Egis Gyogyszergyar

Egis Gyogyszergyar Rt.

Gyogyszerkutato Intezet

Helm Ag

Cf Pharma Gyogyszergyarto Kft.

Geza Schneider

Gabor Blasko

Ivan Beck

Agnes Kovacs Nee Palotai

Andras Dietz

Gabriella Rmos Nee Lassu

Ilma Dinnyes Nee Nagy

Ferenc Andrasi

Istvan Elekes

Pal Berzsenyi

Sandor Elek

Istvan Polgari

Judit Kun

Geza Arvai

Elemer Jakfalvi

Arpad Lazar

Elemer Jakflavi

Zsolt Viski

Attila Gergely Mate

Sandor Garaczi

The present invention relates to a process for the preparation of topiramate, intermediates in this process and a process for the preparation of these intermediates.

Process for the preparation of topiramate

The invention relates to a novel process for preparing 1-[/2S/-methyl-3-mercaptopropionyl]-pyrrolidine-/2S/-carboxylic acid of the formula I ##STR1## in which 1-[/2S/-methyl-3-thiocyanatopropionyl]-pyrrolidine-/2S/-carboxylic acid of the formula II ##STR2## is dissolved in an aqueous mineral acid, the solution obtained is diluted with water and the 1-[/2S/-methyl-3-carbamoylthiopropionyl]-pyrrolidine-/2S/-carboxylic acid of the formula III ##STR3## that forms is hydrolized with an aqueous solution of a base.

Process for preparing 1-[/2S/-methyl

The invention relates to a novel process for preparing 1-[(2S)-3-mercapto-2-methyl-1-oxopropyl]-L-proline (captopril) of formula (I). ##STR1## which comprises hydrogenolysing 1-[(2S)-2-methyl-1-oxo-3-rhodanidopropyl]-L-proline of formula (II) ##STR2## in an inert solvent, in the presence of a catalyst, at a temperature of 50.degree. to 120.degree. C. under a pressure of 10.sup.5 to 10.sup.7 Pa. The above compound of formula (II) is new and can be prepared by acylating L-proline with a reactive acylating derivative of (2S)-2-methyl-3-rhodanido-propionic acid of formula (III). ##STR3##

Process for preparing 1-(2S)-3-mercapto-methyl-1-oxopropyl)-L-proline

4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;

Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives

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Budapest, Hungary

Geza Schneider