Pure enantiomers of 4,5-disubstituted gamma-butyrolactams, and t

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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548532, 548533, 548534, A61K 3140, C07D20708, C07D20712

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active

048472875

ABSTRACT:
The invention provides pure enatiomers of 4,5-disubstituted .gamma.-butyrolactams of the general formula ##STR1## By means of the pure enantiomers of 4,5-disubstituted .gamma.-butyrolactams (I), according to the invention, it is now possible to synthesize (+)-(3R), (4S), (5S), (7R)-3-hydroxy-5-.alpha.-hydroxybenzyl-1-methyl-4-phenyl-pyrrolidin-2-one and derivatives in the form of pure enantiomers.

REFERENCES:
patent: 3178347 (1965-04-01), Bocher
patent: 4296110 (1981-10-01), Johnson
patent: 4731455 (1988-03-01), Hartwig
Burger, Medicinal Chemistry, 2nd Edition, 1960, pp. 42-43.
Hartwig et al., Chem. Abst. vol. 95 (1981) 62704c.
Chemische Berichte, Jahrgang 100, Heft 4, 1967, Seiten 1137-1143 F. Zymalkowski et al.: "Eine Stereoselektive Synthese von Cisund Trans-3-Phenyl-2-Carboxy-Pyrrolidon-(5)", *Seite 1138, Beispiel 2b.sub.2 *.
Synthesis, Nr. 9, Sep. 1986, Seiten 737-740 U. Schollkopf et al.: "Assymmetric Synthesis via Heterocyclic Intermediates. XXX. Asymmetric Synthesis of Glutamic Acids and Derivatives thereof by the Bislactim-Ether Method. Michael-Addtion of Methyl 2-Alkenoates to the Lithiated Bislactim-Ether of Cyclo-(L-Val-Gly)", *Insgesamt*.

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