Egis Gyogyszergyar

Egyt Gyogyszervegyeszeti Gyar

Egis Gyogyszergyar Rt.

Ivan Beck

Attila Mandi

Frigyes Gorgenyi

Istvan Simonyi

Andras Dietz

Elemer Jakfalvi

Lujza E Petocz

Marton Fekete

Pal Benko

Gabor Gigler

Gabor Blasko

Kalman Nagy

Daniel Bozsing

Peter Tompe

Laszlo Levai

Janos Imre

Geza Schneider

Eva Furdyga

Agnes Kovacs Nee Palotai

Eva J Tajthy Nee Juhasz

Gabriella Rmos Nee Lassu

Gyorgyi Kovanyi Nee Lax

Gyorgy Mikite

Gyorgyi Zalavari Nee Dosa

Eva Poczik

Ilona Dinnyes Nee Nagy

Erzsebet Kiss Nee Bertok

Ilma Dinnyes Nee Nagy

Eniko Szirt Nee Kiszelly

Jozsef Rakoczi

Eniko Kiszelly

Judit Kun

Katalin Zukovics Nee Sumeg

Klara Gado

Maria Hegedus

Csaba Kiss

Imre Horvath

Miklos Nemes

Katalin Sumeg Nee Zukovics

Elemer Jakflavi

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 process for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitro-phenyl)-pyridine-3,5-dicarbo xylate of the Formula I ##STR1## which comprises a) reacting a compound of the general Formula II ##STR2## (wherein n is 1 or 3; if n is 1, then R stands for a group of the Formula (a) ##STR3## and if n is 3, then R represents hydrogen) with methyl acetoacetate of the Formula III

1,4,Dihydro-pyridine intermediates

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

The invention is directed to processes for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitrophenyl)-pyridine-3,5-dicarbox ylate by reacting 1-methoxy-1-(2'-nitrophenyl)-N-(2'-nitrophenyl)methylene methanamie or 1-(2'-nitrophenyl)-N,N'-bis-(2'-nitrophenyl) methylene methanediamine with methyl acetoacetate in the presence of an amine compound or by reacting the monomeric or trimeric from of 2-nitrobenzaldimine with methyl acetoacetate.

Process for the preparation of 1,4-dihydro-pyridine derivatives

The compounds of the general Formula I ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different and each stands for hydrogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy-C.sub.1-6 alkoxy, C.sub.2-6 alkenyloxy or phenyl-(C.sub.1-3 alkoxy), or R.sup.1 and R.sup.2 together form C.sub.1-2 alkylenedioxy; with the proviso that at least one of symbols R.sup.1 and R.sup.2 is other than hydrogen and with the further proviso that R.sup.1 and R.sup.2 can not represent 3,4-dimethoxy substitution) and their pharmaceutically acceptable acid addition salts exhibit useful analgesic, antipyretic, anti-inflammatory, anti-anginal and antioxidant effect.

Pharmaceutical compositions

The invention relates to pharmaceutical compositions having analgesic and/or anti-inflammatory effect comprising as active ingredient 2,4-diamino-5-(3,4-dimethoxy-benzyl)-pyrimidine or a pharmaceutically acceptable acid addition salt thereof.

Pharmaceutical composition

The invention relates to a novel process for preparing 2-guanidinomethyl-perhydroazocine-sulfate of formula I ##STR1## comprising the steps of catalytically reducing the 2-nitromethylene-perhydroazocine of formula IV ##STR2## in solution in acetone at a temperature of 20.degree. to 50.degree. C, treating the separated reaction product with an aqueous mineral acid and then reacting it with S-methyl-isothiocarbamid-sulfate. The process gives the desired end-product of formula I also on industrial scales.

Process for preparing 2-guanidinomethyl-perhydroazocine-sulfate

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Budapest, Hungary

Ivan Beck