248 results about "Phthalide" patented technology

The present invention relates to the use of 3-sbustituted phthalide or analogue for preparing the medicine for treating Alzheimer disease or other neurotic disease. The structural formula is shown in the right formula. Filtering is executed through a high-effective living model which integrates gene technique and biological technique. The research shows that most compounds have a certain function that the defective individual recovers learning capacity, wherein a plurality of specific compounds represent better activity. The learning capacity of deflective individual can be recovered for above 85%. Furthermore a stable treating effect can be shown in a plurality of tests.

The invention relates to an ester obtained by the reaction of 3-(3'-hydroxyl)-butylphthalide and acids, wherein, the acids can be acceptable inorganic acids or organic acids in pharmacy. Proved by testing, the efficacy of the ester is increased significantly. Part of the ester can go on reacting with the acids or alkalis to form salts in order to increase water solubility and prepare injection preparations; being proved by testing, the injection preparations have no muscle and vascular stimulation.

A therapeutic agent and prophylactic agent for a disease accompanying an abnormality in an amount of insulin or insulin response, an agent for an insulin-mimetic action, a food, beverage and feed, an agent for enhancing glucose uptake into a cell, and an agent for inducing differentiation into an adipocyte, characterized in that each comprises as an effective ingredient at least one compound selected from the group consisting of a chalcone compound, an acetophenone compound, a coumarin compound, a phthalide compound, derivatives thereof, and pharmacologically acceptable salts thereof.

The invention relates to the pharmaceutical chemistry filed, and particularly relates to novel nitric oxide donor butyl phthalide derivatives (I), the preparation method thereof, a drug preparation containing the derivatives (I) and the application as a drug for resisting thrombosis and cerebral ischemia. Wherein, the definitions of R and A are shown in the instruction.

The invention provides acetone extract, chloroform extract, or hexane extract from Chinese angelica and active ingredient obtained from purification thereof such as p-butylidene phthalide for effective treatment to cancer.

The invention discloses a preparation method of Olaparib and an analogue of the Olaparib. 2-fluoro-5-formyl benzoic acid is taken as a raw material and reacts with 1-substitutent piperazine to produce 3-(4-substitutent)piperazine-1-carbonyl)-4-fluorobenzalde which reacts with (3-oxo-1,3-dihydro-isobenzofuran-1-yl)dialkyl phosphate to produce 1-(substitutent)-4-[5-(3-oxo-3H-isobenzofuran-1-yl-methylene)-2-fluorobenzoyl]piperazine, then the 1-(substitutent)-4-[5-(3-oxo-3H-isobenzofuran-1-yl-methylene)-2-fluorobenzoyl]piperazine reacts with hydrazine hydrate to produce the Olaparib (Ia,R=cyclopropyl formyl) and the analogue (Ib,R=BOC) of the Olaparib; or 3-(4-substitutent)paperazine-1-carbonyl)-4-fluorobenzalde reacts with phthalide to produce 1-(substituent)-4-[5-(2,3-dihydro-1,3-dioxo-1H-indene-2-yl)-2-fluorobenzoyl]piperazine which reacts with the hydrazine hydrate to produce the Olaparib (Ia,R=cyclopropyl formyl) and the analogue (Ib,R=BOC) of the Olaparib.

The preparation method of the fungicide intermediate (E)-2-(2'-chloromethyl)-2-methicillin imino acetic methyl ester is: 1) the phenyl phthalate and the thionyl dihalide react with the influence of a catalyst; the catalyst is the Louis acid and phosphonic derivative; 2) the product of the first step and the alkali metal cyanide react with the influence of the organic solvent and phase transfer catalyst; the organic solvent is selected from the non-polar aromatic solvent or the halogen hydrocarbon; the phase transfer catalyst is selected from the halide of the four-level nitride or the ammonium salt; the alkali metal cyanide is selected from the sodium cyanide and potassium cyanide; 3) the products of the second step and the methanol react under the condition with the organic solvent and the chlorinated hydrogen; 4) the products of the third step and the methicillin amine hydrochloride under the condition with the organic solvent; thus, the target product can be got. The energy consumption and production risk of the present invention are obviously lowered; the relative collection rate is high; the safety in the production process is improved; and the present invention has no drawbacks such as the obstruction.

