Deutsche Gold- Und Silber-scheideanstalt Vormals Roessler

Erich Bickel

Karl H Klingler

Karl-Heinz Klingler

Franz Hitzel

There is described a process for the production of theophylline derivatives of the formula ##STR1## where T is the theophyllinyl-(7)-residue, Alk is a straight or branched alkylene chain having 2 to 4 carbon atoms, R is hydrogen or a methyl group, n is 1 or 2 with the proviso that two hydroxy groups of the phenyl ring cannot be in the 3,4-positions by reacting an aminoalkyltheophylline of the formula ##STR2## with a bromoketone of the formula ##STR3## where R' is a lower alkyl group and the two --OCOR' groups of the phenyl ring cannot be in the 3,4 positions to an intermediate compound of the formula ##STR4## and subsequently hydrolytically splitting off the R'CO protective group wherein the bromoketone of formula III is produced free of dibromide by bromination of a ketone of the formula ##STR5## followed by treatment with a lower trialkyl phosphite.

Process for the production of basic substituted alkyltheophylline

Basic substituted alkyl theophylline derivatives of the formula ##STR1## in which Alk is a straight or branched chain alkylene group with 2 to 4 carbon atoms and R is hydrogen or a methyl group are produced by catalytic hydrogenation of compounds of the formula ##STR2## where the phenolic hydroxyl groups and/or the secondary basic nitrogen atom can contain protective groups using as the solvent a compound of the formula ##STR3## where R', R' and R'' are the same or different and are alkyl groups of 1 to 2 carbon atoms and R' together with R'' can also be an alkylene bridge with 3 to 4 carbon atoms and in a given case the protective groups present are split off.

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Frankfurt am Main, Germany

Erich Bickel