NEW MATERIAL:A compound (salt) shown by formula I [R is Lyn-NH2, group shown by formula II, Lys-OR1 (R1 is lower alkyl) or group shown by the formula NH(CH2)nNH2 (n is 1W6 integer)].
USE: An antitumor agent.
PREPARATION: For example, histidine ester hydrochloride and N- methylmorpholine are dissolved in dimethylformamide, etc., reacted with a compound shown by the formula Boc-Ala-OSu (Box is tertiary butoxycarbonyl; OSn is N-hydroxysuccinimide ester), converted into a hydrazide by adding a solution of hydrazine hydrate in methanol to the reaction product, then reacted with lysinamide and α-amino group is removed to give a compound shown by formula III (Z is benzyloxycarbonyl). Then, this compound is reacted with aspartic acid containing a protected functional group and the protecting group is removed to give a compound shown by formula I.
NEYA MASAHIRO
HENMI KEIJI
HASHIMOTO SHINJI
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