Egyt Gyogyszervegyeszeti Gyar

Egis Gyogyszergyar Rt.

Gis Gyogyszergyar Rt.

Anna Bakonyi

Pal Vago

Imre Moravcsik

Istvan Gyertyan

Ferenc Andrasi

Tamas Hamori

Pal Berzsenyi

Jozsef Reiter

Gabor Zolyomi

Eszter Szentkuti

Katalin Horvath

Edit Horvath

Gyorgyne Mate

Gyula Simig

Gabor Gigler

Istvan Gacsalyi

Gabor Blasko

Janos Fischer

Andras Egyed

Gyorgy Somogyi

Laszlo Rozsa

Andras Bilkei-Gorzo

Gabor Fazekas

Karoly Tihanyi

Judit Bajnogel

Erszebet Birkas

Peter Botka, Deceased

Jeno Korosi, Deceased

Cecilia Salamon Haskane

Peter Korosi

Hilda Botka

Klara Daroczi Kazone

The invention relates to new 1-[2-(substituted vinyl)]-3,4-dihydro-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof and pharmaceutical compositions comprising them. The new 1-[2-(substituted vinyl)]-3,4-dihidro-5H-2,3-benzodiazepine derivatives according to the invention correspond to the general formula (I), ##STR1## wherein the variables are hereinbelow defined: The new compounds according to the invention affect the central nervous system and can be used to advantage in the therapy.

1-[2-(substituted vinyl)]-3,4-dihydro-4-dihydro-5H-2,3-benzodiazepine

This invention relates to new 1-�2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said benzodiazepine derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The compounds according to the invention correspond to the general formula (I), ##STR1## wherein the variables are herein below defined, and the compounds possess central nervous activities.

1-�2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives

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

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Budapest, Hungary

Anna Bakonyi