PROCESS FOR PREPARING 4'-DEMETHYL-4-EPIPODO PHYLOTOXIN DERIVATIVES

摘要

Cpds. of formula (I) and their salts are prepd. by reacting a cpd. of formula (II) with an aldehyde of formula R-CHO or an acetal, in a solvent in the presence of an acid catalyst at -10 to 100OC for 5 mins. to 10 hrs. Any protecting gps. are then removed. In the formulas, R is lower alkyl; X1 and X2 are each OH or NH2 and when one is OH, the other is NH2; either X"1 and X"2 is opt. protected OH and the other is opt. protected NH2; Y is H or a protecting gp.. (I) have high carcinostatic activity and relatively high water solubility.