284 results about "Piperazidine" patented technology

Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

The invention relates to preparation methods and uses of two dioxypiperazine compounds. The invention adopts aspergillus effuses H1-1 from root mud of Fujian mangrove forest to product novel structural dioxypiperazine compounds. Tests prove that: the compounds can be used as cellular breeding depressant or anti-tumor agent.

The present invention is the non-halogen flame-retardant synthetic resin composition characterized in that the said synthetic resin contains the (poly)phosphate compounds represented by the general formulae (1) and (3), described in Claim 1, and layered silicate;

• • n in the general formula (1) represents a number of 1˜100, X¹ is ammonia, or a triazine derivative represented by the general formula (2) described in Claim 1, p is a number satisfying the relational expression of 0<p≦n+2;
  • Z¹ and Z² in the general formula (2) are groups selected independently from groups consisting of a —NR⁵R⁶ group, a hydroxyl group or the like, and the above R⁵ and R⁶ are a hydrogen atom, an alkyl group having 1-6 carbon atoms, or a methylol group independently.
  • r in the general formula (3) represents a number of 1-100, Y¹ is a diamine containing a [R¹R²N(CH₂)mNR³R⁴], piperazine or a diamine containing a piperazine ring, R²˜R⁴ are a hydrogen atom, an alkyl group having 1-5 carbon atoms independently. m is an integer of 1-10, q is a number satisfying the relational expression of 0<q≦r+2.

The invention discloses a method for preparing piperaquine phosphate. 4,7-dichloroquinoline is taken as an initial raw material and is subjected to condensation reaction with anhydrous piperazidine first to obtain 7-chloro-4-(1-piperazinyl)quinoline, then the 7-chloro-4-(1-piperazinyl)quinoline is subjected to condensation reaction with 1, 3-bromochloropropane to obtain piperaquine, and finally the piperaquine is salified with phosphorous acid to obtain the piperaquine phosphate. The method has a simple process, is easy to purify intermediate products and a final product, has high product yield and good quality, avoids the use of toxic reagents, has small pollution to the environment and low production cost, and is suitable for industrialized production.

The invention discloses a synthesis and preparation method of fasudil hydrochloride, which comprises the steps of taking 5-isoquinoline sulfoacid as raw material, refluxing in thionyl chloride to obtain 5-isoquinoline sulfonyl chloride hydrochloride, adding dichloromethane after dissolving with ice water, adjusting pH value of the solution to be neutral and performing liquid eparation; washing organic phase with water and edible salt, drying and filtering to obtain dichloromethane solution of 5-isoquinoline sulfonyl chloride; performing reaction of the solution with high purity piperazine in the presence of other alkaline reagents, washing the reaction solution with hydrochloric acid aqueous solution and sodium hydroxide aqueous solution after reaction, and extracting the washing solution respectively with dichloromethane; combining organic phases, washing with water, drying and filtering, and dropwise adding saturated hydrogen chloride ethanol solution to separate out crude product of fasudil hydrochloride; and recrystalizing the crude product with ethanol aqueous solution to obtain fasudil hydrochloride. The method provided by the invention greatly reduces the usage amount of high purity piperazine that is expensive by using deacidifying agents that are low in cost so as to reduce the preparation cost of fasudil hydrochloride effectively.

The invention relates to a novel piperazidine or homopiperazine oxalyl hydrazine class compound as represented by formula I, wherein each symbol has meanings defined in the description. The invention further relates to the preparation of the piperazidine or homopiperazine oxalyl hydrazine class compound, use of the piperazidine or homopiperazine oxalyl hydrazine class compound in preparing medicament for treating and/or preventing tumor and/or cancer, medicament composition containing the piperazidine or homopiperazine oxalyl hydrazine class compound. The piperzzidine or homopiperazine oxalyl hydrazine class compound has effective anti-tumor activity.

The invention relates to a catalyst for producing piperazidine and triethylenediamine and a preparation method thereof, and belongs to the technical field of a zeolite molecular sieve catalyst. The preparation method comprises the following steps of: sequentially carrying out water vapor treatment, NaOH solution soaking, 600-800 DEG C roasting on H-ZSM-5; then adding to a straight type condensation tube; sealing both ends of a molecular sieve by respectively using filter papers; plugging rubber plugs with stainless steel tubes on both ends of the condensation tube; circularly accessing a metal nitrate solution into the condensation tube through a peristaltic pump; carrying out 60-110 DEG C oil bath on the shell of the condensation tube; taking out the molecular sieve, carrying out suction filtration, placing a filter cake into a quartz glass tube, placing into liquid nitrogen in a sealing way, and taking out the filter cake for drying; and placing into muffle furnace for roasting. The catalyst disclosed by the invention keeps high selectivity on the triethylenediamine, keeps the activity still good with the change of time and has long life.

