- Preparation method of levetiracetam intermediate
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The invention relates to a preparation method of alpha-ethyl-2-oxo-1-pyrrolidine acetate. Particularly, by optimizing a post-treatment process, the reaction yield and the product purity are remarkably improved.
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Paragraph 0039-0041
(2022/01/08)
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- Preparation method of levetiracetam and intermediates thereof
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The invention provides a preparation method of levetiracetam and intermediates thereof. The specific steps are as follows: dropwise adding pyrrolidone into a toluene solution of sodium methoxide or sodium hydride, performing concentrating to dryness after a reaction is completed, adding toluene again, dropwise adding ethyl 2-bromobutyrate, and carrying out a reaction by heating to obtain a compound of a formula 3; adding a NaOH aqueous solution to the compound of the formula 3, performing heating until a reaction is completed, and dropwise adding concentrated hydrochloric acid to precipitate acompound of a formula 4; carrying out a reaction of the compound of the formula 4, R-(+)-phenylethylamine, and triethylamine to obtain a compound of a formula 6; performing hydrolysis by a NaOH solution, acidification by concentrated hydrochloric acid, and purification to a compound of a formula 7; and performing esterification by TsOH/EtOH to obtain a compound of a formula 8, and then performingammonia hydrolysis to obtain levetiracetam.
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Paragraph 0043-0046
(2020/01/08)
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- REACTIONS OF N-SILYLATED LACTAMS WITH α-BROMO CARBOXYLATES
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The reactions of N-trimethylsilyl lactams with α-bromo carboxylates proceeds in two directions: the N-alkylation of the lactams, and elimination with the formation of α,β-unsaturated carboxylic esters.The proportion between the two processes depends on the structure of the initial compounds.
- Orlova, N. A.,Shipov, A. G.,Baukov, Yu. I.
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p. 1877 - 1880
(2007/10/02)
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- POTENTIAL NOOTROPIC AGENTS: SYNTHESIS OF A SERIES OF (2-OXO-1-PYRROLIDINYL)ACETIC ACID PIPERAZIDES
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The title compounds VI-XXIII were prepared by heating ethyl (2-oxo-1-pyrrolidinyl)acetate (II) with a series of N-monosubstituted piperazines.The propionamides XXVI and XXX were obtained by reactions of the acid chlorides IV and XXXIII with 3-(1-piperazinyl)propionamide.Compounds VI (VUFB-13 763) and VIII (VUFB-14 745) proved more active than piracetam (I) by their antiamnestic effects in rats by antagonising the brain demaging effects of cycloheximide in infantile rats, and by their potentation of the effects of anticolvunsant agents.
- Valenta, Vladimir,Sindelar, Karel,Holubek, Jiri,Ryska, Miroslav
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p. 1613 - 1629
(2007/10/02)
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