Deutsche Gold- Und Silber-scheideanstalt Vormals Roessler

Karl H Klingler

Klaus Thiemer

Fritz Stroman

Axel Kleemann

Heribert Offermanns

Erich Bickel

Ansgar Von Schlichtegroll

Rudolf Aurich

Horst Traube

Franz Hitzel

Silke Habersang

Erik Westermann

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

Optically active bases are prepared by reacting the racemic base with an optically active half amide of an unsaturated aliphatic dicarboxylic acid of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are the same of different and are hydrogen, halogen, a hydroxy group, a methyl group or a methoxy group or two of R.sub.1, R.sub.2 and R.sub.3 together are a methylenedioxy group, R.sub.4 is hydrogen or a methyl group, R.sub.5, R.sub.6 and R.sub.7 independently are hydrogen or a C.sub.1 -C.sub.4 alkyl group and n is 0 or 1 and optionally splitting an optically homogeneous salt fraction into the corresponding optically active base and the added half amide.

Process for production of optically active bases

There are prepared compounds of the formula ##STR1## in which T is the theophyllin-7-yl group and alk is a straight or branched alkylene chain with 2 to 4 carbon atoms and salts thereof. The compounds promote circulation and produce a marked and persistent increase in renal circulation.

Dihydroxyphenylethylaminoalkyl theophyllines

There are prepared compounds corresponding to the general formula

Basic substituted xanthine derivatives

There are prepared quaternary xanthinylalkylnortropine derivatives of the general formula I ##STR1## where T represents a theophyllinyl-7 radical or a theobrominyl-(1)-radical, Alk is a straight or branched chain alkylene group having 2 to 10 carbon atoms or such a group substituted by a hydroxyl group, R is an alkyl group of 1 to 4 carbon atoms and A.sup.(-) is an equivalent to an anion of a physiologically compatible mono- or polyvalent acid. The compounds are useful as medicines having a spasmolytic activity.

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Langen, Germany

Karl H Klingler