- Synthesis process of levetiracetam
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The invention relates to the technical field of pharmaceutical preparation, in particular to a preparation method of an antiepileptic drug. The synthesis process of levetiracetam designed by the invention takes (S)-2-(4-chlorobutyramide) butyric acid as an initial raw material, pyridine as an alkali and (Boc)2O as an activating reagent of carboxylic acid, an ammonium salt is added to prepare (S)-2-(4-chlorobutyramide) butyramide, and finally a cyclization reaction is carried out in the presence of alkali to obtain levetiracetam. The process does not need chemical resolution, does not use highly toxic or corrosive chemical reagents, is simple to operate, mild in conditions, environment-friendly and high in finished product quality, and is suitable for industrial production.
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Paragraph 0031-0033; 0036-0038
(2019/01/14)
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- Levetiracetam and pharmaceutical composition containing the same
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The invention provides high-purity levetiracetam and a pharmaceutical composition comprising high-purity levetiracetam. The high-purity levetiracetam is prepared with a one-pot method. According to the invention, (S)-2-aminobutyryl hydrochloride is adopted as an initial material, and is subjected to condensation and cyclization with 4-chlorobutyryl chloride, such that levetiracetam with a purity higher than 99.5% and with unknown individual impurity lower than 0.05% is obtained. Further, the levetiracetam obtained with the above method is dissolved in an organic solvent; the solution is filtered with a filter of 0.22-0.45mum while still hot, such that a chloride-qualified product with a chloride impurity amount lower than 0.02% can be obtained with high conversion rate. According to the invention, levetiracetam purity can be substantially improved, and a raw material and a pharmaceutical composition with excellent qualities can be further obtained.
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Paragraph 0053; 0054; 0055; 0060; 0061; 0062 0067; 0068
(2017/08/25)
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- PROCESSES FOR THE PREPARATION OF LEVETIRACETAM, ITS INTERMEDIATE AND THE USE OF LEVETIRACETAM IN PHARMACEUTICAL COMPOSITIONS
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The invention relates to processes for the preparation of (S)-2-aminobutanamide of Formula I, and to the use of the compound of Formula I as intermediate for the preparation of levetiracetam of Formula (II).The invention also relates to a process for the preparation of levetiracetam and pharmaceutical compositions that include the levetiracetam.
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Page/Page column 8-9
(2008/06/13)
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- PROCESS FOR PRODUCING LEVETIRACETAM
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The invention relates to a method of making optically and chemically pure levetiracetam and to the levetiracetam produced by such process.
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- (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide
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(S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (S)-2-aminobutanamide of the formula X--CH2 CH2 --Y--NHCH(C2 H5)CONH2 wherein Y is a --CH2 -- radical when X represents a ZOOC-- radical and Y is a --CO-- radical when X represents a HalCH2 -- radical, Z being a C1 -C4 alkyl radical and Hal a halogen atom. This laevorotatory enantiomer has been found to have significantly higher protective activity against hypoxia and ischemia than the corresponding racemate.
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