Naphthacenequinone derivatives and process for their preparation

摘要

A suitable process for the synthesis of anthracyclinone derivatives of the general formula (I) <IMAGE> and their analogues which are substituted in the 1, 2, 3 and 4 position is described. According to the process, a suitable quinizarin quinone is reacted with 2-( alpha -hydroxyethyl)-1,3-butadiene under Diels-Alder conditions. After this, aromatisation and suitable manipulation of the side chain of the resulting adduct follows. The process products are important intermediates in the synthesis of daunorubicin and its analogues, which are useful antibiotics in the treatment of certain neoplastic diseases.