10(ALPHA)-METHOXY-6-METHLERGOLIN-DERIVATE, VERFAHREN ZU DEREN HERSTELLUNG UND ARZNEIMITTELPRAEPARATE

A process for the preparation 10???-methoxy-6-methyl-ergoline derivatives of formula (I> wherein R is hydrogen or methyl, X is hydrogen, chlorine, bromine oriodine, R' is hydrogen or a 5-bromo-nicotinoyl group, and physiologically acceptable acid addition salts thereof, comprises photochemic...

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Hauptverfasser: KISS,BELA, STEFKO,BELA,.DR, SZPORNY,LASZLO,DR, PALOSI,EVA,DR, MEGYERI,GABOR,..DR, LAPIS,ERZSEBET, GROO,DORA,DR, BOGSCH,ERIK, KARPATI,EGON,DR, LASZLOVSZKY,ISTVAN,DR, GALAMBOS,JANOS,..DR, SZOMBATHELYI,ZSOLT,DR, ZIEGER,ANNA,. KASSAI,GEB, TRISCHLER,FERENC,.DR, KEVE,TIBOR,.DR
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Zusammenfassung:A process for the preparation 10???-methoxy-6-methyl-ergoline derivatives of formula (I> wherein R is hydrogen or methyl, X is hydrogen, chlorine, bromine oriodine, R' is hydrogen or a 5-bromo-nicotinoyl group, and physiologically acceptable acid addition salts thereof, comprises photochemical methoxylations of a 2-halo-lysergol, optionally followed by modification of the groups at R, X and R . The partly new compounds of formula (I) are valuable intermediates in the preparation of nicergoline, a potent peripheral vasodilator. Moreover, the compounds of formula (I) in which R is Hormethyl, R' is H and X is chlorine, bromine or iodine claimed per se, show D2-receptor blocking activity.