53 results about "Topiroxostat" patented technology

The invention provides a preparation method of topiroxostat. The preparation method comprises the steps that 2-cyano methyl isonicotinate is used as raw materials; hydrazinolysis is performed at -10 DEG C to -20 DEG C to obtain an intermediate; the intermediate and 4-cyanopyridine react under the conditions with sodium ethoxide and the pH being 4 to 6 to obtain the topiroxostat. The preparation method has the advantages that the 2-cyano methyl isonicotinate is used as a starting material; the 2-cyano methyl isonicotinate and hydrazine hydrate take condensation reaction at low temperature to prepare the intermediate; the intermediate and the 4-cyanopyridine are subjected to condensation and loop closing under the acid condition with sodium ethoxide to prepare the topiroxostat. The raw materials can be easily obtained; the reaction conditions are mild and are easy to control; a reagent with high toxicity is not used in the reaction process; the released toxic substances are few; the sidereaction products are few; the reaction safety is high; the pollution is small; the obtained purity is high; the preparation method is suitable for industrial production.

The invention provides a topiroxostat tablet and a preparation method thereof, and belongs to the technical field of medicine. The invention relates to a topiroxostat clathrate compound dispersible tablet; the topiroxostat is firstly prepared into a clathrate compound and then the clathrate compound is prepared into the dispersible table. The topiroxostat tablet has the advantages of quick dissolving, quick absorption, high bioavailability, convenience for taking and the like.

The invention provides a topiroxostat oral preparation and a preparation method thereof. The topiroxostat oral preparation is composed of an active ingredient topiroxostat as well as a filling agent, a disintegrating agent, a binding agent and a lubricating agent. The prepared topiroxostat oral preparation has no special requirement on particle size on the active ingredient, superfine grinding does not need to be carried out, energy consumption is low, dissolution rate reaches more than 95%, bioavailability is high, the defects of low dissolution rate and low bioavailability of the active ingredient are overcome, quality is stable and reliable, and a market development prospect is broad.

The invention relates to the field of organic chemistry and pharmaceutical chemistry, specifically to a preparation method of topiroxostat. The technical scheme of the preparation method comprises a step I, dissolving a crude product (an oily product) of a compound I in an alcohol solvent or a mixed solution of an alcohol solvent and another solvent, raising the temperature to a reflux temperature, performing stirring and dissolving, slowly dropwise adding water till a few solid is precipitated, performing thermal insulation and stirring, reducing the temperature to 0 DEC C, performing stirring, carrying out cooling for crystallization, and performing filtration and drying to obtain a compound I with high purity; a step 2, adding the compound I obtained in the step I into a mixed solution of toluene and isopropanol, raising the temperature to 80 DEG C for solution, dropwise adding concentrated hydrochloric acid, performing thermal insulation and stirring, performing cooling to reach the room temperature, and performing drying at 60 DEG C to obtain topiroxostat hydrochloride; and a step 3, preparing topiroxostat. According to the preparation method of high-purity topiroxostat, concentrated hydrochloric acid instead of p-toluenesulfonic acid is used, and through purification of the intermediate compound I, the high-purity compound I is obtained, so that high-purity topiroxostat is prepared.

The invention belongs to the technical field of medicines, and particularly relates to an intermediate for topipitastat, a preparation method thereof, and a method for preparing topipitastat from theintermediate. The intermediate for the topipitastat is 3-(4-pyridyl)-5-(1-oxo-4-pyridyl)-1,2,4-triazole p-toluenesulfonate, and the structural formula of the intermediate is represented by formula (I). The preparation methods are characterized in that methyl isonicotinate oxynitride and hydrazine hydrate undergo a condensation reaction, a ring closing reaction and a salt formation reaction to obtain the intermediate, and the intermediate and N,N-dimethylformyl chloride undergo a cyanation reaction and a refining reaction to obtain the topipitastat. The methods effectively solve the technical problems of complex preparation process and low purity of topiroxostat, and have the advantages of simple process, good reproducibility, low cost, environmental protection and energy saving, so the methods have high industrial values and remarkable social and economic benefits. The preparation methods are used for preparing the key intermediate for the topiroxostat and the topiroxostat.

The invention belongs to the field of medicine and chemical industry and discloses a synthesis method of topiroxostat. The method comprises that 4-cyanopyridine as a starting raw material is oxidized by hydrogen peroxide to form an intermediate 1, the intermediate 1, sodium methoxide and ammonium chloride undergo a reaction to produce an intermediate 2, the intermediate 2 and 4-cyanopyridine undergo an annulation reaction under action of cuprous bromide and sodium carbonate to produce an intermediate 3, and the intermediate 3 and trimethylsilyl cyanide undergo a cyanation reaction to produce topiroxostat. The method utilizes low-price 4-cyanopyridine as a starting raw material, and in the first reaction step, methanol is used as a solvent and 4-cyanopyridine nitrogen oxide as the intermediate 1 is prepared. The method has a high yield and produces a high-purity product. The whole route is easy to operate and is conducive to industrial mass production.

The invention discloses a topiroxostat controlled-release tablet and a preparation method thereof. The topiroxostat controlled-release tablet is composed of a drug-containing tablet core and a coating membrane layer covering the drug-containing tablet core, the drug-containing tablet core comprises topiroxostat, a filling agent and sodium chloride, and the coating membrane layer comprises a controlled-release material, plasticizer and a pore-foaming agent. During preparation, the drug-containing tablet core is wrapped with the coating membrane layer, and the topiroxostat controlled-release tablet is obtained. The topiroxostat controlled-release tablet and the preparation method thereof are characterized in that the topiroxostat controlled-release tablet is composed of a quick-release part and a controlled-release part; after the topiroxostat controlled-release tablet enters a human body, the quick-release part is released rapidly, a certain plasma concentration is achieved, the controlled-release part is released slowly, the certain plasma concentration is maintained, good drug efficacy can be achieved, and the side effect of the drug can be effectively avoided. The topiroxostat controlled-release tablet has the advantages of being rapid to dissolve, rapid to absorb, high in bioavailability, good in stability, convenient to take and the like, and therefore the side effect brought by taking the drug to a patient is reduced. The preparation technology is simple, the obtained product is stable in quality, and the preparation method is suitable for large-scale production.

The invention relates to a topiroxostat tablet. The topiroxostat tablet is prepared by the following steps: grinding effective components and a carrier material through a ball mill to prepare a topiroxostat pharmaceutical composition, carrying out wet granulation, and carrying out tabletting. An effective component in the tablet is topiroxostat, and the tablet comprises the following materials inpercentages by weight: 30% of topiroxostat, 40-68.5% of a carrier material, 2-4% of an adhesive, 2-20% of a disintegrating agent and 0.5-4% of a lubricating agent, wherein the carrier material is composed of a filler and a pH regulator. According to the topiroxostat tablet and the preparation method thereof, tartaric acid or citric acid with proper dosage is added as a pH regulator, and ball milling is carried out at specific grinding time, so that the prepared topiroxostat tablet is high in dissolution rate and high in bioavailability, topiroxostat is limited to be in a crystal form I ratherthan a mixed crystal form, and the stability of the raw materials is ensured.

The invention belongs to the field of drug synthesis and relates to a method for refining high-purity topirastat. The refining method of topirastat according to the present invention comprises the following steps: adding topirastat crude product into an organic solvent, heating and stirring until completely dissolved, activated carbon decolorization, natural cooling and crystallization, filtering and drying to obtain high-purity topirastat Stata. The refined method of the invention has simple process, convenient operation, low production cost, high product purity, stable process and is suitable for industrialized production.