Disclosed are nitrate derivant of glycyrrhizic acid or glycor represented by formula Ia and Ib and its nontoxic salt which can be accepted in the sphere of pharmacy, their precoss for preparing, and components and usage of the drugs which contain these compounds.Thereinto, R1, R2 and R3 stand for hydroxyl or -X-L-oxo-oxonitryl (X stands for oxygen,imino; L stands for alkyl with 2-6 of canbon atoms, substituted alkyl or cycloalkyl, hydroxyl amino acid residue or N,Ní»-disubstituted piperazine); R3 stands for hydrogen, oxonitryl or carbonyl -Lí»oxo-oxonitryl (Lí»stands for alkyl with 1-6 of canbon atoms, substituted alkyl or cycloalkyl, aralkyl, N,Ní»-disubstituted piperazine); in formula Ib, R1, R2 and R3 may be the same or different, but in which at least one of them contains -X-L-oxo-oxonitryl; in formula Ib, at least one of R3 or R4 must contain oxonitryl. In formula Ia and Ib, hydrogen of 18-carbon can be alpha-isomer or beta-isomer.

The invention provides a one-step synthesizing method of levofloxacin and ofloxacin. According to the invention, S-9,10-difluoro-2,3-dihydro-3-methyl-7-oxygen-7H-pyrido[1,2,3-delta]-[1,4]-benzoxazine-6-carboxylic acid ester or 9,10-difluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-delta]-[1,4]-benzoxazine-6-carboxylic acid ester is adopted as a raw material; the raw material is subjected to a reaction with alkali in an organic solvent or water or a mixed solvent of an organic solvent and water, such that a corresponding carboxylic acid salt is formed; the solvent is directly removed by evaporation after a hydrolysis process; The product is directly added into N-methylpiperazine in a form of a carboxylic acid salt; and a piperazine concentration reaction is carried out, such that levofloxacin or ofloxacin is obtained. The method provided by the invention is simple to operate. With the method, a hydrolysis and then acid adjusting process is not needed, reaction cost is reduced, production period is short, pollution is low, raw material utilization rate is high, the method is economical and simple, and the yield and purity of obtained levofloxacin and ofloxacin are high.

The invention provides a preparation method of lurasidone. On the basis of the existing preparation method of lurasidone, a one-pot method is adopted to replace the method including multiple steps and obtain a target product once. The preparation method comprises the following steps: adding 3-(1-piperazinyl)-1,2-benzisothiazole in toluene, stirring to dissolve; adding (1R,2R)-1,2-bis(methanesulfonyloxymethyl)cyclohexane and an inorganic alkali, heating and carrying out reflux reaction for 12-36 hours; adding (3alpha R,4S,7R,7alpha S)4,7-methano-1H-isoindole-1,3(2H)-dione; heating and refluxing; recycling toluene at reduced pressure; adding ethyl acetate in the residue, stirring to dissolve, washing for 2-3 times with 5% hydrochloric acid, separating out the organic layers, drying for 20-120 minutes, filtering to remove the drying agent, concentrating the obtained ethyl acetate solution, dropwise adding concentrated hydrochloric acid, precipitating the solid, and performing suction filtration to obtain crude lurasidone; and refining crude lurasidone to obtain pure lurasidone. By adopting the preparation method of lurasidone, the solvent can be recycled conveniently and the method is simple in operation.

The invention discloses a triazine ring structure containing caged organic phosphate and a preparation method of the caged organic phosphate. Cyanuric chloride, piperazidine and 1-oxo-4-hydroxymethyl-2,6,7-trioxa-1-phosphabicyclo[2,2,2]octane (PEPA) are used as main raw materials to prepare the triazine ring structure containing caged organic phosphate, and the preparation method has the characteristics of accessible raw materials, simple, convenient and easy process, safe production and operation, and the like. According to the triazine ring structure containing caged organic phosphate disclosed by the invention, three components, namely, a carbon source, an acid source and a gas source are integrated in one molecular structure, phosphorus-nitrogen synergy and compatibility charring effect in the same molecule is exerted, charring performance and flame retardant performance of a flame retardant system are greatly improved, and in addition, the triazine ring structure and a caged structure both exist in the molecular structure so that the caged organic phosphate has extremely good thermal stability, can be used as a flame retardant in most polymer materials, and has good application prospect.

