| abstract |
NEW MATERIAL: An anthracycline derivative of formula I (R<1> and R<4> are each H or OH; R<2> is H or CH2 ; R<3> is COOH or OH; R<5> is R<2> or CH2 OH; R<6> is a 1-4C alkoxy, an azide, CN, 9-N-adenine, 9-N-guanine, 1-N-cytosine, 1-N-uracil or 1-N-thymine, and in cases where R<1> =OH and R<3> =COOCH3 , R<6> is H; R<5> and R<6> together form OCH2 ; R<7> and R<8> H or CN). EXAMPLE: 7-0-(3'(6"(S)-hydroxymethyl-2"(S)-methoxy-4"-morpholinyl)-2',3',6'- trideoxy-α-L-lyxohexopyranosyl)-β-rhodomycinone. USE: Antitumor agent. PROCESS: Rhodomycinone glycoside of formula II or a salt of its acid adduct is made to react with an excess amount of a dialdehyde of formula III in the presence of an alkali metal cyanoborohydride and a polar organic solvent at 10-50 deg.C to obtain a compound of formula I. |