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.

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.

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%.