| 摘要 |
<p>NEW MATERIAL:A compound (salt) shown by formula I [R is Lyn-NH2, group shown by formula II, Lys-OR<1> (R<1> is lower alkyl) or group shown by the formula NH(CH2)nNH2 (n is 1-6 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 alpha-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.</p> |
