Development of New Antitumor Anthracyclines

A short and efficient synthesis of a C-7 CH2 analog of 4-demethoxyadriamycin-9-one as a nearly equimolar mixture of diastereomers is described. The Diels-Alder cycloaddition, deoxygenation and concomitant enolization-tautomerization can be done in a single pot.