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US 2010/0076204 A1Published application
Process for the preparation of levetiracetam
AssigneeZach System S.P.A.
InventorsMassimiliano FORCATO, Ivan MICHIELETTO, Paolo MARAGNI, Franco MASSACCESI, Livius COTARCA
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Abstract
The present invention relates to a process for the preparation of levetiracetam and, more particularly, to an improved process for the preparation of levetiracetam characterized by a crystallization-induced dynamic resolution of a diastereoisomeric mixture of an (±)-alpha-ethyl-2-oxo-1-pyrrolidine acetamide derivative.
Claims27
A process for the preparation of levetiracetam which comprises a crystallization-induced dynamic resolution of a diastereoisomeric mixture of an (±)-alpha-ethyl-2-oxo-1-pyrrolidine acetic amide of formula
- wherein
- R1 is hydrogen or a benzyl group;
- R2 is a 1-phenylethyl group optionally substituted on the phenyl ring by nitro or (C1-C4)-alkoxy;
- a 1-phenylpropyl group;
- a 1-naphtylethyl group;
- a 3-pinylmethyl group;
- or R1 and R2 taken together form a 5 or 6 membered saturated heterocycle containing from 1 to 3 heteroatoms selected among nitrogen, oxygen and sulfur, substituted by one or more (C1-C4)-alkyl group;
- from basic catalysis.
5 more elements
A compound of formula
- wherein
- R1 is hydrogen or a benzyl group;
- R2 is a 1-phenylethyl group optionally substituted on the phenyl ring by nitro or (C1-C4)-alkoxy;
- a 1-phenylpropyl group;
- a 3-pinylmethyl group;
- or R1 and R2 taken together form a 5 or 6 membered saturated heterocycle containing from 1 to 3 heteroatoms selected among nitrogen, oxygen and sulfur, substituted by one or more (C1-C4)-alkyl group;
- its stereoisomers, mixture thereof and acid addition salts.
4 more elements
Dependencies are inferred from the claim text.