osteocarcinoma and have very strong anticancer effect. The compounds have the advantages of good water solubility and stability, and are highly suitable for being used as anticancer drugs.

The present invention relates to a lubricating grease, which comprises base oil, 12-hydroxystearic acid, lithium hydroxide, potassium hydroxide, petroleum calcium sulfonate, rosin, vegetable oil, (NH4)xMoS2, a first solid additive, a second solid additive, a first composite modifier comprising trioctylmethylammonium bromide, glycerol and polytetrafluoroethylene, a second composite modifier comprising diphenylamine, 2,6-di-tert-butyl and benzotriazole, and a third composite modifier comprising sulfurized cottonseed oil T404, bis(2-mercapto-4-n-propylamino-1,3,5-triazine)thioether and bis(2-mercapto-4-cyclopentylamino-1, 3,5-triazine)thioether. The lubricating grease of the present invention has advantages of good sealing performance, strong corrosion resistance, excellent anti-wear performance, and excellent anti-extreme pressure performance.

The invention discloses a preparation method of a palbociclib intermediate. The method comprises the following steps: preparing 5-bromine-2-chloro-N-cyclopentylamine pyrimidine-4 amine from 5-bromine-2,4-dichloropyrimidine and cyclopentylamine by taking solvents such as dichloromethane and water as solvents and taking inorganic base as an acid-binding agent; with DIEA as an acid-binding agent, DMF as a solvent and TBAB as a phase transfer catalyst, in the presence of water, catalyzing with a trace amount of palladium, and carrying out normal hexane reflux dehydration; further subjecting the acetic anhydride to dehydration cyclization, such that 2-chloro-8-cyclopentyl-5-methylpyridino[2,3-D]pyrimidine-7-(8H)-ketone is obtained; and reacting the obtained compound with NBS (N-bromosuccinimide) in acetonitrile to obtain the 6-bromo-2-chloro-8-cyclopentyl-5-methylpyridino[2, 3-D]pyrimidine-7(8H)-ketone. The method is mild in reaction, simple and convenient to operate, recyclable in solvent, less in environmental pollution, high in yield, low in cost, high in product quality and suitable for industrial production.

The invention discloses methods for preparing 3-cyclopentamine and slats thereof. The method for preparing the 3-cyclopentamine comprises the following steps of: adding cis-1,4-dichloro-2-butene and nitromethane serving as initial raw materials into a solvent to perform a reaction in the presence of an alkaline catalyst and at the temperature of 25 to 80 DEG C to obtain 4-nitro-cyclopentyl-1-alkenyl; and reducing the 4-nitro-cyclopentyl-1-alkenyl in a reduction system to obtain the 3-cyclopentamine. The new process provided by the invention reduces the course for synthesizing the target product to a relatively large extent, successfully solves the problems of high-price, rareness and the like of the raw materials of the target product and avoids a diazotization reaction at the same time. The new process greatly reduces production cost, improves yield and product purity and is simple in operation and convenient for mass production.

The invention belongs to the technical field of biomedicine, and particularly relates to a cyclohexane amine D3 / D2 receptor partial agonist, and a pharmaceutically acceptable salt, a synthesis methodand use of the cyclohexane amine D3 / D2 receptor partial agonist. According to the cyclohexane amine D3 / D2 receptor partial agonist, compared with the prior art, N-fluorocycloaminoformoxyl linked by cyclopentamine in a molecular structure has stronger metabolic stability than that of original N,N-dimethyl carbamoyl group, and time of action in drug bodies is prolonged. The introduction of fluorocycloamino changes the physical and chemical properties of original molecules, thus changing pharmacokinetic properties, the distribution of drugs in target tissues is enhanced, and the bioavailability of the drugs is improved. The inventors further surprisingly find that the introduction of the fluorocycloamino affects the local conformation of compounds, enhances mutually binding ability between ligands and target protein, and improves the selectivity of target spots.

