4,6-0-Alkyliden-β-D-glucopyranoser til anvendelse som mellemprodukter ved fremstilling af terapeutisk værdifulde 4'-demethylepipodophyllotoxin-β-D-alkylidenglucosider og fremgangsmåde til fremstilling deraf.

摘要

Glucosides of general formula (I): R1=alkyl (C1-5). (I) have in vitro a strong cytostatic activity to mastocytoma cells and fibroblast cultures. They also have high activity against experimental tumours esp. mouse leukemia L-210. They may be used therapeutically against pathological processes connected with cell multiplication such as malignant neoplasms. R2=formyl or acetyl (II) is reacted with (III) in the presence of borontrifluoride etherate at -15 to -25 deg.C in inert solvent. The protective groups are then split off selectively, acetyl groups by reacting with zinc acetate-sodium acetate in methanol-tetrahydrofuran and formyl groups with zinc acetate in methanol. The mixture is then subjected to hydrogenolysis in the presence of ca. 0.5% of Pd.-metal catalyst at 20-40 deg.C, pref. in alcohol with 10-50% acetone.