| abstract |
Anthracycline derivatives I of the formula:- <IMAGE> and salts thereof, wherein R1 = H or CH3, R2 = H or CH3, R1 = R2 = CH3 excepted, R4 = C1-C4 alkyl, R5 = H or OH, R3 = daunosaminyl, 4-epidaunosaminyl, 3,4-bis-epi-daunosaminyl or 4-deoxy-daunosaminyl or an N-trifluoroacetyl derivative thereof, may be prepared by condensing an anthracyclinone (I, R3 = R5 = H) with an appropriate trifluoroacetyl-daunosamine derivative. Any O-trifluoroacetyl group present may be removed by treatment with methanol in the presence of N(C2H5)3 and the N-trifluoroacetyl group can be removed by mild alkaline hydrolysis. The anthracycline derivatives I are useful as antitumour agents, and may be formulated as pharmaceutical compositions. |