Relating to the technical field of drugs, the invention provides an industrial preparation process of a palbociclib intermediate 5-bromo-2-chloro-4-cyclopentyl aminopyrimidine (M1). The process comprises the steps of: (1) under a room temperature condition, selecting a weak alkaline inorganic salt as an acid-binding agent, adopting a low-boiling point solvent as the reaction solvent, adding cyclopentylamine dropwise into 2, 4-dichloro-5-bromopyrimidine (M0), and carrying out reaction for 12-15h; (2) performing pumping filtration to remove inorganic salt, concentrating mother liquor to dry, andrecrystallizing the residue with a solvent of little polarity to obtain the intermediate M1, with the reaction formula shown as the specification. The preparation process provided by the invention has the advantages of simple operation steps, mild reaction conditions and simpler post-treatment needed by reaction, greatly improves the product yield and purity, effectively reduces the generation of2-substituted impurities, and is of great significance for promotion of palbociclib technology and better application to clinical patients.

The invention discloses a low temperature cured acrylic ester electrostatic flocking adhesive. The low temperature cured acrylic ester electrostatic flocking adhesive comprises, by mass, 35 to 45 parts of methyl methacrylate; 0.5 to 2 parts of a hydroxymethyl free active monomer; 1 to 1.5 parts of peregal O-25, 0.5 to 2 parts of sodium dodecyl sulfate SDS, 1 to 3 parts of potassium sulfate; 0.3 to0.8 part of ethyl acrylate; 0.5 to 2.5 parts of p-methoxyphenol, 0.02 to 0.05 part of cyclopentylamine, and 20 to 45 parts of deionized water. The preparation method comprises following steps: A, emulsion preparation; and B, polymerization; an emulsion prepared in the step A is divided into two parts, one part is stored for further using, and the other part is added into a potassium persulfate aqueous solution, an obtained mixture is stirred and heated to 70 to 85 DEG C, 2.0 to 3.5h later, an obtained system is heated continuously, when the color of an obtained reaction product is changed, the stirring speed is slowed down, the left emulsion prepared in the step A is added, the potassium persulphate aqueous solution, and cyclopentamine are added, an obtained product is stirred, is subjected to constant temperature treatment for 1 to 2h, and is subjected to natural cooling, neutralizing, and filtering so as to obtain a polymer emulsion. The advantages are that the release of formaldehyde is reduced, drying time is shortened, and the curing temperature is reduced.

The invention discloses an organic-inorganic hybrid molecular ferroelectric material which is of a crystal structure, the molecular general formula of the crystal is [CPA] 2CuBr4 (CPA = cyclopentylamine cation), an asymmetric unit is composed of two [CPA] < + > cations and a distorted [CuBr4] < 2-> anion, the crystal belongs to a monoclinic system Pna21 space group at the room temperature of 293 K, and is crystallized in a Pnma space group of an orthorhombic system at the room temperature of 395 K, the Curie temperature 393K exceeds that of most molecular ferroelectric, and the Curie temperature 393K can be comparable with that of a commercial ferroelectric BaTiO3 (393K); the crystal is prepared by adopting a solution volatilization method, the process is simple, the repeatability is high, and the crystal structure is stable. The molecular ferroelectric material shows excellent reversible dielectric properties and ferroelectricity, and can be applied to the fields of information storage, solar energy storage, sensors, variable capacitors, intelligent switches and the like.

The invention discloses a 3,5-disubsitutued 2-amino-pyrazine compound. The compound has the structure shown in the formula I; in the formula I, NR1R2 is n-propylamino, cyclopropylamino, cyclopentylamino, cyclohexylamino, morpholinyl, 4-methyl piperazine, anilino, 4-chloroaniline or 3-chloroaniline; Ar is 3,5-dimethyl-isoxazolyl-4 or 1-methyl-1H-pyrazolyl-4; and the invention further provides the preparation technology and application thereof. The compound has the outstanding inhibiting effect on growth of four kinds of cancer cells including a human cervical cancer cell HeLa, a human brain glioma cell U87, a human hepatoma cancer cell HepG2 and a human colon cancer cell LoVo, wherein a large part of the compound has an obviously higher inhibiting effect on proliferation of the cancer cellsthan positive control VX-680, particularly the compound Ih and Ii have relatively high activity on the four kinds of cancer cells, and have prominent activity inhibiting effect on aurora kinase A andaurora kinase B, and therefore the compound can be applied to preparation of anti-cancer drugs.

