| 摘要 |
<p>PURPOSE:To obtain a 10-[-N(omega-guanidinoacyl)-aminoacyl]-1,5,10-triazadecane derivative useful as an antitumor agent in high yield, by guanidinating a specific novel intermediate, deprotecting a protecting group. CONSTITUTION:A novel 10-[N-(omega-aminoacyl)-aminoacyl]-1,5-diprotected 1,5,10- triazadecane shown by the formula I (R1' is residue obtained by removal of one H from amino group and of OH from COOH of glycine or serine, and R1', neighboring carbonyl group and amino group form acid amide bond; R2 is amino-protecting group; m is 6-8) is guanidinated with O-methylisourea, etc. preferably at 9-11pH at room temperature - the boiling temperature of a solvent for 5-48hr, the protecting groups are removed, to give the desired compound shown by the formula II (R1 is R1'). The novel compound shown by the formula I is prepared by condensing a compound shown by the formula III (R3 is protecting group with a compound shown by the formula IV (to give a novel compound shown by the formula V, removing the protecting group R3 of the compound shown by the formula V.</p> |