The invention relates to a butyl phthalide tablet and a preparation method thereof. The butyl phthalide tablet is composed of butyl phthalide solid powders and other medical troche auxiliary materials; wherein, the butyl phthalide solid powders are composed of the components with the following weight percentage: 9 percent to 30 percent of butyl phthalide, 0.01 percent to 1.2 percent of emulsifiers and 70 percent to 90 percent of cyclodextrin or cyclodextrin ramification. The troche which is made with the invention has favorable forming, stable product quality and high dissolution rate.

The invention is concerned with the injection thick solution and the preparation method that is made of butyl phthalide.

The invention discloses a method for preparing phthalide through phthalic anhydride liquid phase hydrogenation under the action of au-base catalyst. The gold-base catalyst used in the preparation method takes SiO2, ZnO, La2O3, CeO2, TiO2, ZrO2 or Fe2O3 as a carrier and takes gold as an active component, and the loading of gold is between 0.05 and 20 percent. As the gold-base catalyst used in the preparation method has excellent hydrogenation activity and selectivity under mild catalytic reaction conditions, the conversion rate of phthalic anhydride can be more than 95 percent, and the selectivity of phthalide can be more than 93 percent, thereby the single pass yield of the target product phthalide is high. Moreover, the gold-base catalyst is very good in performance stability, and more particularly, the gold-base catalyst after metal oxide modification can still maintain the selectivity over 92 percent even through the activity of the gold-base catalyst declines slightly after repeated recycling use. In addition, the gold-base catalyst provided is simple to prepare and does not pollute the environment. Therefore, the preparation method has significant advantages.

The invention relates to new use of 3-n-butylphthalide (abbreviated as butyl phthalide) and derivatives thereof, in particular to the use of the compounds in the preparation of the medicine for treating Parkinson disease. A mat model of hemiparkinsonian disease is built by using three-dimensional targeted injection of rotenone to perform a test, and the result of the test shows that the butyl phthalide and derivatives thereof can effectively improve symptoms aroused by Parkinson and have a nerve-protecting effect.

A method for inhibiting nitric oxide and / or prostaglandin E2 synthesis. The method comprises administering a composition to a subject, wherein the composition comprises an effective amount of butylidene phthalide, citronellol, geraniol or combinations thereof, which can be used to reduce or relieve the syndromes of the inflammation.

The invention discloses a phthalide type ingredient effective part as well as a preparation method and an application of the phthalide type ingredient effective part and belongs to the technical field of traditional Chinese medicine and natural product extraction and application. The preparation method of the phthalide type ingredient effective part comprises the following steps that hemlock parsley medicinal materials are extracted by an ultrasonic extraction method, a solvent extraction method, a microwave extraction method, a solvent backflow extraction method or a supercritical fluid extraction method, extracts are added with water to be dispersed and are then respectively extracted by two different-polarity solvents, extraction liquid is purified by positive-phase silica gel, the content of the phthalide type ingredient effective part accounts for more than 50 percent of the total weight of the extracts, and in addition, different solid phase extraction operation modes can be adopted according to different ingredient requirements. The phthalide type ingredient effective part, the preparation method and the application have the advantages that the preparation speed is fast, the phthalide type ingredient content in the product is high, the ingredient is definite, the quality is controllable, and good economic benefits and social benefits are realized.

The invention provides a butylphthalide medicine active composition, which comprises the following ingredients: first ingredients: the butylphthalide content is higher than or equal to 98.0 percent; second ingredients: the second ingredients are one kind of materials or several kinds of materials selected from methylene phthalide, ethylene phthalide, propylene phthalide, butane phthalide, amylene phthalide, phthalide, methyl phthalide, ethyl phthalide, propyl phthalide and amyl phthalide, in addition, the content of the second ingredients is higher than 0 but is lower than or equal to 2.0 percent, when the second ingredients comprise any one kind of materials from methylene phthalide, ethylene phthalide, propylene phthalide, butane phthalide and amylene phthalide, the content of any one kind of included ingredients does not exceed 0.5 percent, and when the second ingredients comprise any one kind of materials from phthalide, methyl phthalide, ethyl phthalide, propyl phthalide and amyl phthalide, the content of any one kind of included ingredients does not exceed 1.0 percent. The quality of the medicine active composition is stable, and the clinic curative effect and the medication safety of the butylphthalide preparation can be ensured.