The invention discloses methods for preparing 3-cyclopentamine and slats thereof. The method for preparing the 3-cyclopentamine comprises the following steps of: adding cis-1,4-dichloro-2-butene and nitromethane serving as initial raw materials into a solvent to perform a reaction in the presence of an alkaline catalyst and at the temperature of 25 to 80 DEG C to obtain 4-nitro-cyclopentyl-1-alkenyl; and reducing the 4-nitro-cyclopentyl-1-alkenyl in a reduction system to obtain the 3-cyclopentamine. The new process provided by the invention reduces the course for synthesizing the target product to a relatively large extent, successfully solves the problems of high-price, rareness and the like of the raw materials of the target product and avoids a diazotization reaction at the same time. The new process greatly reduces production cost, improves yield and product purity and is simple in operation and convenient for mass production.

The invention provides 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine and a preparation containing 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine and a pharmaceutic adjuvant. 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine maleate is a derivate of cinepazide, and experiments verify obvious pharmacological effect thereof. The invention concretely provides two injections of the compound, namely solution type and liposome type injections and preparation processes thereof. The solution type injection contains 30-45g of the compound, 20-30g of D-sorbierite, 2-3.5g of disodium hydrogen phosphate and an appropriate amount of water for injection. The preparation method of the solution type injection comprises the following steps: adding the D-sorbierite into water to be dissolved, adding the derivate into the D-sorbierite solution, stirring to partly dissolve the derivate, adding partial disodium hydrogen phosphate solution to completely dissolve the derivate, then regulating the pH value, and filtering, thus the injection preparation is obtained. The liposome type injection contains 1g of the derivate, 1-13g of phospholipid and 0.6-6g of cholesterol. The invention provides a compound with obvious pharmaceutical effect and also provides two safe and stable formulations of the compound and preparation methods thereof.

The invention relates to the field of drug synthesis, in particular to a preparation method of a palbociclib intermediate. In the preparation method of the present invention, compound I: 2,4-dichloropyrimidine is used as the starting material, replaced by cyclopentylamine, and transesterified with methyl acetoacetate, and then catalyzed by boron trifluoride ether The target compound IV is obtained by ring closure: 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-D]pyrimidinyl-7-one. The synthetic route designed by the invention avoids the use of palladium catalyst, the overall reaction conditions are mild, the reaction yield is high, the production cost is low, it is suitable for industrial production and is environmentally friendly.

The invention relates to the field of medicine synthesis, in particular to a preparation method of a palbociclib intermediate. According to the preparation method, a compound I, namely 2,4-dichloropyrimidine is used as an initial raw material, and is subjected to substitution by cyclopentylamine, amine ester exchange with methyl acetoacetate and catalytic cyclization by boron trifluoride diethyl ether so as to obtain a target compound IV, namely 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-D]pyrimidinyl-7-one. The synthesis route designed by the invention avoids the use of a palladium catalyst, has the advantages of mild overall reaction conditions, high reaction yield and low production cost, is suitable for industrial production, and is green and environment-friendly.

Cycloalkylamine derivatives may be used for preventing or treating diseases in humans, animals, and have demonstrated efficacy specifically in treating type 2 diabetes. In an embodiment, the cycloalkylamine derivatives can include a compound selected from the group consisting of cycloheptanamine salts, cyclohexanamine salts, cyclopentanamine salts 1-cycloheptyl-[4,4′-bipyridin]-1-ium, N1,N2-dicycloheptyloxalamide, 1-[3′,5′-bis(trifluoromethyl)phenyl]-3-cycloheptylurea, 1,1′-(4-methyl-1,3-phenylene)bis(3-cycloheptylurea), 1-(2′-aminopyrimidin-4′-yl)-3-cycloheptylurea, 4-amino-N-(cycloheptylcarbamoyl)benzenesulfonamide, 4-(3′-cycloheptylureido)-N-(5″-methylisoxazol-3″-yl)benzenesulfonamide, N-(cycloheptylcarbamoyl)-4-methylbenzenesulfonamide, 1-cycloheptylguanidine hydrochloride, (E)-amino[(amino(cycloheptylamino)methylene)amino]methaniminium chloride, or a pharmaceutically acceptable salt thereof.

