University of Pennsylvania

Adria Laboratories Inc.

Domingo Dominguez

Michael P Cava

It has been found that stereospecific R(-)-4-demethoxy-7-deoxydaunomycinone can be synthesized from the known compound 4-demethoxy-7,9-dideoxydaunomycinone. R(-)-4-Demethoxy-7-deoxy-daunomycinone is an intermediate in the synthesis of (+)-4-demethoxydaunomycinone, the aglycone of the nonnaturally occurring and antitumor active (-)7(S)9(S)-4-demethoxydaunorubicin.

Synthesis of (+)-4-demethoxydaunomycinone

A synthesis of 4-demethoxydaunomycinone and its derivatives from the known compound 9-acetyl-6,11-dihydroxy-7,8,9,10-tetrahydro-5,12-naphthacenedione. 4-Demet hoxydaunomycinone may be converted to 4-demethoxydaunorubicin which is an anthracycline derivative known to have antitumor activity.

Growing community of inventors

Santiago de Compostela, Spain

Domingo Dominguez