PROCESS FOR PRODUCTION OF EPIPODOFILLOTOXIN GLUCOZIDES SUBSTITUATED BY FLUOR AND MEDICAL COMPOSITIONS CONTAINING THEM AS ACTIVE SUBSTANCE

摘要

The present invention provides antitumor fluoro-substituted 4'-demethylepipodophyllotoxin glucosides (I). wherein R<2> is H and R<1> is selected from the group consisting of (C1-10)alkyl; (C2-10)alkenyl; (C5-6)cycloalkyl; 2-furyl; 2-thienyl; (C6-10)aryl; (C7-14)aralkyl; and (C8-14)aralkenyl wherein each of the aromatic rings may be unsubstituted or substituted with one or more groups selected from halo, (C1-8)alkyl, (C1-8)alkoxy, hydroxy, nitro, and amino; or R<1> and R<2> are each (C1-8)alkyl; or R<1> and R<2> and the carbon to which they are attached join to form a (C5-6) cycloalkyl group; one of R<3> or R<4> is OH and the other is F; R<5> is H or a phenol protecting group; and represents an alpha - or beta -glycosidic linkage.'