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AssigneeEsteve Quimica, S.A.
InventorsJuan Jose Surroca, Llorenc Rafecas Jane, Lourdes Garriga Sanahuja, Miquel Pericas Brondo, Lluis Carandell
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A process for obtaining the pharmaceutical active ingredient, levetiracetam, by means of deaminomethylation of a sufficiently pure enantiomer intermediate (S)-(II), or by means of deaminomethylation of an addition salt thereof with an acid, wherein R1 and R2 are either the same or different (C1-C6)-alkyl radicals, or else R1 and R2 together with the nitrogen atom to which they are bonded form a radical selected from the group consisting of 1-pyrrolidinyl, 1-piperidinyl, 1-morpholinyl, 1-piperazinyl and 1-[4-(C1-C4)-alkylpiperazinyl]. The invention also comprises preparing the sufficiently pure enantiomer intermediate (S)-(II) by treating the corresponding chemically new racemic intermediate (II) with an amine resolving agent, followed by selective crystallisation of a diastereoisomeric salt thereof. It is useful for obtaining levetiracetam on an industrial scale and involves neither hydrogenation nor chromatography.
A process for preparing levetiracetam (S)-(I), comprising subjecting the sufficiently pure enantiomer intermediate of general formula (S)-(II) or an addition salt thereof with an acid, to a deaminomethylation relation,
An intermediate compound of formula (II), its stereoisomers, mixtures thereof, solvates, addition salts of any of the foregoing, solvates of said addition salts, and hydrates of said addition salts, wherein R1 and R2 are the same or different (C1-C6)-alkyl radicals, or R1 and R2 together with the nitrogen atom to which they are bonded form a radical selected from the group consisting of 1-pyrrolidinyl, 1-piperidinyl, 1-morpholinyl, 1-piperazinyl and 1-[4-(C1-C4)-alkylpiperazinyl].
Dependencies are inferred from the claim text.