METHOD OF 3-[2-(DIMETHYLAMINO)ETHYL]-N-METHYL-1H-INDOL-5- -METHANESULPHONAMIDE PREPARATION

Prodn. of 2-carboxy-3-(2-(dimethyl-amino) ethyl-N-methyl-IH-indol-5-methano sulphonamide (I) and its lower alkyl esters comprises reacting cpd. of formula (III) (where ALK is lower alkyl; and x is a leaving gp. e.g. halo, mesyl or hosyl) with Me2NH in the presence of a solvent, to give a cpd. of for...

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Hauptverfasser: OLONDRIZ FRANCISCO M, BARJOAN PERE D, ROVIRA ANA BOSCH, CALDERO GES J. M
Format: Patent
Sprache:eng ; slo
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Zusammenfassung:Prodn. of 2-carboxy-3-(2-(dimethyl-amino) ethyl-N-methyl-IH-indol-5-methano sulphonamide (I) and its lower alkyl esters comprises reacting cpd. of formula (III) (where ALK is lower alkyl; and x is a leaving gp. e.g. halo, mesyl or hosyl) with Me2NH in the presence of a solvent, to give a cpd. of formula (II), which is saponified to give (7). There is disclosed a method for the preparation of 3-[2- -(dimethylamino)ethyl]-N-methyl-1H-indol-5-methanesulphonamide having the formula (I) that is processed by decarboxylation of 2-carboxy-3-[2-(dimethylamino)ethyl]-N-methyl-1H-indol-5- -methanesulphonamide of the formula (II) in the presence of a copper catalyst, under inert atmosphere, at temperature ranging from 190 to 250 degrees Celsius. Said compounds of the formula (I), the salts and solvates thereof are useful in the treatment of migraine.