The invention discloses an organic reversible thermochromic microcapsule with long service life and large color difference and a preparation method thereof. A wall material of the organic reversible thermochromic microcapsule is prepared from the following raw materials in percentage by weight through polymerization: 30-95% of acrylate and / or methacrylate, 5-70% of a divinyl and / or polyvinyl monomer mixture, and 0-10% of an acrylic acid and / or methacrylic acid mixture, and a core material is composed of a colour former 3,3-di(4-dimethylaminophenyl)-6-dimethylamino phthalide, a color developing agent 4,4'-dihydroxydiphenylsulfone, and a solvent selected from 1-dodecanol, 1-tetradecanol, 1-hexadecanol and 1-octadecanol; and the preparation method is implemented through carrying out prepolymerization on monomers and carrying out suspension polymerization on the obtained product. The obtained organic reversible thermochromic microcapsule has the advantages of long service life and large color difference; the microcapsule does not release formaldehyde, and does not contain bisphenol A, so that the microcapsule is safer to use.

The invention relates to a medicament for injection containing n-butylphthalide and its preparing process, wherein the constituents include (by weight parts) n-butylphthalide, oil, surface active agent, isotonic agent and water by the proportion of 1:1-100:1-50:1-20:50-70. The preparing process comprises charging the isotonic agent and water soluble surface active agent into water, thus obtaining aqueous phase mixture, then charging n-butylphthalide, surface active agent and stabilizing agent into oil, heating to 60-90 deg. C, high speed stirring and emulsifying.

A gas chromatographic method for determining a residual solvent in a phthalide compound takes cyanopropyl phenyl-dimethyl polysilicone as a stationary liquid capillary chromatographic column, hydrogenas a flame ionization detector and nitrogen as a carrier gas and calculates content of the residual solvent in peak area according to an external standard process. The method can determine normal heptane and other residual solvents in the phthalide compound and has the advantages of high sensitivity, strong specificity and high accuracy.

The invention relates to a method for synthesizing phthalide catalyzed by benzoic anhydride in liquid phase, especially relates to method with loading nickel catalyst. Said method employs phthalide as reacting solvent, prepares phthalide through selective hydrogenation with benzoic anhydride under catalysis of loading nickel catalyst; the ratio by weight between said benzoic anhydride and phthalide is 1: 0.1-10, the reacting temperature is 130-200 Deg. C, reacting pressure is 1.0-5.0 Mpa; said loading nickel catalyst is catalyst with nickel loaded on SiO2, diatom earth, activated char, TiO2, ZrO2, TiO2-SiO2, TiO2-Al2O3 or TiO2-ZrO2, and the loading amount of nickel is 5-50 wt.%. The invention is characterized by high activity and stability of used loading nickel catalyst, no pollution of process, direct usage of phthalide as solvent, low cost for post treatment, and simple process.

An application of a phthalide compound in preparing a medicament. The medicament is specially used for promoting a stem cell to secrete one of the following items: telomerase, a neurotrophic factor (brain-derived neurotrophic factor, BDNF), a stem cell chemotactic factor (stromal cell-derived factor-1, SDF1), a stem cell chemotactic factor receptor (CXC chemokine receptor 4, CXCR4), and an immunoregulatory factor; a kit comprising a phthalide compound and a stem cell is also provided.