The invention discloses an improved method for synthesizing an antianginal medicine ranolazine and belongs to the field of pharmaceutical chemistry. The method comprises the following steps of: amidating 2,6-dimethylaniline which is taken as a raw material, and alkylating to obtain N-(2,6-dimethylphenyl)-2-(1-piperazino)-acetamide; and reacting the N-(2,6-dimethylphenyl)-2-(1-piperazino)-acetamide and 2-(2-methylphenoxymethyl)ethylene oxide which is obtained by reaction of 2-methoxyphenol and epichlorohydrin to obtain crude ranolazine, and recrystallizing to obtain refined ranolazine. A reaction solvent, the molar ratio of raw materials, a phase transfer catalyst, a recrystallization solvent and the like are optimized; and the improved method is convenient to operate and is suitable for industrialized production, the production cost is reduced, and the yield is improved.

Methods are provided for treating mesothelioma patients with a dual PI3K/mTOR inhibitor, GDC-0980: (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, and having the structure:

The invention discloses a preparation method of a catalyst for synthesizing piperazine through a monoethanolamine catalytic amination one-step method. The catalyst is spherical particles prepared by taking a mixture containing gamma-Al2O3 and theta-Al2O3 as a matrix, wherein the specific surface area of the catalyst is 200-300 m<2>/g; the pore volume is 0.45-0.65 cm<3>/g; the particle size is 1.0-3.0 mm. The catalyst mainly comprises the following components: 0-15% of Ni, 0-10% of Co, 0-5% of Mo, 0-10% of Fe, and 0-5% of La. The preparation method of the catalyst comprises the following steps: dipping a carrier for 4.0-12.0 h, then performing dehydration, spraying and performing dehydration, drying, baking, and activating the substance to prepare the spherical particle-like catalyst. The preparation method has the advantages that the solid catalyst for synthesizing piperazine through the monoethanolamine catalytic amination one-step method is prepared; the preparation method of the catalyst adopts a dipping and spraying combined technology, so that the method is simple and convenient to operate; the catalytic medium is free from addition of noble metal, so that the preparation cost of the catalyst is obviously reduced. When the catalyst is used for synthesizing piperazine through the monoethanolamine catalytic amination one-step method, the preparation method has the characteristics of high reaction selectivity and high reaction yield.

The invention relates to a preparation technique of a nanofiltration membrane, particularly a preparation method of an antibacterial polypiperazine-amide nanofiltration membrane, which comprises the following steps: by using IsoparG oil as a solvent and trimesoyl chloride and 2,4,6-trichlorophenyloxyformyl chloride as solutes, immersing a polysulfone base membrane in a piperazidine water solution, taking out, and airing, wherein the piperazidine water solution contains sodium dodecylsulfate; and after airing the solution, contacting a mixed organic phase solution, keeping the treated membrane in a 90 DEG C vacuum drying oven for 10 minutes, and taking out. The prepared membrane has strong antibacterial function, and the formed stable covalent bond structure can not be easily lost in the use process of the nanofiltration membrane, thereby enhancing the fouling resistance and service life of the membrane. The preparation method is simple, and easy to operate.

The invention provides piperazinoltriazole derivatives, in particular dipeptidyl peptidase IV inhibitors shown by a formula (I) below. The substituents in the formula are defined in the description. The compounds can be used for treating or preventing diseases associated with dipeptidyl peptidase IV, such as diabetes, obesity and hyperlipidemia. The invention also provides methods for preparing the compounds shown by the formula (I), pharmaceutically acceptable salts of the compounds and medicinal compositions and the use of the compounds, the pharmaceutically acceptable salts of the compounds and the medicinal compositions in the preparation of medicaments for treating or preventing diseases associated with dipeptidyl peptidase IV.

The invention relates to a process for modifying a polyurethane urea material, which comprises the following steps: firstly, carrying out vacuum melt reaction of lactide, stannous octoate and polyethylene glycol at 130-170 DEG C to produce hydroxyl-terminated macromolecule alcohol with the molecular weight of 2000-10000; and dissolving the hydroxyl-terminated macromolecule alcohol in the benzene series solvent, adding hexamethylene diisocyanate and a catalyst namely stannous octoate, reacting at 60-80 DEG C to generate a prepolymer, adding 2, 2-dihydromethyl propionic acid to the prepolymer, sufficiently reacting, cooling, adding piperazine, and sufficiently reacting to obtain the 2, 2-dihydromethyl propionic acid modified shape memory polyurethane urea material. By the method, each chain end of the modified material can have uniform carboxyl groups with controllable content; the hydrophilicity of the material can be improved by introducing the carboxyl groups, the cell adhesion is benefited, and the mechanical strength, shape memory performance and biological activity of the material are improved; and the material has better hydrolysis performance through introducing a neopentyl structure, so the degradation speed of the material is favorably reduced.