PURPOSE: To obtain a compound useful as an anticancer drug simply in a high yield by a process in which an α-OH type glucosamine derivative is reacted with a specified podophyllotoxin derivative, and the product is treated specifically.

CONSTITUTION: First, an α-OH type glucosamine derivative of formula I (R1, R3 are each an acyl protective group; R2 is H; A is a 1-4C alkyl) is reacted with a podophyllotoxin derivative of formula II (R4 is CH3, a benzyloxycarbonyl protective group) at -50 to 20°C in the presence of a promotor and an anhydrous organic solvent to obtain a compound of formula III. Next, the benzyloxycarbonyl protective group is removed by hydrocracking with a palladium catalyst in an organic solvent, and acetyl protective group and a halogenated acetyl protective group are removed by zinc dichloride and a basic anion exchange resin, respectively, and free amino group is reacted with a 1-4C aldehyde under reductive alkylation conditions in the presence of hydride to obtain the objective compound in which R1 is H; R2, R3 are each H, a 1-4C alkyl; R4 is H.