Anticancer agents with low toxicity

摘要

Cpds. of formula (I) are new. In (I), R1 and R2 are both H or one of them is H and the other is OH or OMe; R3 is acetyl or 1-hydroxyethyl; R'4 is H or halo-substd. lower alkanoyl; R5 is H, OH, lower alkanoyloxy, NH2, halo-substd. lower alkanoylamino or morpholino; R6 is H, OH, lower alkanoyloxy or tetrahydropyranyloxy; R7 is H, Me, hydroxymethyl or lower alkanoyloxymethyl; R is H, OH or lower alkanoyloxy; and n is 0 or 1. - (I) are anticancer agents with low toxicity. (II) are intermediates in the prepn. of EPAB- EP-107486 B 9-Aminonaphthacene derivatives having the formula: wherein R1 and R2 are both hydrogen atoms or either one of them is a hydrogen atom and the other is hydroxy group or methoxy group; R3 is acetyl group or 1-hydroxyethyl group R4 is a hydrogen atom or halogen-substituted C1-C4 alkanoyl group, R5 is a hydrogen atom, hydroxy group, C1-C4 alkanoyloxy group, amino group, halogen-substituted C1-C4 alkanoylamino group or morpholino group, R6 is a hydrogen atom, hydroxy group, C1-C4 alkanoyloxy group or tetrahydroxypyranyloxy group, R7 is a hydrogen atom, methyl group, hydroxymethyl group or C1-C4 alkanoyloxymethyl group, R is a hydrogen atom, hydroxy group or C1-C4 alkanoyloxy group, and n is zero or one. - (29pp) - EP-107486 B Cpds. of formula (I) are new. In (I), R1 and R2 are both H or one of them is H and the other is OH or OMe; R3 is acetyl or 1-hydroxyethyl; R'4 is H or halo-substd. lower alkanoyl; R5 is H, OH, lower alkanoyloxy, NH2, halo-substd. lower alkanoylamino or morpholino; R6 is H, OH, lower alkanoyloxy or tetrahydropyranyloxy; R7 is H, Me, hydroxymethyl or lower alkanoyloxymethyl; R is H, OH or lower alkanoyloxy; and n is 0 or 1. - (I) are anticancer agents with low toxicity. (II) are intermediates in the prepn. of (I). (Dwg.0/0) USAB- US4673668 A New 9-aminonaphthacene derivs. have formula (I) in which R1 and R2 are both H and the other is OH or OMe; R3 is acetyl or 1-hydroxyethyl; R5 is H, OH, loweralkanoyloxy or NH2; R6 is H, OH or loweralkanoyloxy; R7 is H or Me. - d-7alpha-((2-deoxy-beta-D-erythro -pentapyranosyl)oxy)-9alpha -amino-9beta-acetyl -7,8,9,10-tetrahydro-6,11-dihydroxy -5,12-naphthacenedione is one specific cpd. - Cpds. (I) where R3 is acetyl are prepd. by glucosylating a cpd. of formula (II) with a saccharide deriv. in the presence of either a soluble Ag salt or a mercuric salt in a solvent comprising a halogenated alkane or an ether or a mixt. of these, followed by hydrolysis of ester gps. to yield cpd. (I).