Egyt Gyogyszervegyeszeti Gyar

Egis Gyogyszergyar

Laszlo Rozsa

Lujza E Petocz

Gabor Gigler

Ibolya Kosoczky

Eniko Szirt Nee Kiszelly

Katalin Grasser

Jozsef Nagy

Eniko Kiszelly

Marton Fekete

Istvan Gacsalyi

Janos Fischer

Peter Tompe

Maria Szecsey Nee Hegedus

Pal Vago

Gabor Fazekas

Anna Bakonyi

Dioxazocine derivatives, their preparation and composition containing them, said derivatives being represented by the formula I ##STR1## wherein R.sub.1 represents hydrogen or alkyl having from 1 to 4 carbon atoms,

Dioxazocine derivatives compositions and methods containing them having

The invention relates to optically active 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]dioxaz ocine of the Formula ##STR1## and pharmaceutically acceptable acid additional salts thereof. The enantiomers are especially active against Parkinsion's disease. The optically active enantiomers are prepared by

Optically active

The invention relates to a novel process for the preparation of 1-[3-mercapto-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid through the N-acylation of L-proline. According to the process of the invention L-proline is acylated with a 3-halogen-2-methylpropionyl chloride of the formula III ##STR1## wherein Hal is a halogen atom, preferably chlorine or bromine, the obtained 1-[3-halogen-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid, wherein Hal is as stated above, is reacted with an alkali thiosulfate or alkali trithiocarbonate and the reaction product is hydrolized with an acid. The process of the invention is very economical as compared with the known processes. The desired product is prepared from methacrylic acid in 4 reaction steps with a total yield of 25 percent and from L-proline in 2 reaction steps with a total yield of 30 percent.

Process for the preparation of

This invention relates to novel dibenzo[d,g][1,3,6]dioxazocine derivatives represented by the general formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, cyano or trifluoromethyl,

Dibenzo[d,g][1,3,6]dioxazocine derivatives

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Budapest, Hungary

Laszlo Rozsa