| 摘要 |
<p>The present invention provides in a process for the production of a theophylline derivative of the general formula 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 comprises reaction of an aminoalkyltheophylline of the formula II wherein T and Alk are as above, with a bromoketone of the general formula 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 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 V wherein R, R' and n are as above with after-treatment with a lower trialkylphosphite.</p> |
