Process for the production of basic substituted alkyltheophyllin

Organic compounds -- part of the class 532-570 series – Organic compounds – Chalcogen bonded directly to ring carbon of the purine ring...

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424253, C07D47308

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active

042450934

ABSTRACT:
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.

REFERENCES:
patent: 3728346 (1973-04-01), Klingler
Kloetzel J. Org. Chem., vol. 20, pp. 38-49, (1955).
Klingler, Arzneimittelforschung, vol. 27, pp. 4-14, (1977).

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