Process for the production of basic substituted...

C - Chemistry – Metallurgy – 07 – C

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C07C 69/95 (2006.01) C07D 473/08 (2006.01)

Patent

CA 1101856

ABSTRACT OF THE DISCLOSURE The present invention provides in a process for the production of a theophylline derivative of the general formula Image I wherein T is the theophylline - (7) - residue, Alk is a straight or branched alkylene chain with 2 - 4 carbon atoms, R is hydrogen or a methyl group, n is 1 or 2, and wherein two hydroxy groups of tne phenyl ring are other than in the 3,4 position, which com- prises reaction of an aminoalkyltheophylline of the formula Image II wherein T and Alk are as above, with a bromoketone of the general formula Image III wherein R represents hydrogen or a methyl group, R' is a lower alkyl residue, n is the number 1 or 2 and wherein two -OCOR'-groups of the phenyl ring are other than in the 3,4 position, to form an intermediate compound of the general formula Image IV where T, Alk, R, R' and n are as above and hydrolytic separation of the R'CO-protective group, the improvement in which the bromo ketone is a dibromide-free bromo ketone produced by bromination of a ketone of the general formula Image V wherein R, R' and n are as above with after-treatment with a lower trialkylphosphite.

330439

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