Process for the manufacture of substituted pyrrolidinones

C - Chemistry – Metallurgy – 07 – D

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C07D 403/06 (2006.01) A61K 31/495 (2006.01) C07D 207/26 (2006.01) C07D 403/14 (2006.01)

Patent

CA 1312081

4-15730/+ Process for the manufacture of substituted pyrrolidinones Abstract Substituted pyrrolidin-2-ones of the formula Image (I) wherein R1 represents a phenyl or naphthyl radical that is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl, X1 represents lower alkylidene, X2 represents methylene, ethylene or oxoethylene and R2 represents hydrogen, lower alkyl or a radical of the formula Image (Ia), wherein X4 represents lower alkylidene and R3 represents hydrogen or a phenyl or naphthyl radical that is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl, and their pharmaceutically acceptable salts, having nootropic properties and being useful as nootropic active ingredients in medicaments are prepared, for example, by condensing with one another compounds of the formulae Image (II) and Image (III) wherein Z1 represents a group of the formula -X1-C(=O)-Z3 (IIa) and Z2 represents hydrogen, or Z1 represents hydrogen and Z2 represents a group of the formula -C(=O)-X1-Z4 (IIIa), wherein each of Z3 and Z4 represents a removable radical and R2 represents a radical R2 or an amino-protecting group, or their salts, and removing an amino-protecting group R2 which may be present.

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