6 results about "Febuxostat" patented technology

This invention provides a method for preparing febuxostat. The route uses ethyl 2-(3-aldehyde-4-hydroxyphenyl)-4-methylthiazolium-5-carboxylate as the starting material, first alkylating the 4-hydroxyl group, then reducing the 3-aldehyde group to a cyano group, and finally hydrolyzing to generate febuxostat. This method is simple to operate, has mild reaction conditions, high yield, low cost, is environmentally friendly, and is suitable for large-scale industrial production of febuxostat.

The application belongs to the technical field of medicine detection, and particularly relates to a detection method of impurities in 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The method uses high performance liquid chromatography to detect related substances in 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester, and the content of each impurity is calculated by a principal component self-control method with a correction factor. Methodology verification shows that the detection method provided by the application is good in specificity, high in accuracy and sensitivity, and can be used for quality control of related substances in 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester, so that the product quality can be effectively controlled, and the medication safety of febuxostat medicine is improved.

The application belongs to the technical field of drug use, and particularly relates to an application of febuxostat in preparation of an antifungal drug and an antifungal composition. The application expands the application range and indications of febuxostat, improves the selection range of the antifungal drug, improves the antifungal effect, and has an inhibiting effect on a ketoconazole-resistant strain.

The invention discloses a preparation method of febuxostat tablets, and belongs to the technical field of febuxostat tablet preparation.The preparation method comprises the steps that febuxostat, lactose hydrate, pregelatinized starch and an adhesive are mixed for fluidization granulation, and wet particles are obtained; drying the wet granules, and finishing the granules; mixing a disintegrating agent and a lubricating agent after granulating, and tabletting to obtain the febuxostat tablet. The disintegrating agent accounts for 2% of the febuxostat tablet in percentage by mass; a sample is prepared by controlling the dosage of a disintegrating agent, the model of an adhesive and the particle size of raw materials in a one-step granulation mode. According to the method, the process steps are simplified, the process continuity is optimized, the process amplification stability and reliability are effectively improved, meanwhile, the product release degree is guaranteed, the production efficiency is effectively improved, and the production cost is remarkably reduced.

The invention belongs to the technical field of chemical synthesis, and in particular relates to an N-(1, 3-dioxo-2-aryl octahydrocyclopenta [c] pyrrole-4-yl) benzamide derivative and a synthesis method of the N-(1, 3-dioxo-2-aryl octahydrocyclopenta [c] pyrrole-4-yl) benzamide derivative. The invention successfully develops a [3 + 2] cycloaddition reaction of a photocatalytic cyclopropanamide compound and an N-substituted maleimide derivative, the N-(1, 3-dioxo-2-aryl octahydrocyclopenta [c] pyrrole-4-yl) benzamide derivative can be prepared according to the synthetic method disclosed by the invention, the yield can reach 34-92%, and the preparation method is simple and easy to operate. A convenient, mild-condition and efficient synthesis path is provided for constructing the functional five-membered carbocyclic compound, and a reaction system shows excellent functional group compatibility and substrate universality. Besides, through successful derivatization with complex drug molecules such as febuxostat and adapalene, the application potential of the synthesis method is highlighted, and the compound is expected to be widely applied to drug development and research.

The invention provides a synthesis method of febuxostat and a key intermediate, and belongs to the technical field of medicine synthesis. 4-hydroxybenzaldehyde is used as a raw material and reacts with hydroxylamine hydrochloride and sulfur in continuous flow equipment under the conditions of a photocatalyst, a solvent and illumination to obtain 4-hydroxybenzenesulfamide; the preparation method comprises the following steps: reacting 4-hydroxybenzenesulfamide with ethyl 2-chloroacetoacetate to obtain ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-formate; the preparation method comprises the following steps: reacting 2-(4-hydroxyphenyl)-4-methylthiazole-5-ethyl formate with a cyano source under an illumination condition, so as to obtain 2-(3-cyano-4-hydroxyphenyl)-4-methylthiazole-5-ethyl formate; the preparation method comprises the following steps: carrying out etherification reaction on 2-(3-cyano-4-hydroxyphenyl)-4-methylthiazole-5-ethyl formate and bromo-iso-butane, so as to obtain the febuxostat key intermediate. The obtained febuxostat key intermediate does not need to be separated, and the febuxostat is synthesized by a two-step one-pot method.