The invention discloses a preparation method of a palbociclib intermediate, and belongs to the field of chemical synthesis. The method specifically comprises the following steps: a) carrying out a substitution reaction on 5-bromine-2, 4-dichloropyrimidine and cyclopentylamine under the condition of taking organic alkali as a solvent to obtain 5-bromine-2-chloro-4-cyclopentylaminopyrimidine; and b) under the condition of an organic solvent, adding a palladium catalyst, polyethylene glycol, organic alkali, 5-bromine-2-chloro-4-cyclopentyl aminopyrimidine and butenoic acid to carry out a heck reaction, and after the reaction is completed, adding acetic anhydride to carry out dehydration and ring closing to obtain the intermediate 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2, 3-d] pyrimidine-7-ketone. The organic alkali is used as the solvent in the step a), the reaction system is simpler, the reaction time is short, and the yield is higher. In the step b), polyethylene glycol is used as a palladium catalyst ligand to replace a traditional expensive phosphine ligand, so that the reaction time is shortened, the reaction effect is better, and acetic anhydride can be directly added for dehydration and ring closure without treatment.

The invention discloses a ribociclib intermediate preparation method, which comprises: (1) mixing a compound I, iodine, a catalyst A and a solvent A, heating to a temperature of 70-80 DEG C, and carrying out a heat preservation reaction for 5-6 h to generate a compound II; (2) mixing the compound II, phosphorus oxychloride and alkali B, and reacting to generate a compound III; (3) dissolving the compound III and alkali C in a solvent C, cooling to-10-0 DEG C, dropwise adding a mixed solution of cyclopentylamine and the solvent C, and reacting for 1-5 hours after dropwise adding to obtain a compound IV; (4) under the protection of inert gas, adding the compound IV, propargyl alcohol, a palladium catalyst, alkali D, a ligand and an activating agent into a solvent D, and carrying out Sonogashira coupling reaction for 5-10 hours to obtain a compound V; the method is mild in reaction condition, high in reaction yield, high in operability, low in production cost, green, environmentally friendly and suitable for large-scale industrial production.

The invention provides a simple preparation method of palbociclib. The method comprises the steps: performing dehydration on an acetacetate under the action of an acid catalyst so as to prepare 2-acetyl-3-methyl-2-pentenediate diester (II), then performing amidation condensation on the 2-acetyl-3-methyl-2-pentenediate diester (II) and cyclopentylamine so as to prepare 3-acetyl-1-cyclopentyl-4-methylpyridine-2,6-(1H,5H)-dione (III), then performing condensation on 3-acetyl-1-cyclopentyl-4-methylpyridine-2,6-(1H,5H)-dione (III) and a methylenation reagent so as to prepare 3-acetyl-1-cyclopentyl-4-methyl-5-dialkylaminomethylenepyridine-2,6-(1H,5H)-dione (IV), then performing a pyrimidine cyclization reaction on the 3-acetyl-1-cyclopentyl-4-methyl-5-dialkylaminomethylenepyridine-2,6-(1H,5H)-dione (IV) and N-[5-(4-tert-butoxycarbonylpiperazin-1-yl)pyridin-2-yl]guanidine (V) so as to obtain Boc-protected palbociclib (VI), and removing a Boc protecting group so as to obtain the palbociclib (I). The method has the advantages of a short process, simple operation, easy realization, low cost, less waste, high product purity and high yield.

