Anthracycline antibiotics

A review with 18 references covering R&D work on anthracycline antibiotics carried out at the Pharmaceutical Research Institute (PRI), Warsaw, during the last decade. The main goal was antitumor drug idarubicin whose active ingredient, (+)-(7-S, 9-S)-9-acetyl-7-(3'-amino-2',3',6'-trideoxy-alpha-L-lyxo-hexapyranosyloxy-)-7,8,9,10-tetrahydro-6,9,11-trihydroxynaphthacene-5,12-dione, is prepared in a process involving 30 synthetic steps and more than hundred unit operations. The general strategy developed at PRI for anthracycline antibiotics involves, the total synthesis of aglycone and de novo synthesis of sugar moieties is quite flexible and can be applied to generic drugs as well as to new chemical entities, particularly to these modified in the sugar part.