| 摘要 |
<p>Prepn. of 8-R1-8-R2-7,8,9,10- tetrahydro-1,6,11- trimethoxy- 5,12-dioxo-naphthacenes of formula (VII) from new 2-R1-2-R2-1,2,3,4- tetrahydro-5- hydroxy-8- methoxynaphthalenes of formula (I) via new intermediates ; is claimed, (where R1 is COOR or CXMe; R is lower alkyl; X is opt. protected oxo; R2 is H or OH; R5 is lower alkyl; R10 is COOH or CXMe). . The steps in the process are carried out as follows: (a) reaction of (I) with (II) in the presence of an aromatic boronic acid and treatment of the resulting boronate ester with a diol; (b) reductive cleavage of the phthalide ring; (c) methylation and saponification; (d) cylisation and, if necessary, esterification; (e) oxidn. The cpds. are intermediates for antibacterial and antitumour activity, e.g. adriamycin and daunohydrin.</p> |