The invention discloses a preparation method of a palbociclib intermediate, which uses 5-bromo-2,4-dichloropyrimidine and cyclopentylamine, uses dichloromethane and other solvents and water as solvents, and uses inorganic bases as acid-binding Preparation of 5-bromo-2-chloro-N-cyclopentaline-4 amine, then DIEA is used as an acid-binding agent, DMF is a solvent, and TBAB is a phase transfer catalyst. In the presence of water, a small amount of palladium is used to catalyze, Through normal hexane reflux dehydration, further dehydration ring closure of acetic anhydride obtains 2-chloro-8-cyclopentyl-5-picoline [2,3-D] pyrimidin-7 (8H)-one, the obtained compound is in acetonitrile In reaction with NBS, 6-bromo-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-D]pyrimidin-7(8H)-one is obtained. The method has the advantages of mild reaction, simple and convenient operation, reusable solvent, less environmental pollution, high yield, low cost and high product quality, and is suitable for industrialized production.

The invention belongs to the technical field of rubber and plastic products, and provides a DOP-free rubber and plastic product. The DOP-free rubber and plastic product comprises, in parts by mass, 15-20 parts of nitrile rubber, 5-7 parts of polyvinyl chloride resin, 3-5 parts of a ethylene-vinyl acetate copolymer, 20-30 parts of talcum powder, 13-15 parts of chlorinated paraffin oil, 1-2 parts ofepoxidized soybean oil, 2-4 parts of protective wax, 3-5 parts of white carbon black, 0.2-0.3 part of an active agent, 0.1-0.3 part of stearic acid, 10-20 parts of a flame retardant, 0.1-0.3 part ofan anti-aging agent, 1-3 parts of an accelerant, 0.1-0.3 part of a vulcanizing agent, 0.5-1 part of EDDHA-Na, 0.8-1.2 parts of sodium diamyl sulfosuccinate, 1-2 parts of di-n-butylamine and 1-1.5 parts of cyclopentylamine. By means of such a technical scheme, the problem that DOP-free rubber is poor in comprehensive performance in the prior art is solved.

The invention relates to platinum (IV) anticancer compounds with a dihydrogen phosphate radical as an axial ligand. The chemical structure of the compounds is shown in the description. In the structure, a carrier group 2A is an ammonia / amine liand, and comprises 2NH3, 1R,2R-cyclohexanediamin, 1,2-bis(aminomethyl)cyclobutane, NH3 / cyclopentamine and NH3 / cyclohexylamine; and leaving groups 2X are the leaving groups of platinum (II) anticancer compounds existing at present, and comprise 2Cl<->, an oxalate radical, a 1,1-cyclobutanedicarboxylate radical and a propane dicarboxylate radical. Phosphoric acid bonding is helpful for running of compounds to cancer cell nuclei, improving the selectivity of cancer cells, and makes the compounds mediate compound targeting osteocarcinoma and have very strong anticancer effect. The compounds have the advantages of good water solubility and stability, and are highly suitable for being used as anticancer drugs.

Disclosed herein is a process for the manufacture of 2-(aminomethyl)-1-cyclopentylamine by low-pressure hydrogenation of 1-amino-2-cyano-1-cyclopentene using a combination catalyst system of nickel with palladium on carbon, or a single palladium-doped Raney-type catalyst.

The present invention relates to the fields of pharmaceutical chemistry and pharmaceutical therapeutics. Provided are an amino-substituted rutaecarpin analog and a synthesis method and use thereof in the preparation of an anti-obesity drug. An experiment confirms that the amino-substituted rutaecarpin analog of the present invention can dramatically reduce the lipopexia of 3T3-L1 fat cells, and can reduce the high levulose-induced lipopexia of FAO rat liver cells. A cellular level experiment indicates that the compound can reduce lipopexia, relieve obesity and alleviate fatty liver. The amino-substituted rutaecarpin analog has a chemical formula (I), wherein R0=-NH(CH2)nR2, n=1, 2, 3, 4 or 5, and R2=-N(CH3)2, -N(CH2CH3)2, cyclopentylamino or cyclohexylamino; or R0= morpholinyl, piperazinyl or methylpiperazinyl.