Process for producing 10-hydroxyanthracyclines

Details Process for producing 10-hydroxyanthracyclines Process for producing 10-hydroxyanthracyclines

1987-06-30

1989-10-31

Griffin, Ronald W.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

552201, C07H 1524, C07C 4966

Patent

active

048778702

ABSTRACT:
Disclosed is a process for producing a 10-hydroxyanthracycline of the following formula (II) which comprises reacting a compound of the following formula (I) or an acid addition salt thereof with an N-oxide of a tertiary amine ##STR1## wherein: R.sup.1 through R.sup.6 each designate any of H, OH and OCH.sub.3 ; R.sup.7 designates any of H, OH and a sugar residue; and R.sup.8 designates any of C.sub.2 H.sub.5, COCH.sub.3, CH(OH)CH.sub.3, CH(OH)CH.sub.2 (OH) and COCH.sub.2 OH. In accordance with this process, it is possible to efficiently introduce a hydroxyl group into the 10-position of an anthracycline having no substitutent at the same position thereof.

REFERENCES:
patent: 4045498 (1977-08-01), Deno
patent: 4457920 (1984-07-01), Mrozik
patent: 4617146 (1986-10-01), Helmlinger et al.

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