TAXOL DERIVATIVE AND ITS PRODUCTION

摘要

PURPOSE: To obtain the subject new compound having antineoplastic activity, and useful for treating a wide range of tumors such as breast cancer, oophoroma, lung cancer and malignant melanoma. CONSTITUTION: This new compound (or a salt thereof), a taxol derivative, is expressed by formula I (R is H or a lower alkanoyl; R<3> is a lower alkanoyl; R<4> is benzoyl; R<5> is a lower alkoxycarbonyl, etc.; X is an aryl, etc.; Y is a group freed from OH from one of the carboxyl groups in an amino acid or dipeptide; Z is O or NH; (n) is 1-6), e.g. 4α-acetoxy-13α- (2R,3S)-3-t- butoxycarbonylamino-2-[((3S)-3-amino-3-ethoxycarbonylpropionyloxy) acetoxy]-3- phenylpropionyloxy}-2α-benzoyloxy-5β, 20-epoxy-1β, 7β, 10β-trihydroxytax-11-en-9- one methanesulfonate. The compound of formula I is obtained by reaction between a compound of formula II and a compound of formula Y'-Z(CH2 )n COOH to eliminate the protecting group for the hydroxyl group.