| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new taxol derivative having excellent antitumor activity and improved water solubility, and useful as a treating agent for mammary cancer, ovarian cancer or malignant melanoma. SOLUTION: A compound of formula I [R is H or an alkanoyl; R<3> is an alkanoyl; R<4> is benzoyl; R<5> is an alkoxycarbonyl; X is an aryl, etc.; Y is a residue obtained by removing OH from the COOH of an amino acid, etc., Z is O, etc.; (n) is 1-6] or its salt, e.g. 4αacetoxy-13α- (2R,3S)-3- tbutoxycarbonylamino-2[(3S)-3benzyloxyacrbonylamino-3- ethoxycarbonylpropinoloxyacetoxyl ]-3phenylpropionyloxy}-2α-benzoyloxy-5β, 20-epoxy-1β,7β,10βtrihydroxytaxic-11-en-9-one. A compound of formula I is obtained e.g. by reacting a compound of formula II (R<1> is an alkanoyl, etc.) with a compound of formula III to obtain a compound of formula IV and subsequently reacting the obtained compound with a compound of formula V (Y' is Y, etc.). |
