New anthracyclinones and their production
AssigneeMeiji Seika Kaisha, Ltd.
InventorYoshito Kishi
Life of this patent
Estimating the term…
Abstract
A new compound of the formula ##STR1## wherein R.sup.1 is a hydrogen atom, a hydroxyl group or an alkoxyl group of 1-4 carbon atoms and R.sup.2 is an ethyl group or acetyl group is now provided, which is an intermediate compound useful for synthesis of antitumor anthracyclines. This new anthracycline is produced by cyclization of a new compound of the formula ##STR2## wherein R.sup.1 is as defined above and TMS denotes a trimethylsilyl group, followed by decarboxylation of the cyclization product.
Claims14
A compound of the formula ##STR64## wherein R.sup.1 denotes a hydrogen atom, a hydroxyl group or an alkoxyl group of 1-4 carbon atoms and R.sup.2 denotes an ethyl group or an acetyl group.
A process for the production of a compound of the formula ##STR65## wherein R.sup.1 denotes a hydrogen atom, a hydroxyl group or an alkoxyl group of 1-4 carbon atoms and R.sup.2 denotes an ethyl group or an acetyl group, which comprises the steps of:
- (a) cyclizing the compound of the formula ##STR66## wherein R.sup.1 and R.sup.2 are as defined above and TMS denotes a trimethylsilyl group by treating with a base in an organic solvent to produce the compound of the formula ##STR67## wherein R.sup.1, R.sup.2 and TMS are as defined above, and (b) decarboxylating the compound of the formula (I') by treating the latter with a tetra-alkyl ammonium fluoride or hydrogen fluoride in an organic solvent to produce the desired compound of the formula (I).
A compound of the formula (II) ##STR84## wherein R.sup.1 is a hydrogen atom, a hydroxyl group or an alkoxyl group of 1-4 carbon atoms and R.sup.2 is an ethyl group or an acetyl group.
Dependencies are inferred from the claim text.