Egis Gyogyszergyar

Egis Gyogyszergyar Rt.

Elemer Jakfalvi

Ivan Beck

Andras Dietz

Lujza E Petocz

Marton Fekete

Attila Mandi

Gabor Gigler

Frigyes Gorgenyi

Istvan Simonyi

Gabor Blasko

Eniko Szirt Nee Kiszelly

Eniko Kiszelly

Geza Schneider

Agnes Kovacs Nee Palotai

Katalin Zukovics Nee Sumeg

Gabriella Rmos Nee Lassu

Klara Gado

Maria Hegedus

Ilma Dinnyes Nee Nagy

Katalin Sumeg Nee Zukovics

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 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

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Budapest, Hungary

Elemer Jakfalvi