Fluoro-substituted epipodophyllotoxin glucosides

Details Fluoro-substituted epipodophyllotoxin glucosides Fluoro-substituted epipodophyllotoxin glucosides

C - Chemistry, Metallurgy

07

H

167/202, 260/228

C07H 15/26 (2006.01) A61K 31/70 (2006.01) C07H 17/04 (2006.01)

Patent

CA 1323628

ABSTRACT The present invention provides antitumor fluoro-substituted 4'- demethylepipodophyllotoxin glucosides. These compounds have the formula Image wherein R2 is H and R1 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 R1 and R2 are each (C1-8)alkyl; or R1 and R2 and the carbon to which they are attached join to form a (C5-6) cycloalkyl group; one of R3 or R4 is OH and the other is F; R5 is H or a phenol protecting group; and Image represents an .alpha.- or .beta.-glycosidic linkage.

610251

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