PURPOSE: To obtain a new 4-desoxy-4-epipodopyllotoxin derivative useful for treating tumor, having excellent antitumor activity.
CONSTITUTION: A compound of formula I [R1 is H or benzyloxycarbonyl; R2 is OH, lower alkyl-substituted piperazinyl, piperidino-substituted piperidino or NR3R4 (R3 and R4 are H or substitutable lower alkyl; substituent group amino which may be substituted with lower alkyl or nitrogen-containing heterocyclic group which may be substituted with lower alkyl); n is 1-6] such as 4- desoxy-4'-dimethyl-O-benzyloxycarbonyl-4-4-(2-oxo-2-hydroxy-1-ethyl)-4- epipodophyllotoxin. A compound of formula I wherein R1 is not H and R2 is OH is obtained by reacting the compound of formula II (R5 is benzyloxycarbonyl) with the compound of formula III [R5 is (CH2)nCH-CH2], reacting the prepared compound formula IV in a proper solvent to give a compound of formula V [R8 is (CH2)nCHO] and oxidizing the compound in an inert solvent.
YAMASHITA JUNICHI
ASAO TETSUJI
BUIEJIBA KONSUTANTEI
UTSUKI TERUHIRO
YAMADA YUJI
YAMAZAKI RYOKO
YAMAGUCHI HIDEO