The invention discloses a quantitative measurement method of ligustilide. In the method, butyl phthalide is used as a substitute reference, high-efficiency liquid chromatography is used for measurement, octadecylsilane chemically bonded silica is used as a filler, a flowing phase consists of methanol and water in a volume ratio of (30-70):(70-30) or acetonitrile and water in a volume ratio of (30-60):(70-40), the detection wavelength is 208 to 334 nanometers, the peak areas A and Ai of the ligustilide in a measured sample and the phthalide substitute reference are measured respectively, and based on the concentration Ci of the butyl phthalide, the concentration C of the measured ligustilide component is calculated by using a correction factor f according to formula below, wherein the correction factor f is between 0.08572 and 1.3283. Experiment results show that the result of the ligustilide content measurement performed by the method is consistent with that of the ligustilide contentmeasurement performed by a method using the freshly prepared ligustilide as a reference, and the measurement result of the method is stable.

The invention discloses a penicillium vulpinum fungi strain and a method for preparing levo 7-hydroxyl butylphthalide ((S)-(-)-butyl-7-hydroxyl phthalide) employing the fungi strain. The fungi strain disclosed by the invention is a penicillium vulpinum fungi strain NCC3421 (penicillium vulpinum) and is preserved at the China General Microbiological Culture Collection Center (CGMCC for short); and the preservation number is CGMCC No.9094. Under the culture condition provided by the method, the fermentation unit of the levo 7-hydroxyl butylphthalide reaches over 1600mg / L; the fermented product is relatively single in components, and easy to separate and purify, and can be applied to industrialized production of the levo 7-hydroxyl butylphthalide.

The present invention provides a Chuanxiong rhizome volatile oil soft capsule and its preparation method and use. The Chuanxiong rhizome volatile oil described in the invention is prepared by a carbon dioxide supercritical extraction method, the contend of the effective component Chuanxiong rhizome phthalide in the Chuanxiong rhizome volatile oil reaches the medicinal standard, and the quality is stable and can be controlled. The invention also provides the use of the Chuanxiong rhizome volatile oil soft capsule for preparing the medicine for curing cerebral apoplexy during recovery period.

This invention discloses a preparation method of 2-carboxybenzaldehyde. In the method, phthalide dissolved in chlorobenzene or toluene solvent is first used to react with bromine to obtain 3-bromo phthalide, and then the 3-bromo phthalide is hydrolyzed to obtain wet 2-carboxybenzaldehyde, at last the wet 2-carboxybenzaldehyde is refined by recrystal to obtain the 2-carboxybenzaldehyde. In the method of invention, the mol ratio of phthalide to bromine to chlorobenzene or toluene and to water is 1: 1-3: 0.5-2: 1-20. The preparation method of 2-carboxybenzaldehyde has the advantages of low cost,simple steps, good controlability of each step, high yield and high purity of products, and is conducive to the expanding production and realizing industrialization.

The present invention relates to a composition for the prevention or treatment of diseases associated with angiogenesis, and in detail, to a composition comprising the extract of Cnidium officinale Makino or the fraction thereof for the prevention or treatment of diseases associated with angiogenesis. The present invention also provides 3-butyl-7-hydroxyphthalide, vanillin, coniferyl ferulate, and falcarindiol as active compounds. The composition of the present invention inhibits angiogenesis, so that it can be applied to the prevention or treatment of diseases related to angiogenesis, such as arthritis, diabetic retinopathy, psoriasis, and cancer.

The invention belongs to the technical field of drug synthesis, and relates to position selective synthesis of alpha-narcotine with participation of a blockage group, preparation of serial phthalide tetrahydroisoquinoline compounds and preparation of various phthalide-3-carboxylic acid compounds and various 3-oxo isochroman-1-carboxylic acid compounds through a universal mode. In the method, 2, 3-dimethoxy benzoic acid is used as a raw material and condensed with glyoxylate through the universal mode to obtain 6, 7-dimethoxy phthalide-3-carboxylic acid, the carboxylic acid and 2-(2-bromo-3, 4-methylenedioxy-5-methoxy-phenyl)-ethylamine hydrochloride are condensed to prepare amide, the amide reacts with Bischler-Napieralski to prepare bromo-alpha-narcotine through reaction, methylation and salt formation, and (-)-alpha-narcotine is then prepared through dehalogenation and resolution. Due to the positioning function of the blockage group, the invention effectively reduces the position selectivity of Bischler-Napieralski cyclization, and realizes the simple and efficient synthesis of alpha-narcotine through removal of the blockage group and the chiral resolution.

