76 results about "Favipiravir" patented technology

The invention relates to a favipiravir synthesis process, which comprises: 1) dissolving a pyrazine compound in an organic reagent I, adding an oxidizing agent M, and carrying out a nitrogen oxidation reaction to obtain a white solid; 2) adding the obtained white solid to an organic reagent II, and carrying out a chlorination reaction to obtain a pale yellow solid; 3) uniformly mixing the obtained pale yellow solid, a dried aprotic polar solvent, a dried fluorine ion donor reagent and tetrabutylammonium bromide, and carrying out a stirring reaction to obtain a pale yellow solid; 4) adding the obtained pale yellow solid to water, and carrying out a reaction with 1,4-dioxane and sodium acetate to obtain a yellow oily matter; and 5) uniformly mixing the obtained yellow oily matter and concentrated sulfuric acid to obtain the target product favipiravir. According to the present invention, the method has advantages of simple and easily available raw materials, simple synthesis process and mild conditions, nitrogen oxidation, chlorination, fluorization and hydrolysis are performed to finally prepare the 6-fluoro-3-hydroxypyrazine-2-formamide, and the good industrial value is provided.

The invention relates to a favipiravir L-arginine frozen-dried preparation for injection. The frozen-dried preparation comprises favipiravir and L-arginine, wherein the molar ratio of the favipiravirto the L-arginine is (1 to 1.1) to (1 to 1.3) ( weight ratio is (1 to 22) to (1 to 1.44) ). The invention further discloses a preparation method of the favipiravir L-arginine frozen-dried preparationfor injection, the obtained frozen-dried preparation can be guaranteed to have favorable redissolution properties, and based on high unit load dosage, the favipiravir L-arginine frozen-dried preparation for injection has favorable stability.

The invention relates to a freeze-dried preparation of favipiravir for injection. A formula of the freeze-dried preparation specifically comprises an active component favipiravir, a pH regulator sodium hydroxide, an excipient mannitol, a freeze-drying additive tert-butyl alcohol, and water for injection. The invention also discloses a method for preparing the freeze-dried preparation of favipiravir for injection. With the method, quality defects, such as clarity, turbidity and the like, of the freeze-dried preparation caused by sublimation of favipiravir can be effectively controlled; and theprepared freeze-dried preparation has good stability.

The invention provides a preparation method of favipiravir, which comprises the following step: by using one or two of 6-fluoro-3-hydroxyl-2-cyanopyrazine and 6-fluoro-3-hydroxyl-2-cyanopyrazine organic amine salt as raw materials, carrying out high-yield preparation in an anhydrous organic solvent under alkaline conditions to obtain favipiravir. Compared with the existing concentrated sulfuric acid hydrolysis process and hydrogen peroxide hydrolysis process, a large amount of acidic wastewater generated in the concentrated sulfuric acid hydrolysis process is avoided, explosion hazards possibly caused by use of hydrogen peroxide are also avoided, meanwhile, hydrolysis and oxygenolysis phenomena of products in the concentrated sulfuric acid hydrolysis process and the hydrogen peroxide hydrolysis process are avoided, and the preparation method is environmentally friendly, simple and safe to operate and relatively high in yield.

A method for prevention or treatment of a viral-mediated infectious disease in a mammal. The mammal may be a human being. A therapeutic dose of a composition is administered, via an inhalation delivery apparatus, to the mammal. The composition includes microparticles and / or nanoparticles. The microparticles and / or nanoparticles include a first pharmaceutically active agent and a second pharmaceutically active agent. The first pharmaceutically active agent includes unfractionated heparin (UFH), Low Molecular Weight Heparin (LMWH), sulfated non-anticoagulant heparin (S-NACH) or combinations thereof. The second pharmaceutically active agent includes 10-30 mg of hydroxychloroquine in a form of hydroxychloroquine sulfate, 10-30 mg of favipiravir, or a combination thereof. The viral-mediated infectious disease is caused by one or more viruses in the mammal.

The invention belongs to the field of medicinal chemistry and particularly relates to a new synthesis method of Favipiravir. The method comprises the following steps: carrying out carboxyl protection on raw material shown in the formula (II) to generate a compound (III); carrying out diazotization hydrolysis reaction in the presence of concentrated sulfuric acid and sodium nitriteto generate a compound (IV); carrying out benzyl protection reaction to generate a compound (V), and then generating a compound (VI) in the presence of potassium fluoride and tetrabutylammonium bromide; removing a benzyl protection group to generate a compound (VII); and then adding an aminating agent to carry out amination to generate Favipiravir shown in the formula I. The method disclosed by the invention has the advantages that the reaction cycle is short, the operation is simple, the production cost is low, and the product is high in quality; therefore, the method is suitable for industrial production.

The invention discloses a favipiravir pharmaceutical composition containing different particle size ranges. According to special particle size distribution and preparation process, the problem of dissolution rate of favipiravir preparations in water is solved, the favipiravir is rapidly released, the human bioavailability is provided, and the problems that the dissolution rate of favipiravir in the preparation is limited, in-vivo absorption is influenced and the clinical treatment aim is achieved due to different pH value environments are solved. The invention also provides a method for preparing the favipiravir pharmaceutical composition.