The method of obtaining anti-convulsants "barton"

 

The invention relates to pharmaceutical industry and relates to a method of receiving anticonvulsant drug, which is a 3-benzylpyrrolidine-2,4-dione (1), namely, that the aminouksusnoy acid esters acelerou anhydrides of monoamino malonic acid in the presence of the solvent chloroform, the resulting product is converted into 3-alkoxycarbonylmethyl-2,4 in an alcohol solvent in the presence of ciclismo agent sodium alcoholate, the resulting product carbalkoxy by three times with boiling acetonitrile, at a concentration of product (V) 20-30 g/l in the reaction mixture, followed by cooling, filtration, distillation of acetonitrile, the resulting pyrrolidin-2,4-dione is administered in the reaction with the corresponding dialkylated of dimethylformamide or triakontameron, the resulting product is treated with benzylamine at 0-5oWith subsequent isolation of the target product. The method allows to increase the yield of the final product without further purification stages, and to provide a higher degree of purity of the drug. 2 C.p. f-crystals.

Description text in facsimile form (see graficheski a 3-benzylpyrrolidine-2,4-dione (1), with anticonvulsant activity, characterized in that the esters aminouksusnoy acid acelerou anhydrides of monoamino malonic acid in the presence of the solvent chloroform, the resulting product (IV) is converted into 3-alkoxycarbonylmethyl-2,4 (V) in an alcohol solvent in the presence of ciclismo agent sodium alcoholate, carbalkoxy (V) by three times with boiling acetonitrile, at a concentration of product (V) 20-30 g/l in the reaction mixture, followed by cooling, filtration, distillation of acetonitrile, the resulting pyrrolidin-2,4-dione is administered in the reaction with the corresponding dialkylated of dimethylformamide or triakontameron, then the obtained product is treated with benzylamine at 0-5With subsequent isolation of the target product.

2. The method according to p. 1, characterized in that the product obtained 3-benzylpyrrolidine-2,4-dione is subjected to recrystallization from 85% aqueous acetone in the ratio 1:4.

The method according to PP.1 and 2, characterized in that the target product is mixed with pharmaceutically acceptable excipients.

 

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