The invention provides a compound air cleaning agent and a preparing method and application thereof. The compound air cleaning agent is formed by compounding multiple components of thyme essential oil, tea tree essential oil, castanea mollissima flower extracting solution, peony root and skin extracting solution, vine tea extracting solution, gardenia essential oil, osmanthus fragrans essential oil, costustoot essential oil, may lily of the valley alcohol, nerol, citric acid, 2-isopentyloxy allyl acetate, alcohol, assistant, 4-hydroxy-3-butylphthalide and deionized water. The air cleaning agent has the advantages of better sterilizing, mosquito repelling and aroma enhancing performances due to proper selecting of component and proportion and the coordinated action among the components, less using amount, long time effectiveness, and is more saved and fast in the aspect of life and use of people.

The invention provides 3-substituent phthalide compounds first. The constitutional formula of the compounds is shown in the right. The compounds are sifted through a drosophila study ability model to find that most of the compounds play the role of restoring study ability on defected individuals; and specific compounds thereof express better activities, allow the defected individuals to restore over 85 percent of study ability and play the role of stable treatment in multiple rounds of experiments. Based on the experiments, the novel 3-substituent phthalide compounds are bioactive molecules for treating Alzheimer's disease.

The invention relates to a high-selectivity catalyst for preparing phthalide by hydrogenation of phthalic anhydride, which is a supported monometallic and bimetallic catalyst prepared by taking a hydrotalcite or hydrotalcite-like material as a precursor as well as preparation and application thereof. The composition of the catalyst is MM' / S, wherein the supported amount of metal M (Ni, Co, Fe, Cu, Mo and W) is 5-70%, the supported amount of metal M' (Au, La and Mg) is not higher than 30%, and S is an oxide of Al, Zn, Nb, Fe, Zr, Cr and Ti. The catalyst disclosed by the invention is applicable to kettle-type (intermittent or continuous) stirring reaction and is also applicable to continuous fixed-bed hydrogenation reaction, the selected solvent is gamma-butyrolactone, the activity for phthalic anhydride hydrogenation is high, the selectivity of phthalide is high, the phthalic anhydride conversion ratio can reach 99%, and the phthalide selectivity can reach 98%. The catalyst has high activity, high selectivity and high stability, raw materials are easily obtained, and the process is simple, so that the catalyst has a good industrial prospect.

The invention relates to a preparation method of an Olaparib intermediate (IV), namely, 2-fluoro-5-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]benzoic acid. The method comprises steps as follows: 1, 2-fluoro-5-formyl benzoic acid is used as a raw material and reacts with (3-oxo-1,3-dihydro-isobenzofuran-1-yl)dialkyl phosphate to produce 2-fluoro-5-(3-oxo-3H-isobenzofuran-1-yl-methylene)benzoic acid, namely, an intermediate (V); or 2-fluoro-5-formyl benzoic acid reacts with phthalide to produce 5-(2,3-dihydro-1,3-dioxo-1H-indene-2-yl)-2-fluobenzoic acid, namely, an intermediate (VI); 2, the intermediate V or the intermediate VI reacts with hydrazine hydtaye to produce an Olaparib intermediate (IV). The preparation method is concise in process, environment-friendly, economical and suitable for the industrial key Olaparib intermediate, raw materials are easy to obtain, and purification is easy.

A pure-component Chinese medicinal preparation for treating headache and its preparation process, using Gastrodia elata and Ligusticum chuanxiong as basic formulation, adopting modern flash extraction technique, combining macroporous resin, normal / reversed-phase silica gel chromatography technique and high-speed counter-current chromatography preparation technique, extracting a volatile oil fraction containing butylphthalide as main component, an alkaloid fraction containing ligustrazine as main component, an organic acid fraction containing ferulic acid as main component, a lactone fraction containing ligustilide as main component, a phenols fraction containing gastrodine as main component and a polysaccharide fraction containing polysaccharides from Ligusticum chuanxiong as main component. The Chinese medicinal preparation provided by the invention has definite curative effect, definite composition, controllable quality, and simple operation method.