Selective demethylation of anthracycline derivatives

Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal

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C07C 8710

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039637603

ABSTRACT:
Anthracycline derivatives of the formula ##SPC1##
Wherein R.sub.1, R.sub.2, R.sub. 3 and R.sub.4 are independently selected from the group consisting of hydrogen, chlorine, bromine and methoxy, with the proviso that at least one of the substituents is methoxy, and wherein R.sub.5 is selected from the group consisting of hydrogen, OH OR and OCOR; R being an alkyl group of 1 to 4 carbon atoms are prepared, in a single step, by selectively demethylating a compound of the formula: ##SPC2##
Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above by treating same with an aluminum halide in the presence of a suitable solvent at a temperature of 0.degree. to 50.degree.C.

REFERENCES:
patent: 3201424 (1965-08-01), McCormick et al.
patent: 3636063 (1972-01-01), McCormick et al.
patent: 3665018 (1972-05-01), Jolles

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