A. Villalobos et al., TOTAL SYNTHESIS OF A NOVEL BENZ[A]ANTHRACYCLINE ANALOG OF THE ANTITUMOR AGENT 4-DEMETHOXYDAUNORUBICIN, Bioorganic & medicinal chemistry letters, 4(23), 1994, pp. 2781-2786
The total synthesis of 2S, ydro-2,5,6-trihydroxy-benz[a]anthracene-7,1
2-dione (5) and its 2R, 4R-diastereomer (23) was accomplished in 11 st
eps (1.4% overall yield) from 5,6-dimethoxy-2-tetralone (8). These ang
ular analogs of 4-demethoxydaunorubicin were inactive in tissue cultur
e assays in comparison with doxorubicin.