36 results about "1-pyrrolidineacetamide" patented technology

A preparation method of (s)-4-hydroxy-2-oxo-1-pyrrolidineacetamide. The preparation method comprises the following steps of crude product preparation and crystallization, wherein the step of crystallization adopts acetone and water as solvents. Levo-oxiracetam prepared through the preparation method has high purity above 99.3 wt% and low impurity content of 0 to 0.5 wt%. The preparation method has the advantages that a material addition mode adopted by the preparation method realizes that frequency of addition of an inorganic base is reduced; operation is simple; and the preparation method is in favor of industrialized production.

An (S)-4-hydroxy-2-oxo-1-pyrrolidine acetamide racemate referred to as (S)-oxiracetam crystal form II has a diffraction peak at a diffraction angle 2θ of 10.669, 13.25, 13.847, 14.198, 16.729, 17.934, 18.746, 18.816, 20.273, 20.413, 21.431, 21.617, 21.663, 23.38, 24.324, 24.415, 26.069, 26.107, 27.901, 28.621, 28.925, 29.449, 29.484, 31.702, 36.516, 37.685, or 39.721 degrees. The purity of the (S)-oxiracetam crystal form II can be up to 98.5%, and the (S)-oxiracetam crystal form II has the advantages of simple preparation method, mild control condition, low production cost, and the produced oxiracetam hydrate crystal form II has a high purity (the oxiracetam hydrate crystal form having a purity of 8%˜98.5% can be prepared by a crude levo-oxiracetam having a purity of 92%, and thus having a good reproducibility in production.

The invention belongs to the field of medicine synthesis, and particularly relates to an oxiracetam derivative and a method for preparing (S)-4-hydroxy-2-oxo-1-pyrrolidinyl acetamide from the derivative. The derivative is prepared from racemate oxiracetam and phthalic anhydride under the existence of pyridine and then reacts with a resolving agent of (S) type chiral amine to obtain solid, and the solid is acidified and extracted and then hydrolyzed under the alkaline condition to obtain (S)-4-hydroxy-2-oxo-1-pyrrolidinyl acetamide. The method is high in yield, good in product purity and suitable for the large-scale industrial preparation method.

A preparation method of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide comprises allowing reaction of ethyl glycinate hydrochloride and ethyl (S)-4-halo-3-hydroxybutyrate in alcohol solvent and alkaline conditions, filtering, washing, concentrating, extracting, separating, introducing ammonia water to obtain a crude product, and purifying the crude product, wherein the ethyl glycinate hydrochloride is dissociated by using diethyl ether and ammonia gas to obtain ethyl glycinate; the alcohol solvent is anhydrous methanol or anhydrous ethanol; and the alkaline condition is provided by sodium carbonate or sodium bicarbonate. The method adopts ethyl (S)-4-halo-3-hydroxybutyrate and ethyl glycinate hydrochloride as main raw materials, which has the characteristics of cheap and easily-accessible raw material, environment friendliness and no pollution; and the method firstly carries out dissociation on the ethyl glycinate hydrochloride, which effectively reduces the material consumption in reaction and lowers the cost, and simultaneously plays a positive role in the reaction yield. The method has the characteristics of low preparation cost, high yield up to 36% and mild reaction conditions, and is suitable for industrial production. The prepared (S)-oxiracetam product has high performance liquid chromatography (HPLC) purity up to above 98.5%.

The present invention relates to a method for treating a patient having suffered from severe aphasia associated with cerebrovascular accident chronic stage for at least three years, wherein said treatment consists essentially of administering a composition comprising 2-oxo-1-pyrrolidineacetamide as an active ingredient and a pharmaceutically acceptable carrier.

The invention relates to a stable preparation for injection by taking S-oxiracetam as active ingredient. The preparation is a composition for injection, and is formed by the S-oxiracetam or salts thereof serving as active ingredient and pharmaceutically acceptable auxiliary material. To restrain the racemization of the S-oxiracetam, when the powder injection with the active ingredient is prepared, and only the pH value of the S-oxiracetam medicament solution ranges from 4.5 to 7.0, the pH value is between 5.4 to 6.6 preferably, so that the S-oxiracetam medicament solution can be produced, and the final freeze-dried product has acceptable long stability; and moreover, when injection is produced, a rotary steam sterilization method needs to be adopted, terminal rotating sterilization is performed for 15 to 45 minutes under the temperature of 121 DEG C, and the terminal rotating sterilization is performed for 15 to 20 minutes preferably, so that the S-oxiracetam injection with high purity can be obtained and has acceptable long stability.

The invention relates to a preparation method of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide. The preparation method comprises the following steps of: taking glycine ethyl ester hydrochloride and ethyl-(S)-4-halo-3-hydroxy-butanoate as raw materials, reacting in an alcohol solvent under alkaline conditions, washing with an inorganic alcohol, concentrating, extracting, separating, and introducing ammonia water to get a crude product of the (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide; and performing purification treatment on the crude product, wherein the glycine ethyl ester hydrochloride firstly needs to adopt ethyl ether and ammonia gas to dissociate so as to get glycine ethyl ester. The main raw materials adopted in the preparation method disclosed by the invention are the ethyl-(S)-4-halo-3-hydroxy-butanoate and the glycine ethyl ester hydrochloride, and the raw materials are low in price, easy to obtain, environment-friendly and pollution-free; and according to the preparation method disclosed by the invention, dissociation treatment is firstly performed on the glycine ethyl ester hydrochloride, thus the using quantity of the materials in the reaction is effectively reduced, the cost is lowered, and a positive role is simultaneously played for the reaction yield. (S)-oxiracetam prepared by the preparation method disclosed by the invention has low cost, high yield which is as high as 36% and mild reaction conditions, and is conductive to industrialized large-scale production, and the HPLC (high-performance liquid chromatography) purity of the prepared (S)-oxiracetam product is above 98.5%.